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Chem. Ltrs. 2(5), 407-10 (1992).","npl_type":"a","external_id":["10.1016/s0960-894x(00)80157-2"],"record_lens_id":"104-945-928-445-853","lens_id":["150-222-038-933-256","104-945-928-445-853"],"sequence":158,"category":[],"us_category":[],"cited_phase":"APP","rel_claims":[]}},{"npl":{"num":60,"text":"Halbfinger, E. et al., \"Molecular Recognition of Modified Nucleotides by the P2Y1-Receptor. 1. A Synthetic, Biochemical, and NMR Approach,\" J. Med. Chem. 1999, 42, 5325-5337.","npl_type":"a","external_id":["10639276","10.1021/jm990156d"],"record_lens_id":"099-694-635-017-908","lens_id":["106-913-505-539-993","099-694-635-017-908","150-229-066-275-15X"],"sequence":159,"category":[],"us_category":[],"cited_phase":"APP","rel_claims":[]}},{"npl":{"num":61,"text":"Han, M.J. et al., \"Polynucleotide analogs. VI. Synthesis and characterization of alternating copolymers of maleic anhydride and dihydropyran-containing guanine derivatives,\" J. of Polymer Science, Part A: Polymer Chemistry 33(11), 1829-39 (1995).","npl_type":"a","external_id":["10.1002/pola.1995.080331110"],"record_lens_id":"016-447-847-997-574","lens_id":["154-655-315-645-404","016-447-847-997-574"],"sequence":160,"category":[],"us_category":[],"cited_phase":"APP","rel_claims":[]}},{"npl":{"num":62,"text":"Hartmann et al., \"Effects of the tyrosine-kinase inhibitor gelanamycin on ligand-induced her-2/heu activation, receptor expression and proliferation of her-2-positive malignant cell lines,\" Int. J. Cancer, 1997, 70:221-229.","npl_type":"a","external_id":["10.1002/(sici)1097-0215(19970117)70:2<221::aid-ijc14>3.0.co;2-l","9009164"],"record_lens_id":"036-160-404-928-796","lens_id":["094-972-992-510-560","036-160-404-928-796","138-480-937-265-56X"],"sequence":161,"category":[],"us_category":[],"cited_phase":"APP","rel_claims":[]}},{"npl":{"num":63,"text":"Herdewijn, P. et al., \"Synthesis and Structure-Activity Relationships o Analogs of 2'-Deoxy-2'-(3-mehoxybenzamido)adenosine, a Selective Inhibitor of Trypanosomal Glycosomal lyceraldehyde-3-phosphate Dehydrogenase,\" J. Med. Chem. 1995, 38, 3838-3849.","npl_type":"a","external_id":["10.1021/jm00019a014","7562915"],"record_lens_id":"020-810-031-916-434","lens_id":["036-987-209-229-75X","020-810-031-916-434","065-910-022-005-939"],"sequence":162,"category":[],"us_category":[],"cited_phase":"APP","rel_claims":[]}},{"npl":{"num":64,"text":"Holy, A. et al., \"Structure-Antiviral Activity Relationship in the Series of Pyrimidine and Purine N-[2-(2-Phosphonomethoxy)ethyl] Nucleotide Analogues. 1. Derivatives Substituted at the Carbon Atoms of the Base,\" J. Med. Chem. 1999, 42, 2064-2086.","npl_type":"a","external_id":["10377214","10.1021/jm9811256"],"record_lens_id":"029-622-053-741-400","lens_id":["157-911-675-804-308","029-622-053-741-400","103-799-175-964-376"],"sequence":163,"category":[],"us_category":[],"cited_phase":"APP","rel_claims":[]}},{"npl":{"num":65,"text":"Holy, A. et al., \"Acyclic nucleotide analogs. VI. Synthesis of (3-hydroxy-2-phosphonylmethoxypropyl) derivatives of heterocyclic bases,\" Collection of Czechoslovak Chemical Communications 54(9), 2470-501 (1989).","npl_type":"a","external_id":["10.1135/cccc19892470"],"record_lens_id":"047-801-835-744-549","lens_id":["180-830-753-735-221","047-801-835-744-549"],"sequence":164,"category":[],"us_category":[],"cited_phase":"APP","rel_claims":[]}},{"npl":{"num":66,"text":"Hossain, N. et al., \"Synthesis of homo-N-nucleosides, a series of C1' branched-chain nucleosides,\" Tetrahedron 52(15), 5563-78 (1996).","npl_type":"a","external_id":["10.1016/0040-4020(96)00192-5"],"record_lens_id":"101-242-589-614-21X","lens_id":["186-490-740-189-575","101-242-589-614-21X"],"sequence":165,"category":[],"us_category":[],"cited_phase":"APP","rel_claims":[]}},{"npl":{"num":67,"text":"Hotoda, H. et al., \"Biologically active oligodeoxyribonucleotides. X. 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Chem. 1999, 42, 1625-1638.","npl_type":"a","external_id":["10229631","pmc6211166","10.1021/jm980657j"],"record_lens_id":"071-707-736-934-645","lens_id":["090-292-778-782-392","071-707-736-934-645","091-158-919-489-931"],"sequence":168,"category":[],"us_category":[],"cited_phase":"APP","rel_claims":[]}},{"npl":{"num":70,"text":"Janeba, Z., Collection of Czechoslovak Chemical Communications 66(9), 1393-1406 (Sep. 2001).","npl_type":"a","external_id":["10.1135/cccc20011393"],"record_lens_id":"077-511-006-419-741","lens_id":["136-457-783-308-003","077-511-006-419-741"],"sequence":169,"category":[],"us_category":[],"cited_phase":"APP","rel_claims":[]}},{"npl":{"num":71,"text":"Jeromin, G.E. et al., \"Seitenkettenchlorierungen von N-Heterocyclen mit Trichlorisocyanursaure (TCC),\" Chem. 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for invention","granted":true,"earliest_filing_date":"2004-09-20","grant_date":"2006-11-21","anticipated_term_date":"2024-11-17","has_disclaimer":false,"patent_status":"ACTIVE","publication_count":2,"has_spc":false,"has_grant_event":true,"has_entry_into_national_phase":false},"abstract":{"en":[{"text":"The present invention provides compounds represented by Formula I. R 0 is selected from hydrogen, halogen, lower alkyl, —SR 8 , —OR 8 , —CN, and —NHR 8 , R 1 is halogen, or lower alkyl; R 2 is —NHR 8 ; R 3 is selected from the group consisting of hydrogen, halogen, —SR 8 , —OR 8 , —CN, —C(O)R 9 , —C(O)OH, —NO 2 , —NR 8 R 10 , lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic and heterocyclic, all optionally substituted, and R 5 is aryl, heteroaryl, alicyclic, or heterocyclic:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"}]},"abstract_lang":["en"],"has_abstract":true,"claim":{"en":[{"text":"1. A compound represented by Formula I, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof: wherein: R 0 is selected from hydrogen, halogen, lower alkyl, —SR 8 , —OR 8 , —CN, and —NHR 8 , R 1 is halogen, or lower alkyl; R 2 is —NHR 8 ; R 3 is selected from the group consisting of hydrogen, halogen, —SR 8 , —OR 8 , —CN, —C(O)R 9 , —C(O)OH, —NO 2 , —NR 8 R 10 , lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic and heterocyclic, all optionally substituted, wherein: the aryl, heteroaryl, alicyclic and heterocyclic groups are optionally mono-, bi- or tri-cyclic, R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N, and the optional substituents on R 3 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; When R 0 or R 3 is —OH or —SH, the compound may exist as the corresponding (thio)keto tautomer or a mixture of keto-enol tautomers; R 4 is —CHR 12 —, —C(O)—, —C(S)—, —S(O)— or —SO 2 —; R 5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 3 to 5 substituents, the heteroaryl group is substituted with 2 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, the heterocyclic group is substituted with 3 to 5 substituents, and the substituents are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 8 is hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 ; R 9 is H, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, —NR 10 R 10 , or —OR 11 , wherein R 10 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 10 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl or lower heteroaryl; R 11 is lower alkyl, lower alkenyl, or lower alkynyl, lower heteroaryl or lower aryl; and R 12 is hydrogen or lower alkyl.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"2. The compound of claim 1 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein each of said aryl, heteroaryl, alicyclic or heterocyclic group is monocyclic or bicyclic.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"3. The compound of claim 1 or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 0 is hydrogen, halogen, —SH, —OH, or —CN; R 1 is halogen; and R 2 is —NHR 8 , where R 8 is hydrogen or —C(O)R 9 .","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"4. The compound of claim 1 , or a polymorph, ester, tautomer, enantiomer pharmaceutically acceptable salt or prodrug thereof, wherein: R 1 is chloro or bromo, R 2 is —NHR 8 , where R 8 is hydrogen or —C(O)R 9 ; and R 3 is hydrogen, halogen, —OR 8 , —SR 8 , —NR 8 R 10 , lower alkyl, lower alkenyl, or lower alkynyl, lower perhaloalkyl, lower aryl, or lower heteroaryl.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"5. The compound of claim 1 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 0 is hydrogen, halogen or —CN; R 2 is —NHR 8 , where R 8 is hydrogen or —C(O)R 9 ; and R 4 is —CH 2 —.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"6. The compound of claim 1 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 0 is hydrogen, halogen, —SH, —OH or —CN; R 1 is halogen; R 2 is —NH 2 ; R 3 is hydrogen, halogen, —OR 8 , —SR 8 , —NR 8 R 10 , lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, lower aryl, or lower heteroaryl, wherein R 8 is hydrogen, lower alkyl, lower aryl, or —C(O)R 9 ; R 4 is —CH 2 —; and R 5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"7. The compound of claim 6 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein R 1 is chloro or bromo, R 2 is —NH 2 , and R 5 is a phenyl having at least three substituents.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"8. The compound of claim 6 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein R 1 is chloro or bromo, R 2 is —NH 2 and R 5 is a pyridyl having at least two substituents.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"9. The compound of claim 6 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein R 1 is chloro or bromo, R 2 is —NH 2 , and R 5 is 1-oxy-pyridyl (N-oxy-pyridyl) having at least two substituents.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"10. The compound of claim 6 , wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"11. The compound of claim 6 , wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"12. The compound of claim 6 , wherein the compound is a member selected from the group of compounds below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"13. The compound of claim 6 , wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"14. The compound of claim 6 , wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"15. The compound of claim 6 , wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"16. The compound of claim 6 , wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"17. The compound of claim 6 , wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"18. The compound of claim 6 , wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"19. The compound of claim 6 , wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"20. The compound of claim 6 , wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"21. The compound of claim 6 , wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"22. The compound of claim 6 , wherein said compound is a member selected from the group below wherein Py is pyridinyl, a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"23. The compound of claim 6 , wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"24. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"25. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"26. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"27. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"28. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"29. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"30. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"31. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"32. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"33. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"34. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"35. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"36. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"37. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"38. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"39. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"40. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"41. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"42. The compound of claim 6 , wherein said compound is represented by the formula below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"43. A pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and at least one compound represented by Formula I below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof: wherein: R 0 is selected from hydrogen, halogen, lower alkyl, —SR 8 , —OR 8 , —CN, and —NHR 8 , R 1 is halogen, or lower alkyl; R 2 is —NHR 8 ; R 3 is selected from the group consisting of hydrogen, halogen, —SR 8 , —OR 8 , —CN, —C(O)R 9 , —C(O)OH, —NO 2 , —NR 8 R 10 , lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic and heterocyclic, all optionally substituted, wherein: the aryl, heteroaryl, alicyclic and heterocyclic groups are optionally mono-, bi- or tri-cyclic, R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N, and the optional substituents on R 3 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; When R 0 or R 3 is —OH or —SH, the compound may exist as the corresponding (thio)keto tautomer or a mixture of keto-enol tautomers; R 4 is —CHR 12 —, —C(O)—, —C(S)—, —S(O)— or —SO 2 —; R 5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 3 to 5 substituents, the heteroaryl group is substituted with 2 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, the heterocyclic group is substituted with 3 to 5 substituents, and the substituents are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 8 is hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 ; R 9 is H, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, —NR 10 R 10 , or —OR 11 , wherein R 10 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 10 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl or lower heteroaryl; R 11 is lower alkyl, lower alkenyl, or lower alkynyl, lower heteroaryl or lower aryl; and R 12 is hydrogen or lower alkyl.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"44. The pharmaceutical composition of claim 43 , wherein: R 0 is hydrogen, halogen, —SH, —OH, or —CN, R 1 is halogen; and R 2 is —NHR 8 , where R 8 is hydrogen or —C(O)R 9 .","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"45. The pharmaceutical composition of claim 43 , wherein: R 0 is hydrogen, halogen or —CN, R 2 is —NHR 8 , where R 8 is hydrogen or —C(O)R 9 ; and R 4 is —CH 2 —.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"46. The pharmaceutical composition of claim 43 , wherein: R 0 is hydrogen, halogen, —SH, —OH or —CN, R 1 is halogen; R 2 is —NH 2 , R 3 is hydrogen, halogen, OR 8 , SR 8 , NR 8 R 10 , lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, lower aryl, or lower heteroaryl, wherein R 8 is hydrogen, lower alkyl, lower aryl, or —C (O)R 9 ; R 4 is —CH 2 —; and R 5 is aryl or heteroaryl, wherein each of the aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"47. The pharmaceutical composition of claim 43 , wherein: R 1 is chloro or bromo; R 2 is —NH 2 ; and R 5 is a phenyl having at least three substituents, a pyridyl having at least two substituents, or 1-oxy-pyridyl (N-oxy-pyridyl), each of which has at least two substituents.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"48. A compound represented by Formula II, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof: wherein: R 0 is hydrogen, halogen, lower alkyl, —SR 8 , —OR 8 , —CN or —NHR 8 ; R 1 is halogen, or lower alkyl; R 2 is —NH 2 ; R 4 is —CHR 12 —, —C(O)—, —C(S)—, —S(O)— or —SO 2 —; R 5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein: the aryl group is substituted with 3 to 5 substituents, the heteroaryl group is substituted with 2 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, the heterocyclic group is substituted with 3 to 5 substituents, and the substituents on R 5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 ; R 9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR 10 R 10 , or —OR 11 , wherein R 10 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl; R 11 is lower alkyl, lower alkenyl, or lower alkynyl, lower heteroaryl or lower aryl; R 12 is hydrogen or lower alkyl; and R 0 and R 10 taken together optionally form an exocyclic double bond which is optionally substituted, or optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"49. The compound of claim 48 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 1 is halogen or lower alkyl; R 4 is —CHR 12 —; and R 5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"50. The compound of claim 49 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein R 0 is hydrogen or —NHR 8 ; R 1 is halogen, or lower alkyl; R 10 is hydrogen or lower alkyl.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"51. The compound of claim 49 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 0 is hydrogen; R 1 is halogen; R 4 is —CH 2 —; R 5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents; and R 10 is hydrogen.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"52. The compound of claim 51 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 1 is chloro or bromo; R 5 is phenyl, pyridyl or 1-oxy-pyridyl (N-oxy-pyridyl), each R 5 has at least two substituents.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"53. The compound of claim 51 , wherein said compound is a member selected from the group below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"54. The compound of claim 51 , wherein said compound is a member selected from the group below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"55. The compound of claim 51 , wherein said compound is a member selected from the group below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"56. The compound of claim 51 , wherein said compound is a member selected from the group below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"57. A pharmaceutical composition comprising one or more pharmaceutical acceptable excipients and at least one compound represented by Formula II below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof: wherein: R 0 is hydrogen, halogen, lower alkyl, —SR 8 , —OR 8 , —CN or —NHR 8 ; R 1 is halogen, or lower alkyl; R 2 is —NH 2 ; R 4 is —CHR 12 —, —C(O)—, —C(S)—, —S(O)— or —SO 2 —; R 5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein: the aryl group is substituted with 3 to 5 substituents, the heteroaryl group is substituted with 2 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, the heterocyclic group is substituted with 3 to 5 substituents, and the substituents on R 5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 . R 9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR 10 R 10 , or —OR 11 , wherein R 10 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl, R 11 is lower alkyl, lower alkenyl, lower alkynyl, lower heteroaryl or lower aryl; R 12 is hydrogen or lower alkyl; and R 0 and R 10 taken together optionally form an exocyclic double bond which is optionally substituted, or optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"58. A compound represented by Formula III, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof: wherein: R 1 is halogen, or lower alkyl; R 2 is —NH 2 ; R 3 is selected from the group consisting of hydrogen, halogen, —SR 8 , —OR 8 , —CN, —C(O)R 9 , —C(O)OH, —NO 2 , —NR 8 R 10 , lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic, heterocyclic, all optionally substituted, wherein: the aryl, heteroaryl, alicyclic and heterocyclic groups are optionally mono-, bi- or tri-cyclic, R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N, and the optional substituents on R 3 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 and R 10 with the N to which they are attached together optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 4 is —CHR 12 —, —C(O)—, —C(S)—, —S(O)— or —SO 2 —; R 5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 3 to 5 substituents, the heteroaryl group is substituted with 2 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, the heterocyclic group is substituted with 3 to 5 substituents, and the substituents on R 5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 ; R 9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR 10 R 10 , or —OR 11 , wherein R 10 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl, R 11 is lower alkyl, lower alkenyl, lower alkynyl, lower heteroaryl or lower aryl; R 12 is hydrogen or lower alkyl; and R 3 and R 10 taken together optionally form an exocyclic double bond which is optionally substituted, or optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"59. The compound of claim 58 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 1 is halogen; R 3 is hydrogen, halogen, —OR 8 , —SR 8 , —NR 8 R 10 , lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, lower aryl, or lower heteroaryl, wherein R 8 is hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 ; R 4 is —CH 2 —; R 5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents, and R 10 is hydrogen or lower alkyl.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"60. The compound of claim 58 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 1 is halogen; R 4 is —CH 2 —; R 5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents; and R 10 is hydrogen.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"61. The compound of claim 58 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 1 is halogen; R 3 is hydrogen; R 4 is —CH 2 —; R 5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents; and R 10 is hydrogen.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"62. The compound of claim 61 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 1 is chloro or bromo; and R 5 is phenyl, pyridyl or 1-oxy-pyridyl (N-oxy-pyridyl), wherein each R 5 has at least two substituents.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"63. A pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and at least one compound represented by Formula III below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof: wherein: R 1 is halogen, or lower alkyl; R 2 is —NH 2 ; R 3 is selected from the group consisting of hydrogen, halogen, —SR 8 , —OR 8 —CN, —C(O)R 9 , —C(O)OH, —NO 2 , —NR 8 R 10 , lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic, heterocyclic, all optionally substituted, wherein: the aryl, heteroaryl, alicyclic and heterocyclic groups are optionally mono-, bi- or tri-cyclic, R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N, and the optional substituents on R 3 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 4 is —CHR 12 —, —C(O)—, —C(S)—, —S(O)— or —SO 2 —; R 5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 3 to 5 substituents, the heteroaryl group is substituted with 2 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, the heterocyclic group is substituted with 3 to 5 substituents, and the substituents on R 5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 and —NR 8 R 10 lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 ; R 9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR 10 R 10 , or —OR 11 , wherein R 10 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl, R 11 is lower alkyl, lower alkenyl, lower alkynyl, lower heteroaryl or lower aryl; R 12 is hydrogen or lower alkyl; and R 3 and R 10 taken together optionally form an exocyclic double bond which is optionally substituted, or optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"64. A compound represented by Formula IV, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof: wherein: R 1 is halogen, or lower alkyl; R 2 is —NH 2 ; R 4 is —CHR 12 —, —C(O)—, —C(S)—, —S(O)— or —SO 2 —; R 5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 3 to 5 substituents, the heteroaryl group is substituted with 2 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, the heterocyclic group is substituted with 3 to 5 substituents, and the substituents on R 5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 ; R 9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR 10 R 10 , or —OR 11 , wherein R 10 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl, R 11 is lower alkyl, lower alkenyl, lower alkynyl, lower heteroaryl or lower aryl; and R 12 is hydrogen or lower alkyl.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"65. The compound of claim 64 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 1 is halogen; R 4 is —CH 2 —; and R 5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"66. The compound of claim 65 , or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein R 1 is chloro or bromo, R 5 is phenyl, pyridyl or 1-oxy-pyridyl (N-oxy-pyridyl), wherein each R 5 has at least two substituents.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"67. A pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and at least one compound represented by Formula IV below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof: wherein: R 1 is halogen, or lower alkyl; R 2 is —NH 2 ; R 4 is —CHR 12 —, —C(O)—, —C(S)—, —S(O)— or —SO 2 —; R 5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 3 to 5 substituents, the heteroaryl group is substituted with 2 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, the heterocyclic group is substituted with 3 to 5 substituents, and the substituents on R 5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 and —NR 8 R 10 lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 ; R 9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR 10 R 10 , or —OR 11 , wherein R 10 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; R 10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl, R 11 is lower alkyl, lower alkenyl, lower alkynyl, lower heteroaryl or lower aryl; and R 12 is hydrogen or lower alkyl.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"},{"text":"68. The compound of claim 6 , wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"}]},"claim_lang":["en"],"has_claim":true,"description":{"en":{"text":"This application relates and claims priority to U.S. Provisional Application Ser. No. 60/504,135, filed Sep. 18, 2003, and U.S. Provisional Application Ser. No. 60/591,467, filed Jul. 26, 2004. This application also relates to three other U.S. Utility Applications Ser. No. 10/946,645 filed Sep. 20, 2004 (now Publication No. 20050113340; 10/946,637 filed Sep. 20, 2004 (now Publication No. Ser. No. 20050119282) and Ser. No. 10/946,628 filed Sep. 20, 2004 (now Publication No. 20050113339. This application further relates to International Application PCT/US02/35069, filed Oct. 30, 2002 (now Publication No. WO03/37860). All the above cited U.S. utility applications, provisional applications and international application are expressly incorporated herein by reference in their entirety. FIELD OF THE INVENTION The invention relates in general to pyrrolopyrimidines and their broad-spectrum utility, e.g., in inhibiting heat shock protein 90 (HSP90) to thereby treat or prevent HSP90-mediated diseases. BACKGROUND HSP90s are ubiquitous chaperone proteins that are involved in folding, activation and assembly of a wide range of proteins, including key proteins involved in signal transduction, cell cycle control and transcriptional regulation. Researchers have reported that HSP90 chaperone proteins are associated with important signaling proteins, such as steroid hormone receptors and protein kinases, including, e.g., Raf-1, EGFR, v-Src family kinases, Cdk4, and ErbB-2 (Buchner J. TIBS 1999, 24, 136–141; Stepanova, L. et al. Genes Dev. 1996, 10, 1491–502; Dai, K. et al. J. Biol. Chem. 1996, 271, 22030–4). Studies further indicate that certain co-chaperones, e.g., HSP70, p60/Hop/Sti1, Hip, Bag1, HSP40/Hdj2/Hsj1, immunophilins, p23, and p50, may assist HSP90 in its function (see, e.g., Caplan, A. Trends in Cell Biol. 1999, 9, 262–68). Ansamycin antibiotics, e.g., herbimycin A (HA), geldanamycin (GM), and 17-alkylaminogeldanamycin (17-AAG) are thought to exert their anticancerous effects by tight binding of the N-terminus pocket of HSP90, thereby destabilizing substrates that normally interact with HSP90 (Stebbins, C. et al. Cell 1997, 89, 239–250). This pocket is highly conserved and has weak homology to the ATP-binding site of DNA gyrase (Stebbins, C. et al., supra; Grenert, J. P. et al. J. Biol. Chem. 1997, 272, 23843–50). Further, ATP and ADP have both been shown to bind this pocket with low affinity and to have weak ATPase activity (Proromou, C. et al. Cell 1997, 90, 65–75; Panaretou, B. et al. EMBO J. 1998, 17, 4829–36). In vitro and in vivo studies have demonstrated that occupancy of this N-terminal pocket by ansamycins and other HSP90 inhibitors alters HSP90 function and inhibits protein folding. At high concentrations, ansamycins and other HSP90 inhibitors have been shown to prevent binding of protein substrates to HSP90 (Scheibel, T. H. et al. Proc. Natl. Acad. Sci. USA 1999, 96, 1297–302; Schulte, T. W. et al. J. Biol. Chem. 1995, 270, 24585–8; Whitesell, L., et al. Proc. Natl. Acad. Sci. USA 1994, 91, 8324–8328). Ansamycins have also been demonstrated to inhibit the ATP-dependent release of chaperone-associated protein substrates (Schneider, C. L. et al. Proc. Natl. Acad. Sci., USA 1996, 93, 14536–41; Sepp-Lorenzino et al. J. Biol. Chem. 1995, 270, 16580–16587). In either event, the substrates are degraded by a ubiquitin-dependent process in the proteasome (Schneider, C. L., supra; Sepp-Lorenzino, L., et al. J. Biol. Chem. 1995, 270, 16580–16587; Whitesell, L. et al. Proc. Natl. Acad. Sci. USA 1994, 91, 8324–8328). HSP90 substrate destabilization occurs in tumor and non-transformed cells alike and has been shown to be especially effective on a subset of signaling regulators, e.g., Raf (Schulte, T. W. et al. Biochem. Biophys. Res. Commun. 1997, 239, 655–9; Schulte, T. W., et al. J. Biol. Chem. 1995, 270, 24585–8), nuclear steroid receptors (Segnitz, B.; U. Gehring J. Biol. Chem. 1997, 272, 18694–18701; Smith, D. F. et al. Mol. Cell. Biol. 1995, 15, 6804–12), v-Src (Whitesell, L., et al. Proc. Natl. Acad. Sci. USA 1994, 91, 8324–8328) and certain transmembrane tyrosine kinases (Sepp-Lorenzino, L. et al. J. Biol. Chem. 1995, 270, 16580–16587) such as EGF receptor (EGFR) and HER2/Neu (Hartmann, F., et al. Int. J. Cancer 1997, 70, 221–9; Miller, P. et al. Cancer Res. 1994, 54, 2724–2730; Mimnaugh, E. G., et al. J. Biol. Chem. 1996, 271, 22796–801; Schnur, R. et al. J. Med. Chem. 1995, 38, 3806–3812), CDK4, and mutant p53. Erlichman et al. Proc. AACR 2001, 42, abstract 4474. The ansamycin-induced loss of these proteins leads to the selective disruption of certain regulatory pathways and results in growth arrest at specific phases of the cell cycle (Muise-Heimericks, R. C. et al. J. Biol. Chem. 1998, 273, 29864–72), and apoptosis, and/or differentiation of cells so treated (Vasilevskaya, A. et al. Cancer Res., 1999, 59, 3935–40). Ansamycins thus hold great promise for the treatment and/or prevention of many types of cancers and proliferative disorders, and also hold promise as traditional antibiotics. However, their relative insolubility makes them difficult to formulate and administer, and they are not easily synthesized and currently must, at least in part, be generated through fermentation. Further, the hepatic toxicity of ansamyins is dose limiting. In addition to anti-cancer and antitumorgenic activity, HSP90 inhibitors have also been implicated in a wide variety of other utilities, including use as anti-inflammation agents, anti-infectious disease agents, agents for treating autoimmunity, agents for treating stroke, ischemia, multiple sclerosis, cardiac disorders, central nervous system related disorders and agents useful in promoting nerve regeneration (See, e.g., Rosen et al. WO 02/09696 (PCT/US01/23640); Degranco et al. WO 99/51223 (PCT/US99/07242); Gold, U.S. Pat. No. 6,210,974 B1; DeFranco et al., U.S. Pat. No. 6,174,875. Overlapping somewhat with the above, there are reports in the literature that fibrogenetic disorders including but not limited to scleroderma, polymyositis, systemic lupus, rheumatoid arthritis, liver cirrhosis, keloid formation, interstitial nephritis, and pulmonary fibrosis also may be treatable with HSP90 inhibitors. Strehlow, WO 02/02123 (PCT/US01/20578). Still further HSP90 modulation, modulators and uses thereof are reported in Application Nos. PCT/US03/04283, PCT/US02/35938, PCT/US02/16287, PCT/US02/06518, PCT/US98/09805, PCT/US00/09512, PCT/US01/09512, PCT/US01/23640, PCT/US01/46303, PCT/US01/46304, PCT/US02/06518, PCT/US02/29715, PCT/US02/35069, PCT/US02/35938, PCT/US02/39993, 60/293,246, 60/371,668, 60/335,391, 60/128,593, 60/337,919, 60/340,762, 60/359,484 and 60/331,893. Recently, purine derivatives showing HSP90 inhibitory activity have been reported, e.g., in PCT/US02/35069; PCT/US02/36075. Purine moieties are well accepted bioisosteres for a variety of ATP-dependent molecular targets, see, JP 10025294; U.S. Pat. No. 4,748,177; U.S. Pat. No. 4,772,606; U.S. Pat. No. 6,369,092; WO 00/06573; WO 02/055521; WO 02/055082; WO 02/055083; European Patent 0178178 ; Eur. J. Med. Chem. 1994, 29(1), 3–9; and J. Het. Chem. 1990, 27(5), 1409. However, compounds having the desired potency, selectivity and pharmaceutical properties required for effective HSP90 inhibition in vivo have not been reported. Therefore, a need remains for additional novel and potent HSP90 inhibitors that meet the demanding biological and pharmaceutical criteria required to proceed towards human clinical trials. SUMMARY OF THE INVENTION The present invention is directed towards heterocyclic compounds, in particular, pyrrolopyrimidines and related compounds that show broad utility, e.g., by inhibiting HSP90 and treating diseases that are HSP90-dependent. In one aspect, the invention comprises heterocyclic compounds as specified below in Formulae A, I, II, III and IV. Also included in the scope of the present invention are stereoisomic forms, including the individual enantiomers and diastereomers, racemic mixtures, and diasteromeric mixtures, and combinations thereof, where appropriate, as well as polymorphs, specific racemates and stereoisomers, solvates, esters, tautomers, pharmaceutically acceptable salts and prodrugs of these compounds. Stereoisomers of the compounds of the present invention may be isolated by standard resolution techniques such as, for example, fractional crystallization and chiral column chromatography. In one embodiment, the invention provides compounds of Formula A, or a polymorph, solvate, ester, tautomer, diastereomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, which show utility by inhibiting HSP90 and treating and preventing diseases that are HSP90-dependent. wherein: X 1 and X 2 are the same or different and each is nitrogen or —CR 6 ;X 3 is nitrogen or —CR 3 wherein R 3 is hydrogen, OH, a keto tautomer, —OR 8 , —CN, halogen, lower alkyl, or —C(O)R 9 ;X 4 is nitrogen or —CR 6 when X 3 is nitrogen, and X 4 is —CR 6 R 7 when X 3 is —CR 3 ;R 1 is halogen, —OR 8 , —SR 8 , or lower alkyl;R 2 is —NR 8 R 10 ;R 4 is —(CH 2 ) n — wherein n=0–3, —C(O), —C(S), —SO 2 —, or —SO 2 N—; andR 5 is alkyl, aromatic, heteroaromatic, alicyclic, or heterocyclic, each of which is optionally bi- or tri-cyclic, and optionally substituted with H, halogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower alicyclic, aralkyl, aryloxyalkyl, alkoxyalkyl, perhaloalkyl, perhaloalkyloxy, perhaloacyl, —N 3 , —SR 8 , —OR 8 , —CN, —CO 2 R 9 , —NO 2 , or —NR 8 R 10 . In certain embodiments, there are exclusionary provisos with respect to compounds disclosed in JP 10025294; U.S. Pat. No. 4,748,177; U.S. Pat. No. 4,748,177; U.S. Pat. No. 6,369,092; WO 00/06573; WO 02/055521; WO 02/055082; WO 02/055083 ; Eur. J. Med. Chem. 1994, 29(1), 3–9; and J. Het. Chem. 1990, 27(5), 1409, which disclose compounds with, —R 4 R 5 comprising ribose or a derivative thereof, or a sugar or derivative thereof; and compounds where —R 4 R 5 is a phosphonate or phosphonic acid, or is substituted with a phosphonate or phosphonic acid; or compounds connected where R 4 is —CH 2 — or —(CH 2 ) n — that are connected through an oxygen atom to another group. In another embodiment, the invention features compounds of Formulae I, II, III, & IV: or a polymorph, solvate, ester, diastereomer, enantiomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 0 is selected from hydrogen, halogen, lower alkyl, —SR 8 , —OR 8 , —CN, and —NHR 8 ,R 1 is halogen, —OR 11 , —SR 11 or lower alkyl;R 2 is —NHR 8 ;R 3 is selected from the group consisting of hydrogen, halogen, —SR 8 , —OR 8 , —CN, —C(O)R 9 , —C(O)OH, —NO 2 , —NR 8 R 10 , lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic, and heterocyclic, all optionally substituted, wherein: the aryl, heteroaryl, alicyclic and heterocyclic groups are optionally mono-, bi- or tri-cyclic;R 8 and R 10 taken together optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; andthe optional substituents on R 3 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;when R 0 or R 3 is —OH or —SH, the compound may exist as the corresponding (thio)keto tautomer or a mixture of keto-enol tautomers;R 4 is —CHR 12 —, —C(O)—, —C(S)—, —S(O)— or —SO 2 —;R 5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein: the aryl group is substituted with 3 to 5 substituents,the heteroaryl group is substituted with 2 to 5 substituents,the alicyclic group is substituted with 3 to 5 substituents,the heterocyclic group is substituted with 3 to 5 substituents, andthe substituents are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 and R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;R 8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 ;R 9 is H, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, —NR 10 R 10 , or —OR 11 , wherein R 10 and R 10 taken together optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;R 10 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl or lower heteroaryl;R 11 is lower alkyl, lower alkenyl, lower alkynyl, lower heteroaryl or lower aryl;R 12 is hydrogen or lower alkyl;R 0 and R 10 taken together optionally form an exocyclic double bond which is optionally substituted, or optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N; andR 3 and R 10 taken together optionally form an exocyclic double bond which is optionally substituted, or optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N. In another aspect, the invention features pharmaceutical compositions comprising the compounds of the invention, in particular, the compounds of Formulae A, I, II, III or IV, or a polymorph, solvate, ester, tautomer, diastereoisomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, and one or more pharmaceutical excipients, for use in treatment or prevention of diseases that are HSP90-dependent. In another aspect, the invention features a method of treating an individual having an HSP90-mediated disorder by administering to the individual a pharmaceutical composition that comprises a pharmaceutically effective amount of a compound of Formula A, I, II, III or IV, or a polymorph, solvate, ester, tautomer, diastereomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof. In one embodiment, the invention provides a method for treating an individual having a disorder selected from the group of inflammatory diseases, infections, autoimmune disorders, stroke, ischemia, cardiac disorders, neurological disorders, fibrogenetic disorders, proliferative disorders, tumors, leukemias, neoplasms, cancers, carcinomas, metabolic diseases, and malignant diseases. In another embodiment, the invention provides a method for treating an individual having a fibrogenetic disorder, such as, for example, scleroderma, polymyositis, systemic lupus, rheumatoid arthritis, liver cirrhosis, keloid formation, interstitial nephritis or pulmonary fibrosis. In another embodiment, the invention provides a combination therapy comprising the administration of a pharmaceutically effective amount of a compound of Formula I, II, III, or IV, or a solvate, tautomer, diastereomer, enantiomer, pharmaceutically acceptable salt, polymorph, or prodrug thereof according to any of the preceding aspects or embodiments, and at least one therapeutic agent selected from the group of cytotoxic agents, anti-angiogenesis agents and anti-neoplastic agents. The anti-neoplastic agent may be selected from the group of alkylating agents, anti-metabolites, epidophyllotoxins antineoplastic enzymes, topoisomerase inhibitors, procarbazines, mitoxantrones, platinum coordination complexes, biological response modifiers and growth inhibitors, hormonal/anti-hormonal therapeutic agents, and haematopoietic growth factors. Any of the above described aspects and embodiments of the invention can be combined where practical. The individual compounds, methods and compositions prescribed do not preclude the utilization of other, unspecified steps and agents, and those of ordinary skill in the art will appreciate that additional steps and compounds may also be combined usefully within the spirit of various aspects and embodiments of the invention. Advantages of the invention depend on the specific aspect and embodiment and may include one or more of: ease of synthesis and/or formulation, solubility, and IC 50 relative to previously existing compounds in the same or different classes of HSP90 inhibitors. DETAILED DESCRIPTION OF THE INVENTION I. Definitions A “pharmaceutically acceptable derivative or prodrug” means any pharmaceutically acceptable salt, ester, salt of an ester or other derivative of a compound of this invention, which, upon administration to a recipient, is capable of providing, either directly or indirectly, a compound of this invention or a pharmaceutically active metabolite or residue thereof. Particularly favored derivatives or prodrugs are those that increase the bioavailability of the compounds of this invention when such compounds are administered to a patient (e.g., by allowing orally administered compound to be more readily absorbed into blood) or which enhance delivery of the parent compound to a biological compartment (e.g., the brain or lymphatic system). A “pharmaceutically acceptable salt” may be prepared for any compound of the invention having a functionality capable of forming a salt, for example, an acid or base functionality. Pharmaceutically acceptable salts may be derived from organic or inorganic acids and bases. Compounds of the invention that contain one or more basic functional groups, e.g., amino or alkylamino, are capable of forming pharmaceutically acceptable salts with pharmaceutically acceptable organic and inorganic acids. These salts can be prepared in situ during the final isolation and purification of the compounds of the invention, or by separately reacting a purified compound of the invention in its free base form with a suitable organic or inorganic acid, and isolating the salt thus formed. Examples of suitable acid salts include acetate, adipate, alginate, aspartate, benzoate, benzenesulfonate, bisulfate, butyrate, citrate, camphorate, camphorsulfonate, cyclopentanepropionate, digluconate, dodecylsulfate, ethanesulfonate, formate, fumarate, glucoheptanoate, glycerophosphate, glycolate, hemisulfate, heptanoate, hexanoate, hydrochloride, hydrobromide, hydroiodide, 2-hydroxyethanesulfonate, lactate, maleate, malonate, methanesulfonate, 2-napthalenesulfonate, nicotinate, nitrate, oxalate, palmoate, pectinate, persulfate, 3-phenylpropionate, phosphate, picrate, pivalate, propionate, salicylate, succinate, sulfate, tartrate, thiocyanate, tosylate and undecanoate. Other acids, such as oxalic, while not in themselves pharmaceutically acceptable, may be employed in the preparation of salts useful as intermediates in obtaining the compounds of the invention and their pharmaceutically acceptable acid addition salts. See, e.g., Berge et al. “Pharmaceutical Salts”, J. Pharm. Sci. 1977, 66:1–19. Compounds of the present invention that contain one or more acidic functional groups are capable of forming pharmaceutically acceptable salts with pharmaceutically acceptable bases. The term “pharmaceutically acceptable salts” in these instances refers to the relatively non-toxic, inorganic and organic base addition salts of compounds of the present invention. These salts can likewise be prepared in situ during the final isolation and purification of the compounds, or by separately reacting the purified compound in its free acid form with a suitable base, such as the hydroxide, carbonate or bicarbonate of a pharmaceutically acceptable metal cation, with ammonia, or with a pharmaceutically acceptable organic primary, secondary or tertiary amine. Representative pharmaceutically acceptable cations include alkali or alkaline earth salts such as the lithium, sodium, potassium, calcium, magnesium, and aluminum salts and the like. Illustrative examples of some of the bases that can be used include sodium hydroxide, potassium hydroxide, choline hydroxide, sodium carbonate, N + (C 1-4 alkyl) 4 , and the like. Representative organic amines useful for the formation of base addition salts include ethylamine, diethylamine, ethylenediamine, ethanolamine, diethanolamine, piperazine and the like. This invention also envisions the quaternization of any basic nitrogen-containing groups of the compounds disclosed herein. Water or oil-soluble or dispersible products may be obtained by such quaternization. See, for example, Berge et al., supra. Pharmaceutically acceptable prodrugs of the compounds of this invention include, but are not limited to, esters, carbonates, thiocarbonates, N-acyl derivatives, N-acyloxyalkyl derivatives, quaternary derivatives of tertiary amines, N-Mannich bases, Schiff bases, aminoacid conjugates, phosphate esters, metal salts and sulfonate esters. Suitable positions for derivatization of the compounds of the invention to create “prodrugs” include but are not limited, to, 2-amino substitution. Those of ordinary skill in the art have the knowledge and means to accomplish this without undue experimentation. Various forms of prodrugs are well known in the art. For examples of such prodrug derivatives, see, e.g., a) Design of Prodrugs , Bundgaard, A. Ed., Elsevier, 1985 and Method in Enzymology , Widder, K. et al., Ed.; Academic, 1985, vol. 42, p. 309–396; b) Bundgaard, H. “Design and Application of Prodrugs” in A Textbook of Drug Design and Development , Krosgaard-Larsen and H. Bundgaard, Ed., 1991, Chapter 5, p. 113–191; and c) Bundgaard, H., Advanced Drug Delivery Review, 1992, 8, 1–38. Each of which is incorporated herein by reference. The term “prodrugs” as employed herein includes, but is not limited to, the following groups and combinations of these groups: Hydroxy Prodrugs: Acyloxyalkyl esters;Alkoxycarbonyloxyalkyl esters;Alkyl esters;Aryl esters; andDisulfide containing esters. The term “alkyl,” alone or in combination, refers to an optionally substituted straight-chain, or optionally substituted branched-chain saturated hydrocarbon radical having from one to thirty carbons, more preferably one to twelve carbons. Examples of alkyl radicals include methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, tert-amyl, pentyl, hexyl, heptyl, octyl and the like. The term “cycloalkyl” embraces cyclic alkyl radicals which include monocyclic, bicyclic, tricyclic, and higher multicyclic alkyl radicals wherein each cyclic moiety has from three to eight carbon atoms. Examples of cycloalkyl radicals include cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and the like. A “lower alkyl” is a shorter alkyl, e.g., one containing from one to six carbon atoms. The term “alkenyl,” alone or in combination, refers to an optionally substituted straight-chain, or optionally substituted branched-chain hydrocarbon radical having one or more carbon-carbon double-bonds and having from two to thirty carbon atoms, more preferably two to eighteen carbons. Examples of alkenyl radicals include ethenyl, propenyl, butenyl, 1,3-butadienyl and the like. The term “cycloalkenyl” refers to cyclic alkenyl radicals which include monocyclic, bicyclic, tricyclic, and higher multicyclic alkenyl radicals wherein each cyclic moiety has from three to eight carbon atoms. A “lower alkenyl” refers to an alkenyl having from two to six carbons. The term “alkynyl,” alone or in combination, refers to an optionally substituted straight-chain or optionally substituted branched-chain hydrocarbon radical having one or more carbon-carbon triple-bonds and having from two to thirty carbon atoms, more preferably from two to twelve carbon atoms, or from two to six carbon atoms, as well as those having from two to four carbon atoms. Examples of alkynyl radicals include ethynyl, 2-propynyl, 2-butynyl, 1,3-butadiynyl and the like. The term “cycloalkynyl” refers to cyclic alkynyl radicals which include monocyclic, bicyclic, tricyclic, and higher multicyclic alkynyl radicals wherein each cyclic moiety has from three to eight carbon atoms. A “lower alkynyl” refers to an alkynyl having from two to six carbons. The terms “heteroalkyl, heteroalkenyl and heteroalkynyl” include optionally substituted alkyl, alkenyl and alkynyl structures, as described above, and which have one or more skeletal chain atoms selected from an atom other than carbon, e.g., oxygen, nitrogen, sulfur, phosphorous or combinations thereof. The term “carbon chain” embraces any alkyl, alkenyl, alkynyl, or heteroalkyl, heteroalkenyl, or heteroalkynyl group, which are linear, cyclic, or any combination thereof. If the chain is part of a linker and that linker comprises one or more rings as part of the core backbone, for purposes of calculating chain length, the “chain” only includes those carbon atoms that compose the bottom or top of a given ring and not both, and where the top and bottom of the ring(s) are not equivalent in length, the shorter distance shall be used in determining the chain length. If the chain contains heteroatoms as part of the backbone, those atoms are not calculated as part of the carbon chain length. The term “membered ring” can embrace any cyclic structure, including aromatic, heteroaromatic, alicyclic, heterocyclic and polycyclic fused ring systems as described below. The term “membered” is meant to denote the number of skeletal atoms that constitute the ring. Thus, for example, pyridine, pyran, and pyrimidine are six-membered rings and pyrrole, tetrahydrofuran, and thiophene are five-membered rings. The term “aryl,” alone or in combination, refers to an optionally substituted aromatic hydrocarbon radical of six to about twenty ring atoms, and includes mono-aromatic rings and fused aromatic rings. A fused aromatic ring radical contains from two to four fused rings where the ring of attachment is an aromatic ring, and the other individual rings within the fused ring may be aromatic, heteroaromatic, alicyclic or heterocyclic. Further, the term aryl includes mono-aromatic rings and fused aromatic rings containing from six to twelve carbon atoms, as well as those containing from six to ten carbon atoms. Examples of aryl groups include, without limitation, phenyl, naphthyl, anthryl, chrysenyl, and benzopyrenyl ring systems. The term “lower aryl” refers to an aryl having six to ten skeletal ring carbons, e.g., phenyl and naphthyl ring systems. The term “heteroaryl” refers to optionally substituted aromatic radicals containing from five to twenty skeletal ring atoms and where one or more of the ring atoms is a heteroatom such as, for example, oxygen, nitrogen, sulfur, selenium or phosphorus. The term heteroaryl includes optionally substituted mono-heteroaryl radicals and fused heteroaryl radicals having at least one heteroatom (e.g., quinoline, benzothiazole). A fused heteroaryl radical may contain from two to four fused rings where the ring of attachment is a heteroaromatic ring, the other individual rings within the fused ring system may be aromatic, heteroaromatic, alicyclic or heterocyclic. The term heteroaryl also includes mono-heteroaryls or fused heteroaryls having from five to twelve skeletal ring atoms, as well as those having from five to ten skeletal ring atoms. Examples of heteroaryls include, without limitation, furanyl, benzofuranyl, chromenyl, pyridyl, pyrrolyl, indolyl, quinolinyl, pyridyl-N-oxide, pyrimidyl, pyrazinyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, benzothiozole, benzimidazole, benzoxazoles, benzothiadiazole, benzoxadiazole, benzotriazole, quinolines, isoquinolines, indoles, purinyl, indolizinyl, thienyl and the like and their oxides. The term “lower heteroaryl” refers to a heteroaryl having five to ten skeletal ring atoms, e.g., pyridyl, thienyl, pyrimidyl, pyrazinyl, pyrrolyl, or furanyl. The term “alicyclic” alone or in combination, refers to an optionally substituted saturated or unsaturated nonaromatic hydrocarbon ring system containing from three to twenty ring atoms. The term alicyclic includes mono-alicyclic and fused alicyclic radicals. A fused alicyclic may contain from two to four fused rings where the ring of attachment is an alicyclic ring, and the other individual rings within the fused-alicyclic radical may be aromatic, heteroaromatic, alicyclic and heterocyclic. The term alicyclic also includes mono-alicyclic and fused alicyclic radicals containing from three to twelve carbon atoms, as well as those containing from three to ten carbon atoms. Examples of alicyclics include, without limitation, cyclopropyl, cyclopropenyl, cyclobutyl, cyclopentyl, cyclodecyl, cyclododecyl, cyclopentadienyl, indanyl, and cyclooctatctraenyl ring systems. The term “lower alicyclic” refers to an alicyclic having three to ten skeletal ring carbons, e.g., cyclopropyl, cyclopropenyl, cyclobutyl, cyclopentyl, decalinyl, and cyclohexyl. The term “heterocyclic” refers to optionally substituted saturated or unsaturated nonaromatic ring radicals containing from five to twenty ring atoms where one or more of the ring atoms are heteroatoms such as, for example, oxygen, nitrogen, sulfur, and phosphorus. The term alicyclic includes mono-heterocyclic and fused heterocyclic ring radicals. A fused heterocyclic radical may contain from two to four fused rings where the attaching ring is a heterocyclic, and the other individual rings within the fused heterocyclic radical may be aromatic, heteroaromatic, alicyclic or heterocyclic. The term heterocyclic also includes mono-heterocyclic and fused alicyclic radicals having from five to twelve skeletal ring atoms, as well as those having from five to about ten skeletal ring atoms. Example of heterocyclics include without limitation, tetrahydrofuranyl, benzodiazepinyl, tetrahydroindazolyl, dihyroquinolinyl, and the like. The term “lower heterocyclic” refers to a heterocyclic ring system having five to ten skeletal ring atoms, e.g., dihydropyranyl, pyrrolidinyl, dioxolanyl, piperidinyl, piperazinyl, and the like. The term “alkylaryl,” or “aralkyl,” alone or in combination, refers to an aryl radical as defined above in which at least one H atom is replaced by an alkyl radical as defined above, such as, for example, tolyl, xylyl and the like. The term “arylalkyl,” alone or in combination, refers to an alkyl radical as defined above in which at least one H atom is replaced by an aryl radical as defined above, such as, for example, benzyl, 2-phenylethyl and the like. The term “heteroarylalkyl” refers to an alkyl radical as defined above in which at least one H atom is replaced by a heteroaryl radical as defined above, each of which may be optionally substituted. The term “alkoxy,” alone or in combination, refers to an alkyl ether radical, alkyl-O—, wherein the term alkyl is defined as above. Examples of alkoxy radicals include methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, iso-butoxy, sec-butoxy, tert-butoxy and the like. The term “aryloxy,” alone or in combination, refers to an aryl ether radical wherein the term aryl is defined as above. Examples of aryloxy radicals include phenoxy, thienyloxy and the like. The term “alkylthio,” alone or in combination, refers to an alkyl thio radical, alkyl-S—, wherein the term alkyl is as defined above. The term “arylthio,” alone or in combination, refers to an aryl thio radical, aryl-S—, wherein the term aryl is as defined above. The term “heteroarylthio” refers to the group heteroaryl-S—, wherein the term heteroaryl is as defined above. The term “acyl” refers to a radical —C(O)R where R includes alkyl, alkenyl, alkynyl, aryl, heteroaryl, alicyclic, heterocyclic, arylalkyl or heteroarylalkyl wherein the alkyl, alkenyl, alkynyl, aryl, heteroaryl, alicyclic, heterocyclic, arylalkyl or heteroaryl alkyl groups may be optionally substituted. The term “acyloxy” refers to the ester group —OC(O)R, where R is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, alicyclic, heterocyclic, arylalkyl, or heteroarylalkyl wherein the alkyl, alkenyl, alkynyl, aryl, heteroaryl, alicyclic, heterocyclic, arylalkyl or heteroarylalkyl may be optionally substituted. The term “carboxy esters” refers to —C(O)OR where R is alkyl, aryl or arylalkyl, wherein the alkyl, aryl and arylalkyl groups may be optionally substituted. The term “carboxamido” refers to where each of R and R′ are independently selected from the group consisting of H, alkyl, aryl, heteroaryl, alicyclic, heterocyclic, arylalkyl and heteroarylalkyl, wherein the alkyl, aryl, heteroaryl, alicyclic, heterocyclic, or arylalkyl groups may be optionally substituted. The term “oxo” refers to ═O. The term “halogen” includes F, Cl, Br and I. The terms “haloalkyl, haloalkenyl, haloalkynyl and haloalkoxy” include alkyl, alkenyl, alkynyl and alkoxy structures, as described above, that are substituted with one or more fluorines, chlorines, bromines or iodines, or with combinations thereof. The terms “perhaloalkyl, perhaloalkyloxy and perhaloacyl” refer to alkyl, alkyloxy and acyl radicals as described above, in which all the H atoms are replaced by fluorines, chlorines, bromines or iodines, or combinations thereof. The terms “cycloalkyl, arylalkyl, aryl, heteroaryl, alicyclic, heterocyclic, alkyl, alkynyl, alkenyl, haloalkyl, and heteroalkyl” include optionally substituted cycloalkyl, arylalkyl, aryl, heteroaryl, alicyclic, heterocyclic, alkyl, alkynyl, alkenyl, haloalkyl and heteroalkyl groups. The terms “alkylamino”, refers to the group —NHR where R is alkyl. The terms “dialkylamino”, refers to the group —NRR′ where R and R′ are alkyls. The term “sulfide” refers to a sulfur atom covalently linked to two atoms; the formal oxidation state of said sulfur is (II). The term “thioether” may be used interchangeably with the term “sulfide.” The term “sulfoxide” refers to a sulfur atom covalently linked to three atoms, at least one of which is an oxygen atom; the formal oxidation state of said sulfur atom is (IV). The term “sulfone” refers to a sulfur atom covalently linked to four atoms, at least two of which are oxygen atoms; the formal oxidation state of said sulfur atom is (VI). The terms “optional” or “optionally” mean that the subsequently described event or circumstance may but need not occur, and that the description includes instances where the event or circumstance occurs and instances in which it does not. For example, “aryl optionally mono- or di-substituted with an alkyl” means that the alkyl may but need not be present, or either one alkyl or two may be present, and the description includes situations where the aryl is substituted with one or two alkyls and situations where the aryl is not substituted with an alkyl. “Optionally substituted” groups may be substituted or unsubstituted. The substituents of an “optionally substituted” group may include, without limitation, one or more substituents independently selected from the following groups or designated subsets thereof: lower alkyl, lower alkenyl, lower alkynyl, lower aryl, heteroaryl, alicyclic, heterocyclic, arylalkyl, heteroarylalkyl, lower alkoxy, lower aryloxy, amino, alkylamino, dialkylamino, alkylthio, arylthio, heteroarylthio, oxo, acyl (—C(O)R), (—C(O)), carboxyesters (—C(O)OR), carboxamido (—C(O)NH 2 ), carboxy, acyloxy, —H, halo, —CN, —NO 2 , —N 3 , —SH, —OH, —C(O)CH 3 , perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl. An optionally substituted group may be unsubstituted (e.g., —CH 2 CH 3 ), fully substituted (e.g., —CF 2 CF 3 ), monosubstituted (e.g., —CH 2 CH 2 F) or substituted at a level anywhere in-between fully substituted and monosubstituted (e.g., —CH 2 CF 3 ). The term “pyridine-1-oxy” also means “pyridine-N-oxy.” Some of the compounds of the present invention may contain one or more chiral centers and therefore may exist in enantiomeric and diastereomeric forms. The scope of the present invention is intended to cover all isomers per se, as well as mixtures of cis and trans isomers, mixtures of diastereomers and racemic mixtures of enantiomers (optical isomers) as well. Further, it is possible using well known techniques to separate the various forms, and some embodiments of the invention may feature purified or enriched species of a given enantiomer or diastereomer. A “pharmacological composition” refers to a mixture of one or more of the compounds described herein, or pharmaceutically acceptable salts thereof, with other chemical components, such as pharmaceutically acceptable carriers and/or excipients. The purpose of a pharmacological composition is to facilitate administration of a compound to an organism. The phrase “pharmaceutically acceptable carrier” as used herein means a pharmaceutically-acceptable material, composition or vehicle, such as a liquid or solid filler, diluent, excipient, solvent or encapsulating material, involved in carrying or transporting the subject agent from one organ, or portion of the body, to another organ, or portion of the body. Each carrier must be “acceptable” in the sense of being compatible with the other ingredients of the formulation and not injurious to the patient. Some examples of materials which can serve as pharmaceutically-acceptable carriers include: (1) sugars, such as lactose, glucose and sucrose; (2) starches, such as corn starch and potato starch; (3) cellulose, and its derivatives, such as sodium carboxymethyl cellulose, ethyl cellulose and cellulose acetate; (4) powdered tragacanth; (5) malt; (6) gelatin; (7) talc; (8) excipients, such as cocoa butter and suppository waxes; (9) oils, such as peanut oil, cottonseed oil, safflower oil, sesame oil, olive oil, corn oil and soybean oil; (10) glycols, such as propylene glycol; (11) polyols, such as glycerin, sorbitol, mannitol and polyethylene glycol; (12) esters, such as ethyl oleate and ethyl laurate; (13) agar; (14) buffering agents, such as magnesium hydroxide and aluminum hydroxide; (15) alginic acid; (16) pyrogen-free water; (17) isotonic saline; (18) Ringer's solution; (19) ethyl alcohol; (20) phosphate buffer solutions; and (21) other non-toxic compatible substances employed in pharmaceutical formulations. A physiologically acceptable carrier should not cause significant irritation to an organism and does not abrogate the biological activity and properties of the administered compound. An “excipient” refers to an inert substance added to a pharmacological composition to further facilitate administration of a compound. Examples of excipients include but are not limited to calcium carbonate, calcium phosphate, various sugars and types of starch, cellulose derivatives, gelatin, vegetable oils and polyethylene glycols. A “pharmaceutically effective amount” means an amount which is capable of providing a therapeutic and/or prophylactic effect. The specific dose of compound administered according to this invention to obtain therapeutic and/or prophylactic effect will, of course, be determined by the particular circumstances surrounding the case, including, for example, the specific compound administered, the route of administration, the condition being treated, and the individual being treated. A typical daily dose (administered in single or divided doses) will contain a dosage level of from about 0.01 mg/kg to about 50–100 mg/kg of body weight of an active compound of the invention. Preferred daily doses generally will be from about 0.05 mg/kg to about 20 mg/kg and ideally from about 0.1 mg/kg to about 10 mg/kg. Factors such as clearance rate, half-life and maximum tolerated dose (MTD) have yet to be determined but one of ordinary skill in the art can determine these using standard procedures. In some method embodiments, the preferred therapeutic effect is the inhibition, to some extent, of the growth of cells characteristic of a proliferative disorder, e.g., breast cancer. A therapeutic effect will also normally, but need not, relieve to some extent one or more of the symptoms other than cell growth or size of cell mass. A therapeutic effect may include, for example, one or more of 1) a reduction in the number of cells; 2) a reduction in cell size; 3) inhibition (i.e., slowing to some extent, preferably stopping) of cell infiltration into peripheral organs, e.g., in the instance of cancer metastasis; 3) inhibition (i.e., slowing to some extent, preferably stopping) of tumor metastasis; 4) inhibition, to some extent, of cell growth; and/or 5) relieving to some extent one or more of the symptoms associated with the disorder. As used herein, the term IC 50 refers to an amount, concentration or dosage of a particular test compound that achieves a 50% inhibition of a maximal response in an assay that measures such response. In some method embodiments of the invention, the “IC 50 ” value of a compound of the invention can be greater for normal cells than for cells exhibiting a proliferative disorder, e.g., breast cancer cells. The value depends on the assay used. By a “standard” is meant a positive or negative control. A negative control in the context of HER2 expression levels is, e.g., a sample possessing an amount of HER2 protein that correlates with a normal cell. A negative control may also include a sample that contains no HER2 protein. By contrast, a positive control does contain HER2 protein, preferably of an amount that correlates with overexpression as found in proliferative disorders, e.g., breast cancers. The controls may be from cell or tissue samples, or else contain purified ligand (or absent ligand), immobilized or otherwise. In some embodiments, one or more of the controls may be in the form of a diagnostic “dipstick.” By “selectively targeting” is meant affecting one type of cell to a greater extent than another, e.g., in the case of cells with high as opposed to relatively low or normal HER2 levels. II. Compounds of the Invention Compounds of the invention and their polymorphs, solvates, esters, tautomers, diastereomers, enantiomers, pharmaceutically acceptable salts or prodrugs show utility for inhibiting HSP90 and treating and preventing diseases that are HSP90-dependent. One embodiment of the compounds of the invention is of Formula A: or a polymorph, solvate, ester, tautomer, diastereomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: X 1 and X 2 are the same or different and each is nitrogen or —CR 6 ;X 3 is nitrogen or —CR 3 wherein R 3 is hydrogen, OH, a keto tautomer, —OR 8 , —CN, halogen, lower alkyl, or —C(O)R 9 ;X 4 is nitrogen or a group CR 6 when X 3 is nitrogen, and X 4 is —CR 6 R 7 when X 3 is —CR 3 ;R 1 is halogen, —OR 8 , —SR 8 , or lower alkyl;R 2 is —NR 8 R 10 ;R 4 is —(CH 2 ) n — wherein n=0–3, —C(O), —C(S), —SO 2 —, or —SO 2 N—; andR 5 is alkyl, aryl, heteroaryl, alicyclic, or heterocyclic, each of which is optionally bi- or tricyclic, and optionally substituted with H, halogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower alicyclic, araalkyl, aryloxyalkyl, alkoxyalkyl, perhaloalkyl, perhaloalkyloxy, perhaloacyl, —N 3 , —SR 8 , —OR 8 , —CN, —CO 2 R 9 , —NO 2 , or —NR 8 R 10 ; with the provisos that: the compound is not one found or described in one or more of JP 10025294; U.S. Pat. No. 4,748,177; U.S. Pat. No. 4,748,177; U.S. Pat. No. 6,369,092; WO 00/06573; WO 02/055521; WO 02/055082; WO 02/055083 ; Eur. J. Med. Chem., 1994, 29(1), 3–9; and J. Het. Chem. 1990, 27(5), 1409; —R 4 R 5 is not a ribose or derivative thereof, or a sugar or derivative thereof; —R 4 R 5 is not a phosphonate or phosphonic acid, or a group substituted with a phosphonate or phosphonic acid; and when R 4 is (CH 2 ) n where n=0 or 1, then R 4 and R 5 are not connected with ‘O’, e.g., —CH 2 —O—CH 2 — or —CH 2 —CH 2 —O—CH 2 —. In one embodiment of, the compound, tautomer, pharmaceutically acceptable salt thereof, or prodrug thereof of Formula A, X 1 and X 2 are the same or different and each is nitrogen or —CR 6 ; R 1 is halogen, —OR 8 , —SR 8 , or lower alkyl; R 2 is —NR 8 R 10 ; R3 is hydrogen, —OH or keto tautomer, —OR 8 , halogen, —CN, lower alkyl, or —C(O)R 9 ; R 4 is —(CH 2 ) n — wherein n=0–3, —C(O), —C(S), —SO 2 —, or —SO 2 N—; and R 5 is alkyl, aromatic, heteroaromatic, alicyclic, heterocyclic, each of which is optionally bi- or tricyclic, and optionally substituted with H, halogen, lower alkyl, —SR 8 , —OR 8 , —CN, —CO 2 R 9 , —NO 2 or —NR 8 R 10 ; R 8 is hydrogen, lower alkyl, lower aryl or —(CO)R 9 ; R 9 is lower alkyl, lower aryl, lower heteroaryl, —NR 8 R 10 or OR 11 ; R 11 is lower alkyl or lower aryl; and R 10 is hydrogen or lower alkyl. In one embodiment, the compound, tautomer, pharmaceutically acceptable salt thereof, or prodrug thereof of Formula A, R 1 is selected from halogen, hydroxyl, lower alkoxy, lower thioalkyl and C 1-4 alkyl; and R 2 is —NH 2 . In another embodiment, R 4 is —(CH 2 ) n —, wherein n=0–3. In another embodiment, R 1 is selected from halogen, hydroxyl, lower alkoxy, lower thioalkyl or C 1-4 alkyl; optionally wherein R 2 is NH 2 . In another embodiment, R 4 is —(CH 2 ) n —, wherein n=0–3. In another embodiment, R 4 is —(CH 2 ) n —, wherein n=0–3, R 1 is selected from halogen, hydroxyl, lower alkoxy, lower thioalkyl, and C 1-4 alkyl, and R 2 is optionally NH 2 . In another embodiment, R 1 is halogen, hydroxyl, lower alkoxy, lower thioalkyl, or C 1-4 alkyl; and R 2 is optionally NH 2 , R 4 is —(CH 2 )—, and R 5 is phenyl, benzyl, or pyridyl, all optionally substituted with H, halogen, lower alkyl, —SR 8 , —OR 8 (or cyclic ethers such as methylenedioxy), —CN, —C0 2 R 9 , —NO 2 , or —NR 8 R 10 ; R 8 is hydrogen, lower alkyl, lower aryl or —(CO)R 9 ; R 9 is lower alkyl, lower aryl, lower heteroaryl, —NR 8 R 10 or —OR 11 ; R 11 is lower alkyl or lower aryl; and R 10 is hydrogen or lower alkyl. In another embodiment R 1 is halogen, R 2 is —NH 2 , R 4 is —CH 2 —, R 6 is H or halogen, and R 5 is phenyl optionally substituted with H, halogen, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkylthio, perhaloalkyl, perhaloalkyloxy, —CN, —NO 2 , —NH 2 or —CO 2 R 11 . In another embodiment, R 1 is halogen, R 2 is —NH 2 , R 4 is —CH 2 —, R 6 is H, and R 5 is 2-halo-3,5-dimethoxyphenyl optionally substituted with H, halogen, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkylthio, perhaloalkyl, perhaloalkyloxy, —CN, —NO 2 , —NH 2 , or —CO 2 R 11 at the para (4−) position. In another embodiment, R 1 is chloro, R 2 is —NH 2 , R 4 is —CH 2 —, R 6 is H and R 5 is 2-chloro-3,4,5-trimethoxyphenyl. In another embodiment, R 1 is chloro, R 2 is —NH 2 , R 4 is —CH 2 —, R 6 is H and R 5 is 2-bromo-3,4,5-trimethoxyphenyl. In other embodiments, R 5 is selected from 2-iodo-3,4,5-trimethoxyphenyl, 2-fluoro-3,4,5-trimethoxyphenyl, and 2-bromo-3,4,5-trimethoxyphenyl. Any of the foregoing embodiments can be combined where feasible and appropriate. In another aspect, the invention provides compounds of Formula A1: or a tautomer, pharmaceutically acceptable salt, or prodrug thereof, wherein: X 1 and X 2 are the same or different and each is nitrogen or a group —CR 6 ;R 1 is halogen, —OR 8 , —SR 8 , or lower alkyl;R 2 is —NR 8 R 10 ;R 4 is —(CH 2 ) n — where n=0–3, —C(O), —C(S), —SO 2 — or —SO 2 N—;R 5 is alkyl, aromatic, heteroaromatic, alicyclic, heterocyclic, all optionally bi- or tricyclic, and all optionally substituted with H, halogen, lower alkyl, —SR 8 , —OR 8 , —CN, —CO 2 R 9 , —NO 2 , or —NR 8 R 10 ;R 6 is hydrogen, halogen, lower alkyl, —SR 8 , —OR 8 , —NR 8 R 10 , —N 3 , —CN, —C(O)R 9 , or taken together with R 7 is carbonyl (C═O);R 7 is independently selected from hydrogen, lower alkyl or taken together with R 6 is —C(O);R 8 is hydrogen, lower alkyl, lower aryl, or —(CO)R 9 ;R 9 is lower alkyl, lower aryl, lower heteroaryl, —NR 8 R 10 or —OR 11 ;R 10 is hydrogen or lower alkyl, andR 11 is lower alkyl or lower aryl. In one embodiment of the compounds of Formula A1, or a tautomer, pharmaceutically acceptable salt, or prodrug thereof, R 1 is halogen, hydroxyl, lower alkoxy, lower thioalkyl, or C 1-4 alkyl; and R 2 is NH 2 . In another embodiment of the compounds of Formula A1, or a tautomer, pharmaceutically acceptable salt thereof, or prodrug thereof, R 4 is —(CH 2 ) n —, where n=0–3. In another embodiment of the compounds of Formula A1, or a tautomer, pharmaceutically acceptable salt, or prodrug thereof, R 1 is halogen, hydroxyl, lower alkoxy, lower thioalkyl, or C 1-4 alkyl; and R 2 is NH 2 ; R 4 is —(CH 2 ) n —, and wherein n=0–3. In another embodiment of the compounds of Formula A1, or a tautomer, pharmaceutically acceptable salt thereof, R 1 is halogen; R 2 is NH 2 , R 4 is —CH 2 —. Another embodiment of the invention is compounds of Formula I: or a polymorph, solvate, ester, tautomer, diastereomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 0 is selected from hydrogen, halogen, lower alkyl, —SR 8 , —OR 8 , —CN, and —NHR 8 ,R 1 is halogen, —OR 11 , —SR 11 or lower alkyl;R 2 is —NHR 8 ;R 3 is selected from the group consisting of hydrogen, halogen, —SR 8 , —OR 8 , —CN, —C(O)R 9 , —C(O)OH, —NO 2 , —NR 8 R 10 , lower alkyl, lower alkenyl, lower alkynyl, aryl, lower perhaloalkyl, heteroaryl, alicyclic, heterocyclic, all optionally substituted, wherein: the aryl, heteroaryl, alicyclic and heterocyclic groups are optionally mono-, bi- or tri-cyclic, R 8 and R 10 taken together optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N, andthe optional substituents R 3 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are hetero atoms selected from the group of O, S and N;R 0 or R 3 is —OH or —SH, the compound may exist as the corresponding (thio)keto tautomer or a mixture of keto-enol tautomers;R 4 is —CHR 12 —, —C(O)—, —C(S)—, —S(O)— or —SO 2 —;R 5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 3 to 5 substituents,the heteroaryl group is substituted with 2 to 5 substituents,the alicyclic group is substituted with 3 to 5 substituents,the heterocyclic group is substituted with 3 to 5 substituents, andthe substituents are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;R 8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 ;R 9 is H, lower alkyl, lower alkenyl, or lower alkynyl, lower aryl, lower heteroaryl, —NR 10 R 10 , or —OR 11 , wherein R 10 and R 10 taken together optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;R 10 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl or lower heteroaryl;R 11 is lower alkyl, lower alkenyl,-or lower alkynyl, lower heteroaryl or lower aryl; andR 12 is hydrogen or lower alkyl. In one embodiment of the compounds of Formula I, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, each of the aryl, heteroaryl, alicyclic or heterocyclic group is monocyclic or bicyclic. In another embodiment of the compounds of Formula I, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 0 is hydrogen, halogen, —SH, —OH, or —CN; R 1 is halogen; and R 2 is —NHR 8 , where R 8 is hydrogen or —C(O)R 9 . In another embodiment of the compounds of Formula I, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 1 is chloro or bromo, R 2 is —NHR , where R 8 is hydrogen or —C(O)R 9 ; R 3 is hydrogen, halogen, OR 8 , SR 8 , NR 8 R 10 , lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, lower aryl, or lower heteroaryl. In another embodiment of the compounds of Formula I, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 0 is hydrogen, halogen or —CN; R 2 is —NHR 8 , where R 8 is hydrogen or —C(O)R 9 ; and R 4 is —CH 2 —. In another embodiment of the compounds of Formula I, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 0 is hydrogen, halogen, —SH, —OH or —CN; R 1 is halogen; R 2 is —NH 2 , R 3 is hydrogen, halogen, —OR 8 , —SR 8 , —NR 8 R 10 , lower alkyl, lower alkenyl, lower alkynyl, perhaloalkyl, lower aryl, or lower heteroaryl, wherein R 8 is hydrogen, lower alkyl, lower aryl, or —C(O)R 9 ; R 4 is —CH 2 —; and R 5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents. In another embodiment of the compounds of Formula I, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 1 is chloro or bromo, R 2 is —NH 2 , and R 5 is a phenyl having at least three substituents. In another embodiment of the compounds of Formula I, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 1 is chloro or bromo, R 2 is —NH 2 and R 5 is a pyridyl having at least two substituents. In another embodiment of the compounds of Formula I, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 1 is chloro or bromo, R 2 is —NH 2 , and R 5 is 1-oxy-pyridyl (N-oxy-pyridyl) having at least two substituents. Another embodiment of the invention is a compound of Formula II: polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 0 is hydrogen, halogen, lower alkyl, —SR 8 , —OR 8 , —CN or —NHR 8 ,R 1 is halogen, —OR 11 , —SR 11 or lower alkyl;R 2 is —NH 2 ;R 4 is —CHR 12 —, —C(O)—, —C(S)—, —S(O)— or —SO 2 —;R 5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein: the aryl group is substituted with 3 to 5 substituents,the heteroaryl group is substituted with 2 to 5 substituents,the alicyclic group is substituted with 3 to 5 substituents,the heterocyclic group is substituted with 3 to 5 substituents, andthe substituents on R 5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 R 10 taken with the N to which they are attached together with the N to which they are attached optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;R 8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 ;R 9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR 10 R 10 or —OR 11 , wherein R 10 and R 10 taken together optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;R 10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl,R 11 is lower alkyl, lower alkenyl, lower alkynyl, lower heteroaryl or lower aryl;R 12 is hydrogen or lower alkyl; andR 0 and R 10 taken together optionally form an exocyclic double bond which is optionally substituted, or optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N. In one embodiment of the compounds of Formula II, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 1 is halogen or lower alkyl; R 4 is —CHR 12 —; R 5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents. In another embodiment of the compounds of Formula II, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 0 is hydrogen or —NHR 8 , R 1 is halogen, —OR 11 , —SR 11 or lower alkyl; R 10 is hydrogen or lower alkyl. In another embodiment of the compounds of Formula II, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 0 is hydrogen; R 1 is halogen; R 4 is —CH 2 —; and R 5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents; and R 10 is hydrogen. In another embodiment of the compounds of Formula II, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 1 is chloro or bromo, R 5 is phenyl, pyridyl or 1-oxy-pyridyl (N-oxy-pyridyl) each of which has at least two substituents. Another embodiment of the invention is a compound represented by Formula III: or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 1 is halogen, —OR 11 , —SR 11 or lower alkyl;R 2 is —NH 2 ;R 3 is selected from the group consisting of hydrogen, halogen, —SR 8 , —OR 8 , —CN, —C(O)R 9 , —C(O)OH, —NO 2 , —NR 8 R 10 , lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic, heterocyclic, all optionally substituted, wherein: the aryl, heteroaryl, alicyclic and heterocyclic groups are optionally mono-, bi- or tri-cyclic,R 8 and R 10 taken together optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N, andthe optional substituents on R 3 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR , —OR 8 , —CN, —C(O)OH, —C(O)R , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 R 10 taken with the N to which they are attached together with the N to which they are attached optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;R 4 is —CHR 12 —, —C(O)—, —C(S)—, —S(O)— or —SO 2 —;R 5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 3 to 5 substituents,the heteroaryl group is substituted with 2 to 5 substituents,the alicyclic group is substituted with 3 to 5 substituents,the heterocyclic group is substituted with 3 to 5 substituents, andthe substituents on R 5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 , lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;R 8 is hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 ;R 9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR 10 R 10 or —OR 11 , wherein R 10 and R 10 taken together optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;R 10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl,R 11 is lower alkyl, lower alkenyl, lower alkynyl, lower heteroaryl or lower aryl;R 12 is hydrogen or lower alkyl; andR 3 and R 10 taken together optionally form an exocyclic double bond which is optionally substituted, or optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N. In one embodiment of the compounds of Formula III, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 1 is halogen; R 3 is hydrogen, halogen, —OR 8 , —SR 8 , —NR 8 R 10 , lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, lower aryl, or lower heteroaryl, wherein R 8 is hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 ; R 4 is —CH 2 —; R 5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents; and R 10 is hydrogen or lower alkyl. In another embodiment of the compounds of Formula III, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 1 is halogen; R 4 is —CH 2 —; R 5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents; and R 10 is hydrogen. In another embodiment of the compounds of Formula III, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 1 is halogen; R 3 is hydrogen; R 4 is —CH 2 —; R 5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents; and R 10 is hydrogen. In another embodiment of the compounds of Formula III, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein R 1 is chloro or bromo, R 5 is phenyl, pyridyl or 1-oxy-pyridyl (N-oxy-pyridyl), each of which has at least two substituents. Another embodiment of the invention is compounds represented by Formula IV: or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R 1 is halogen, —OR 11 , —SR 11 or lower alkyl;R 2 is —NH 2 ;R 4 is —CHR 12 —, —C(O)—, —C(S)—, —S(O)— or —SO 2 —;R 5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 3 to 5 substituents,the heteroaryl group is substituted with 2 to 5 substituents,the alicyclic group is substituted with 3 to 5 substituents,the heterocyclic group is substituted with 3 to 5 substituents, andthe substituents on R 5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR 8 , —OR 8 , —CN, —C(O)OH, —C(O)R 9 , —NO 2 , —NR 8 R 10 lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R 8 R 10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;R 8 is hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R 9 ;R 9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR 10 R 10 or —OR 11 , wherein R 10 and R 10 taken together optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;R 10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl,R 11 is lower alkyl, lower alkenyl, or lower alkynyl, lower heteroaryl lower aryl; andR 12 is hydrogen or lower alkyl. In one embodiment of the compounds of Formula IV, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 1 is halogen; R 4 is —CH 2 —; R 5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents. In another embodiment of the compounds of Formula IV, or a polymorph, solvate, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, R 1 is chloro or bromo, and R 5 is phenyl, pyridyl or 1-oxy-pyridyl (N-oxy-pyridyl), each of which has at least two substituents. It should be understood that any of the foregoing embodiments can be combined where feasible and appropriate. Illustrative species of the compounds of the invention that are based on Formula I are described in TABLE 1. Prodrugs which can be employed with the compound of the invention include, but are not limited to, those listed in the Definition section above. TABLE 1Exemplary Compounds based on Formula INo.ExR 1R 2R 3R 4R 5R 619ClNH 2HCH 23,4,5-TrimethoxyphenylH2ClNH 2HCH 22-Chloro-3,4,5-trimethoxyphenylH36ClNH 2HCH 22-Bromo-3,4,5-trimethoxyphenylH47ClNH 2HCH 22-Iodo-3,4,5-trimethoxyphenylH5ClNH 2HCH 22-Fluoro-3,4,5-trimethoxyphenylH6ClNH 2HCH 23,4,5-TrimethylphenylH7ClNH 2HCH 22-Chloro-3,4,5-trimethylphenylH8ClNH 2HCH 22-Bromo-3,4,5-trimethylphenylH9ClNH 2HCH 22-Iodo-3,4,5-trimethylphenylH10ClNH 2HCH 22-Fluoro-3,4,5-trimethylphenylH11ClNH 2HCH 23,5-Dimethoxy-4-methylphenylH12ClNH 2HCH 22-Chloro-3,5-dimethoxy-4-methylphenylH13ClNH 2HCH 22-Bromo-3,5-dimethoxy-4-methylphenylH14ClNH 2HCH 22-Iodo-3,5-dimethoxy-4-methylphenylH15ClNH 2HCH 22-Fluoro-3,5-dimethoxy-4-methylphenylH16ClNH 2i-prCH 23,4,5-TrimethoxyphenylH17ClNH 2i-prCH 22-Chloro-3,4,5-trimethoxyphenylH18ClNH 2i-prCH 22-Bromo-3,4,5-trimethoxyphenylH19ClNH 2i-prCH 22-Iodo-3,4,5-trimethoxyphenylH20ClNH 2i-prCH 22-Fluoro-3,4,5-trimethoxyphenylH21ClNH 2i-prCH 23,4,5-TrimethylphenylH22ClNH 2i-prCH 22-Chloro-3,4,5-trimethylphenylH23ClNH 2i-prCH 22-Bromo-3,4,5-trimethylphenylH24ClNH 2i-prCH 22-Iodo-3,4,5-trimethylphenylH25ClNH 2i-prCH 22-Fluoro-3,4,5-trimethylphenylH26ClNH 2i-prCH 23,5-Dimethoxy-4-methylphenylH27ClNH 2i-prCH 22-Chloro-3,5-dimethoxy-4-methylphenylH28ClNH 2i-prCH 22-Bromo-3,5-dimethoxy-4-methylphenylH29ClNH 2i-prCH 22-Iodo-3,5-dimethoxy-4-methylphenylH30ClNH 2i-prCH 22-Fluoro-3,5-dimethoxy-4-methylphenylH31ClNH 2EtCH 23,4,5-TrimethoxyphenylH32ClNH 2EtCH 22-Chloro-3,4,5-trimethoxyphenylH33ClNH 2EtCH 22-Bromo-3,4,5-trimethoxyphenylH34ClNH 2EtCH 22-Iodo-3,4,5-trimethoxyphenylH35ClNH 2EtCH 22-Fluoro-3,4,5-trimethoxyphenylH36ClNH 2EtCH 23,4,5-TrimethylphenylH37ClNH 2EtCH 22-Chloro-3,4,5-trimethylphenylH38ClNH 2EtCH 22-Bromo-3,4,5-trimethylphenylH39ClNH 2EtCH 22-Iodo-3,4,5-trimethylphenylH40ClNH 2EtCH 22-Fluoro-3,4,5-trimethylphenylH41ClNH 2EtCH 23,5-Dimethoxy-4-methylphenylH42ClNH 2EtCH 22-Chloro-3,5-dimethoxy-4-methylphenylH43ClNH 2EtCH 22-Bromo-3,5-dimethoxy-4-methylphenylH44ClNH 2EtCH 22-Iodo-3,5-dimethoxy-4-methylphenylH45ClNH 2EtCH 22-Fluoro-3,5-dimethoxy-4-methylphenylH46ClNH 2MeCH 23,4,5-TrimethoxyphenylH47ClNH 2MeCH 22-Chloro-3,4,5-trimethoxyphenylH48ClNH 2MeCH 22-Bromo-3,4,5-trimethoxyphenylH49ClNH 2MeCH 22-Iodo-3,4,5-trimethoxyphenylH50ClNH 2MeCH 22-Fluoro-3,4,5-trimethoxyphenylH51ClNH 2MeCH 23,4,5-TrimethylphenylH52ClNH 2MeCH 22-Chloro-3,4,5-trimethylphenylH53ClNH 2MeCH 22-Bromo-3,4,5-trimethylphenylH54ClNH 2MeCH 22-Iodo-3,4,5-trimethylphenylH55ClNH 2MeCH 22-Fluoro-3,4,5-trimethylphenylH56ClNH 2MeCH 23,5-Dimethoxy-4-methylphenylH57ClNH 2MeCH 22-Chloro-3,5-dimethoxy-4-methylphenylH58ClNH 2MeCH 22-Bromo-3,5-dimethoxy-4-methylphenylH59ClNH 2MeCH 22-Iodo-3,5-dimethoxy-4-methylphenylH60ClNH 2MeCH 22-Fluoro-3,5-dimethoxy-4-methylphenylH61ClNH 2PhCH 23,4,5-TrimethoxyphenylH62ClNH 2PhCH 22-Chloro-3,4,5-trimethoxyphenylH63ClNH 2PhCH 22-Bromo-3,4,5-trimethoxyphenylH64ClNH 2PhCH 22-Iodo-3,4,5-trimethoxyphenylH65ClNH 2PhCH 22-Fluoro-3,4,5-trimethoxyphenylH66ClNH 2PhCH 23,4,5-TrimethylphenylH67ClNH 2PhCH 22-Chloro-3,4,5-trimethylphenylH68ClNH 2PhCH 22-Bromo-3,4,5-trimethylphenylH69ClNH 2PhCH 22-Iodo-3,4,5-trimethylphenylH70ClNH 2PhCH 22-Fluoro-3,4,5-trimethylphenylH71ClNH 2PhCH 23,5-Dimethoxy-4-methylphenylH72ClNH 2PhCH 22-Chloro-3,5-dimethoxy-4-methylphenylH73ClNH 2PhCH 22-Bromo-3,5-dimethoxy-4-methylphenylH74ClNH 2PhCH 22-Iodo-3,5-dimethoxy-4-methylphenylH75ClNH 2PhCH 22-Fluoro-3,5-dimethoxy-4-methylphenylH76ClNH 22-PyCH 23,4,5-TrimethoxyphenylH77ClNH 22-PyCH 22-Chloro-3,4,5-trimethoxyphenylH78ClNH 22-PyCH 22-Bromo-3,4,5-trimethoxyphenylH79ClNH 22-PyCH 22-Iodo-3,4,5-trimethoxyphenylH80ClNH 22-PyCH 22-Fluoro-3,4,5-trimethoxyphenylH81ClNH 22-PyCH 23,4,5-TrimethylphenylH82ClNH 22-PyCH 22-Chloro-3,4,5-trimethylphenylH83ClNH 22-PyCH 22-Bromo-3,4,5-trimethylphenylH84ClNH 22-PyCH 22-Iodo-3,4,5-trimethylphenylH85ClNH 22-PyCH 22-Fluoro-3,4,5-trimethylphenylH86ClNH 22-PyCH 23,5-Dimethoxy-4-methylphenylH87ClNH 22-PyCH 22-Chloro-3,5-dimethoxy-4-methylphenylH88ClNH 22-PyCH 22-Bromo-3,5-dimethoxy-4-methylphenylH89ClNH 22-PyCH 22-Iodo-3,5-dimethoxy-4-methylphenylH90ClNH 22-PyCH 22-Fluoro-3,5-dimethoxy-4-methylphenylH91ClNH 24-PyCH 23,4,5-TrimethoxyphenylH92ClNH 24-PyCH 22-Chloro-3,4,5-trimethoxyphenylH93ClNH 24-PyCH 22-Bromo-3,4,5-trimethoxyphenylH94ClNH 24-PyCH 22-Iodo-3,4,5-trimethoxyphenylH95ClNH 24-PyCH 22-Fluoro-3,4,5-trimethoxyphenylH96ClNH 2PhCH 23,4,5-TrimethylphenylH97ClNH 2PhCH 22-Chloro-3,4,5-trimethylphenylH98ClNH 2PhCH 22-Bromo-3,4,5-trimethylphenylH99ClNH 2PhCH 22-Iodo-3,4,5-trimethylphenylH100ClNH 2PhCH 22-Fluoro-3,4,5-trimethylphenylH101ClNH 2PhCH 23,5-Dimethoxy-4-methylphenylH102ClNH 2PhCH 22-Chloro-3,5-dimethoxy-4-methylphenylH103ClNH 2PhCH 22-Bromo-3,5-dimethoxy-4-methylphenylH104ClNH 2PhCH 22-Iodo-3,5-dimethoxy-4-methylphenylH105ClNH 2PrCH 22-Fluoro-3,5-dimethoxy-4-methylphenylH106ClNH 2PrCH 23,5-Dimethoxy-4-methylphenylH107ClNH 2PrCH 22-Chloro-3,5-dimethoxy-4-methylphenylH108ClNH 2PrCH 22-Bromo-3,5-dimethoxy-4-methylphenylH109ClNH 2PrCH 22-Iodo-3,5-dimethoxy-4-methylphenylH110ClNH 2PrCH 22-Fluoro-3,5-dimethoxy-4-methylphenylH111ClNH 2PrCH 23,4,5-TrimethoxyphenylH112ClNH 2PrCH 22-Chloro-3,4,5-trimethoxyphenylH113ClNH 2PrCH 22-Bromo-3,4,5-trimethoxyphenylH114ClNH 2PrCH 22-Iodo-3,4,5-trimethoxyphenylH115ClNH 2PrCH 22-Fluoro-3,4,5-trimethoxyphenylH116ClNH 2PrCH 23,4,5-TrimethylphenylH117ClNH 2PrCH 22-Chloro-3,4,5-trimethylphenylH118ClNH 2PrCH 22-Bromo-3,4,5-trimethylphenylH119ClNH 2PrCH 22-Iodo-3,4,5-trimethylphenylH120ClNH 2PrCH 22-Fluoro-3,4,5-trimethylphenylH121ClNH 2PrCH 23,5-Dimethoxy-4-methylphenylH122ClNH 2PrCH 22-Chloro-3,5-dimethoxy-4-methylphenylH123ClNH 2PrCH 22-Bromo-3,5-dimethoxy-4-methylphenylH124ClNH 2PrCH 22-Iodo-3,5-dimethoxy-4-methylphenylH125ClNH 2PrCH 22-Fluoro-3,5-dimethoxy-4-methylphenylH126BrNH 2HCH 23,4,5-TrimethoxyphenylH127BrNH 2HCH 22-Chloro-3,4,5-trimethoxyphenylH128BrNH 2HCH 22-Bromo-3,4,5-trimethoxyphenylH129BrNH 2HCH 22-Iodo-3,4,5-trimethoxyphenylH130BrNH 2HCH 22-Fluoro-3,4,5-trimethoxyphenylH131BrNH 2HCH 23,4,5-TrimethylphenylH132BrNH 2HCH 22-Chloro-3,4,5-trimethylphenylH133BrNH 2HCH 22-Bromo-3,4,5-trimethylphenylH134BrNH 2HCH 22-Iodo-3,4,5-trimethylphenylH135BrNH 2HCH 22-Fluoro-3,4,5-trimethylphenylH136BrNH 2HCH 23,5-Dimethoxy-4-methylphenylH137BrNH 2HCH 22-Chloro-3,5-dimethoxy-4-methylphenylH138BrNH 2HCH 22-Bromo-3,5-dimethoxy-4-methylphenylH139BrNH 2HCH 22-Iodo-3,5-dimethoxy-4-methylphenylH140BrNH 2HCH 22-Fluoro-3,5-dimethoxy-4-methylphenylH141ClNH 2i-BuCH 23,4,5-TrimethoxyphenylH142ClNH 2i-BuCH 22-Chloro-3,4,5-trimethoxyphenylH143ClNH 2i-BuCH 22-Bromo-3,4,5-trimethoxyphenylH144ClNH 2i-BuCH 22-Iodo-3,4,5-trimethoxyphenylH145ClNH 2i-BuCH 22-Fluoro-3,4,5-trimethoxyphenylH146ClNH 2i-BuCH 23,4,5-TrimethylphenylH147ClNH 2i-BuCH 22-Chloro-3,4,5-trimethylphenylH148ClNH 2i-BuCH 22-Bromo-3,4,5-trimethylphenylH149ClNH 2i-BuCH 22-Iodo-3,4,5-trimethylphenylH150ClNH 2i-BuCH 22-Fluoro-3,4,5-trimethylphenylH151ClNH 2i-BuCH 23,5-Dimethoxy-4-methylphenylH152ClNH 2i-BuCH 22-Chloro-3,5-dimethoxy-4-methylphenylH153ClNH 2i-BuCH 22-Bromo-3,5-dimethoxy-4-methylphenylH154ClNH 2i-BuCH 22-Iodo-3,5-dimethoxy-4-methylphenylH155ClNH 2i-BuCH 22-Fluoro-3,5-dimethoxy-4-methylphenylH156ClNH 2CNCH 23,4,5-TrimethoxyphenylH157ClNH 2CNCH 22-Chloro-3,4,5-trimethoxyphenylH158ClNH 2CNCH 22-Bromo-3,4,5-trimethoxyphenylH159ClNH 2CNCH 22-Iodo-3,4,5-trimethoxyphenylH160ClNH 2CNCH 23,4,5-TrimethoxyphenylH161ClNH 2CNCH 22-Chloro-3,4,5-trimethoxyphenylH162ClNH 2CNCH 22-Bromo-3,4,5-trimethoxyphenylH163ClNH 2CNCH 22-Iodo-3,4,5-trimethoxyphenylH164ClNH 2CNCH 22-Fluoro-3,4,5-trimethoxyphenylH165ClNH 2CNCH 23,4,5-TrimethylphenylH166ClNH 2CNCH 22-Chloro-3,4,5-trimethylphenylH167ClNH 2CNCH 22-Bromo-3,4,5-trimethylphenylH168ClNH 2CNCH 22-Iodo-3,4,5-trimethylphenylH169ClNH 2CNCH 22-Fluoro-3,4,5-trimethylphenylH170ClNH 2CNCH 23,5-Dimethoxy-4-methylphenylH171ClNH 2CNCH 22-Chloro-3,5-dimethoxy-4-methylphenylH172ClNH 2CNCH 22-Bromo-3,5-dimethoxy-4-methylphenylH173ClNH 2CNCH 22-Iodo-3,5-dimethoxy-4-methylphenylH174ClNH 2CNCH 22-Fluoro-3,5-dimethoxy-4-methylphenylH175ClNH 2ClCH 23,4,5-TrimethoxyphenylH176ClNH 2ClCH 22-Chloro-3,4,5-trimethoxyphenylH177ClNH 2ClCH 22-Bromo-3,4,5-trimethoxyphenylH178ClNH 2ClCH 22-Iodo-3,4,5-trimethoxyphenylH179ClNH 2ClCH 22-Fluoro-3;4,5-trimethoxyphenylH180ClNH 2ClCH 23,4,5-TrimethylphenylH181ClNH 2ClCH 22-Chloro-3,4,5-trimethylphenylH182ClNH 2ClCH 22-Bromo-3,4,5-trimethylphenylH183ClNH 2ClCH 22-Iodo-3,4,5-trimethylphenylH184ClNH 2ClCH 22-Fluoro-3,4,5-trimethylphenylH185ClNH 2ClCH 23,5-Dimethoxy-4-methylphenylH186ClNH 2ClCH 22-Chloro-3,5-dimethoxy-4-methylphenylH187ClNH 2ClCH 22-Bromo-3,5-dimethoxy-4-methylphenylH188ClNH 2ClCH 22-Iodo-3,5-dimethoxy-4-methylphenylH189ClNH 2ClCH 22-Fluoro-3,5-dimethoxy-4-methylphenylH190ClNH 2BrCH 23,4,5-TrimethoxyphenylH191ClNH 2BrCH 22-Chloro-3,4,5-trimethoxyphenylH192ClNH 2BrCH 22-Bromo-3,4,5-trimethoxyphenylH193ClNH 2BrCH 22-Iodo-3,4,5-trimethoxyphenylH194ClNH 2BrCH 22-Fluoro-3,4,5-trimethoxyphenylH195ClNH 2BrCH 23,4,5-TrimethylphenylH196ClNH 2BrCH 22-Chloro-3,4,5-trimethylphenylH197ClNH 2BrCH 22-Bromo-3,4,5-trimethylphenylH198ClNH 2BrCH 22-Iodo-3,4,5-trimethylphenylH199ClNH 2BrCH 22-Fluoro-3,4,5-trimethylphenylH200ClNH 2BrCH 23,5-Dimethoxy-4-methylphenylH201ClNH 2BrCH 22-Chloro-3,5-dimethoxy-4-methylphenylH202ClNH 2BrCH 22-Bromo-3,5-dimethoxy-4-methylphenylH203ClNH 2BrCH 22-Iodo-3,5-dimethoxy-4-mcthylphenylH204ClNH 2BrCH 22-Fluoro-3,5-dimethoxy-4-methylphenylH205ClNH 2ICH 23,4,5-TrimethoxyphenylH206ClNH 2ICH 22-Chloro-3,4,5-trimethoxyphenylH207ClNH 2ICH 22-Bromo-3,4,5-trimethoxyphenylH208ClNH 2ICH 22-Iodo-3,4,5-trimethoxyphenylH209ClNH 2ICH 22-Fluoro-3,4,5-trimethoxyphenylH210ClNH 2ICH 23,4,5-TrimethylphenylH211ClNH 2ICH 22-Chloro-3,4,5-trimethylphenylH212ClNH 2ICH 22-Bromo-3,4,5-trimethylphenylH213ClNH 2ICH 22-Iodo-3,4,5-trimethylphenylH214CLNH 2ICH 22-Fluoro-3,4,5-trimethylphenylH215ClNH 2ICH 23,5-Dimethoxy-4-methylphenylH216ClNH 2ICH 22-Chloro-3,5-dimethoxy-4-methylphenylH217ClNH 2ICH 22-Bromo-3,5-dimethoxy-4-methylphenylH218ClNH 2ICH 22-Iodo-3,5-dimethoxy-4-methylphenylH219ClNH 2ICH 22-Fluoro-3,5-dimethoxy-4-methylphenylH220ClNH 2CH 2 —CH 23,4,5-TrimethoxyphenylHNMe 2221ClNH 2CH 2 —CH 22-Chloro-3,4,5-trimethoxyphenylHNMe 2222ClNH 2CH 2 —CH 22-Bromo-3,4,5-trimethoxyphenylHNMe 2223ClNH 2CH 2 —CH 22-Iodo-3,4,5-trimethoxyphenylHNMe 2224ClNH 2CH 2 —CH 22-Fluoro-3,4,5-trimethoxyphenylHNMe 2225ClNH 2CH 2 —CH 23,4,5-TrimethylphenylHNMe 2226ClNH 2CH 2 —CH 22-Chloro-3,4,5-trimethylphenylHNMe 2227ClNH 2CH 2 —CH 22-Bromo-3,4,5-trimethylphenylHNMe 2228ClNH 2CH 2 —CH 22-Iodo-3,4,5-trimethylphenylHNMe 2229ClNH 2CH 2 —CH 22-Fluoro-3,4,5-trimethylphenylHNMe 2230ClNH 2CH 2 —CH 23,5-Dimethoxy-4-methylphenylHNMe 2231ClNH 2CH 2 —CH 22-Chloro-3,5-dimethoxy-4-methylphenylHNMe 2232ClNH 2CH 2 —CH 22-Bromo-3,5-dimethoxy-4-methylphenylHNMe 2233ClNH 2CH 2 —CH 22-Iodo-3,5-dimethoxy-4-methylphenylHNMe 2234ClNH 2CH 2 —CH 22-Fluoro-3,5-dimethoxy-4-methylphenylHNMe 2235ClNH 23-PyCH 23,4,5-TrimethoxyphenylH236ClNH 23-PyCH 22-Chloro-3,4,5-trimethoxyphenylH237ClNH 23-PyCH 22-Bromo-3,4,5-trimethoxyphenylH238ClNH 23-PyCH 22-Iodo-3,4,5-trimethoxyphenylH239ClNH 23-PyCH 22-Fluoro-3,4,5-trimethoxyphenylH2405ClNH 2HCH 23,5-Dimethyl-4-methoxypyridin-2-ylH2418ClNH 2HCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH242ClNH 2HCH 26-Bromo-3,5-dimethyl-4-methoxypyridin-2-ylH24310ClNH 2HCH 26-Chloro-3,5-dimethyl-4-methoxypyridin-2-ylH24413ClNH 2HCH 23,5-Dimethyl-4-bromopyridin-2-ylH24515ClNH 2HCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH24611ClNH 2HCH 23,5-Dimethyl-4-chloropyridin-2-ylH24714ClNH 2HCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH248ClNH 2HCH 23,5-Dimethyl-4-iodopyridin-2-ylH249ClNH 2HCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH250ClNH 2HCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH251ClNH 2HCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH252ClNH 2HCH 23,4,5-Trimethyl-pyridin-2-ylH253ClNH 2HCH 23,4,5-Trimethyl-1-oxypyridin-2-ylH254ClNH 2HCH 24,5,6-Trimethoxypyridin-2-ylH255ClNH 2HCH 24,5,6-Trimethoxy-1-oxypyridin-2-ylH256ClNH 2HCH 23-Bromo-4,5,6-trimethoxypyridin-2-ylH257ClNH 2HCH 23-Chloro-4,5,6-trimethoxypyridin-2-ylH258ClNH 2HCH 23,4,5-Trimethoxy-pyridin-2-ylH259ClNH 2HCH 23,4,5-Trimethoxy-1-oxypyridin-2-ylH260ClNH 2HCH 23-Bromo-3,4,5-trimethoxy-pyridin-2-ylH261ClNH 2HCH 23-Chloro-3,4,5-trimethoxy-pyridin-2-ylH262ClNH 2HCH 24,5,6-Trimethyl-pyridin-2-ylH263ClNH 2HCH 24,5,6-Trimethyl-1-oxypyridin-2-ylH264ClNH 2HCH 24,6-Dimethyl-5-methoxy-pyridin-2-ylH265ClNH 2HCH 24,6-Dimethyl-5-methoxypyridin-3-ylH266ClNH 2HCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH267ClNH 2HCH 24,6-Dimethyl-5-bromopyridin-3-ylH268ClNH 2HCH 24,6-Dimethyl-5-chloropyridin-3-ylH269ClNH 2HCH 25,6-Dimethyl-4-bromopyridin-3-ylH270ClNH 2HCH 25,6-Dimethyl-4-chloropyridin-3-ylH271ClNH 2HCH 22,6-Dimethyl-3-methoxypyridin-4-ylH272ClNH 2HCH 22,6-Dimethyl-pyridin-4-ylH273ClNH 2HCH 22,3,6-Trimethyl-pyridin-4-ylH274ClNH 2HCH 22,3,6-Trimethoxy-pyridin-4-ylH275ClNH 2HCH 22,6-Dimethyl-3-bromopyridin-4-ylH276ClNH 2HCH 22,6-Dimethyl-3-chloropyridin-4-ylH277ClNH 2HCH 22,6-Dimethyl-3-methoxy-1-oxy-pyridin-4-ylH278ClNH 2HCH 22,6-Dimethyl-1-oxy-pyridin-4-ylH279ClNH 2HCH 22,3,6-Trimethyl-1-oxy-pyridin-4-ylH280ClNH 2HCH 22,3,6-Trimethoxy-1-oxy-pyridin-4-ylH281ClNH 2HCH 22,6-Dimethyl-3-bromol-oxy-pyridin-4-ylH282ClNH 2HCH 22,6-Dimethyl-3-chlorol-oxy-pyridin-4-ylH283ClNH 2HCH 24,6-Dimethyl-5-iodopyridin-3-ylH284ClNH 2HCH 23,5-Dimethyl-4-aminopyridin-2-ylH285ClNH 2i-prCH 23,5-Dimethyl-4-methoxypyridin-2-ylH286ClNH 2i-prCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH287ClNH 2i-prCH 26-Bromo-3,5-dimethyl-4-methoxypyridin-2-ylH288ClNH 2i-prCH 26-Chloro-3,5-dimethyl-4-methoxypyridin-2-ylH289ClNH 2i-prCH 23,5-Dimethyl-4-bromopyridin-2-ylH290ClNH 2i-prCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH291ClNH 2i-prCH 23,5-Dimethyl-4-chloropyridin-2-ylH292ClNH 2i-prCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH293ClNH 2i-prCH 23,5-Dimethyl-4-iodopyridin-2-ylH294ClNH 2i-prCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH295ClNH 2i-prCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH296ClNH 2i-prCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH297ClNH 2i-prCH 23,4,5-Trimethyl-pyridin-2-ylH298ClNH 2i-prCH 23,4,5-Trimethyl-1-oxypyridin-2-ylH299ClNH 2i-prCH 24,5,6-Trimethoxypyridin-2-ylH300ClNH 2i-prCH 24,5,6-Trimethoxy-1-oxypyridin-2-ylH301ClNH 2i-prCH 23-Bromo-4,5,6-trimethoxypyridin-2-ylH302ClNH 2i-prCH 23-Chloro-4,5,6-trimethoxypyridin-2-ylH303ClNH 2i-prCH 23,4,5-Trimethoxy-pyridin-2-ylH304ClNH 2i-prCH 23,4,5-Trimethoxy-1-oxypyridin-2-ylH305ClNH 2i-prCH 23-Bromo-3,4,5-trimethoxy-pyridin-2-ylH306ClNH 2i-prCH 23-Chloro-3,4,5-trimethoxy-pyridin-2-ylH307ClNH 2i-prCH 24,5,6-Trimethyl-pyridin-2-ylH308ClNH 2i-prCH 24,5,6-Trimethyl-1-oxypyridin-2-ylH309ClNH 2i-prCH 24,6-Dimethyl-5-methoxy-pyridin-2-ylH310ClNH 2i-prCH 24,6-Dimethyl-5-methoxypyridin-3-ylH311ClNH 2i-prCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH312ClNH 2i-prCH 24,6-Dimethyl-5-bromopyridin-3-ylH313ClNH 2i-prCH 24,6-Dimethyl-5-chloropyridin-3-ylH314ClNH 2i-prCH 25,6-Dimethyl-4-bromopyridin-3-ylH315ClNH 2i-prCH 25,6-Dimethyl-4-chloropyridin-3-ylH316ClNH 2i-prCH 22,6-Dimethyl-3 -methoxypyridin-4-ylH317ClNH 2i-prCH 22,6-Dimethyl-pyridin-4-ylH318ClNH 2i-prCH 22,3,6-Trimethyl-pyridin-4-ylH319ClNH 2i-prCH 22,3,6-Trimethoxy-pyridin-4-ylH320ClNH 2i-prCH 22,6-Dimethyl-3-bromopyridin-4-ylH321ClNH 2i-prCH 22,6-Dimethyl-3-chloropyridin-4-ylH322ClNH 2i-prCH 22,6-Dimethyl-3-methoxy-1-oxy-pyridin-4-ylH323ClNH 2i-prCH 22,6-Dimethyl-1-oxy-pyridin-4-ylH324ClNH 2i-prCH 22,3,6-Trimethyl-1-oxy-pyridin-4-ylH325ClNH 2i-prCH 22,3,6-Trimethoxy-1-oxy-pyridin-4-ylH326ClNH 2i-prCH 22,6-Dimethyl-3-bromol-oxy-pyridin-4-ylH327ClNH 2i-prCH 22,6-Dimethyl-3-chlorol-oxy-pyridin-4-ylH328ClNH 2i-prCH 24,6-Dimethyl-5-iodopyridin-3-ylH329ClNH 2i-prCH 23,5-Dimethyl-4-aminopyridin-2-ylH330ClNH 2MeCH 23,5-Dimethyl-4-methoxypyridin-2-ylH331ClNH 2MeCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH332ClNH 2MeCH 23,5-Dimethyl-4-bromopyridin-2-ylH333ClNH 2MeCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH334ClNH 2MeCH 23,5-Dimethyl-4-chloropyridin-2-ylH335ClNH 2MeCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH336ClNH 2MeCH 23,5-Dimethyl-4-iodopyridin-2-ylH337ClNH 2MeCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH338ClNH 2MeCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH339ClNH 2MeCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH340ClNH 2MeCH 23,4,5-Trimethyl-pyridin-2-ylH341ClNH 2MeCH 23,4,5-Trimethyl-1-oxypyridin-2-ylH342ClNH 2MeCH 24,5,6-Trimethoxypyridin-2-ylH343ClNH 2MeCH 24,5,6-Trimethoxy-1-oxypyridin-2-ylH344ClNH 2MeCH 23,4,5-Trimethoxy-pyridin-2-ylH345ClNH 2MeCH 23,4,5-Trimethoxy-1-oxypyridin-2-ylH346ClNH 2MeCH 24,5,6-Trimethyl-pyridin-2-ylH347ClNH 2MeCH 24,5,6-Trimethyl-1-oxypyridin-2-ylH348ClNH 2MeCH 24,6-Dimethyl-5-methoxy-pyridin-2-ylH349ClNH 2MeCH 24,6-Dimethyl-5-methoxypyridin-3-ylH350ClNH 2MeCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH351ClNH 2MeCH 24,6-Dimethyl-5-bromopyridin-3-ylH352ClNH 2MeCH 24,6-Dimethyl-5-chloropyridin-3-ylH353ClNH 2MeCH 25,6-Dimethyl-4-bromopyridin-3-ylH354ClNH 2MeCH 25,6-Dimethyl-4-chloropyridin-3-ylH355ClNH 2MeCH 22,6-Dimethyl-3-methoxypyridin-4-ylH356ClNH 2MeCH 22,6-Dimethyl-pyridin-4-ylH357ClNH 2MeCH 22,3,6-Trimethyl-pyridin-4-ylH358ClNH 2MeCH 22,3,6-Trimethoxy-pyridin-4-ylH359ClNH 2MeCH 22,6-Dimethyl-3-bromopyridin-4-ylH360ClNH 2MeCH 22,6-Dimethyl-3-chloropyridin-4-ylH361ClNH 2MeCH 24,6-Dimethyl-5-iodopyridin-3-ylH362ClNH 2MeCH 23,5-Dimethyl-4-aminopyridin-2-ylH363ClNH 2EtCH 23,5-Dimethyl-4-methoxypyridin-2-ylH364ClNH 2EtCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH365ClNH 2EtCH 23,5-Dimethyl-4-bromopyridin-2-ylH366ClNH 2EtCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH367ClNH 2EtCH 23,5-Dimethyl-4-chloropyridin-2-ylH368ClNH 2EtCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH369ClNH 2EtCH 23,5-Dimethyl-4-iodopyridin-2-ylH370ClNH 2EtCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH371ClNH 2EtCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH372ClNH 2EtCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH373ClNH 2EtCH 23,4,5-Trimethyl-pyridin-2-ylH374ClNH 2EtCH 23,4,5-Trimethyl-1-oxypyridin-2-ylH375ClNH 2EtCH 24,5,6-Trimethoxypyridin-2-ylH376ClNH 2EtCH 24,5,6-Trimethoxy-1-oxypyridin-2-ylH377ClNH 2EtCH 23,4,5-Trimethoxy-pyridin-2-ylH378ClNH 2EtCH 23,4,5-Trimethoxy-1-oxypyridin-2-ylH379ClNH 2EtCH 24,5,6-Trimethyl-pyridin-2-ylH380ClNH 2EtCH 24,5,6-Trimethyl-1-oxypyridin-2-ylH381ClNH 2EtCH 24,6-Dimethyl-5-methoxy-pyridin-2-ylH382ClNH 2EtCH 24,6-Dimethyl-5-methoxypyridin-3-ylH383ClNH 2EtCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH384ClNH 2EtCH 24,6-Dimethyl-5-bromopyridin-3-ylH385ClNH 2EtCH 24,6-Dimethyl-5-chloropyridin-3-ylH386ClNH 2EtCH 25,6-Dimethyl-4-bromopyridin-3-ylH387ClNH 2EtCH 25,6-Dimethyl-4-chloropyridin-3-ylH388ClNH 2EtCH 22,6-Dimethyl-3-methoxypyridin-4-ylH389ClNH 2EtCH 22,6-Dimethyl-pyridin-4-ylH390ClNH 2EtCH 22,3,6-Trimethyl-pyridin-4-ylH391ClNH 2EtCH 22,3,6-Trimethoxy-pyridin-4-ylH392ClNH 2EtCH 22,6-Dimethyl-3-bromopyridin-4-ylH393ClNH 2EtCH 22,6-Dimethyl-3-chloropyridin-4-ylH394ClNH 2EtCH 24,6-Dimethyl-5-iodopyridin-3-ylH395ClNH 2EtCH 23,5-Dimethyl-4-aminopyridin-2-ylH396ClNH 22-PyCH 23,5-Dimethyl-4-methoxypyridin-2-ylH397ClNH 22-PyCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH398ClNH 22-PyCH 23,5-Dimethyl-4-bromopyridin-2-ylH399ClNH 22-PyCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH400ClNH 22-PyCH 23,5-Dimethyl-4-chloropyridin-2-ylH401ClNH 22-PyCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH402ClNH 22-PyCH 23,5-Dimethyl-4-iodopyridin-2-ylH403ClNH 22-PyCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH404ClNH 22-PyCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH405ClNH 22-PyCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH406ClNH 22-PyCH 23,4,5-Trimethyl-pyridin-2-ylH407ClNH 22-PyCH 23,4,5-Trimethyl-1-oxypyridin-2-ylH408ClNH 22-PyCH 24,5,6-Trimethoxypyridin-2-ylH409ClNH 22-PyCH 24,5,6-Trimethoxy-1-oxypyridin-2-ylH410ClNH 22-PyCH 23,4,5-Trimethoxy-pyridin-2-ylH411ClNH 22-PyCH 23,4,5-Trimethoxy-1-oxypyridin-2-ylH412ClNH 22-PyCH 24,5,6-Trimethyl-pyridin-2-ylH413ClNH 22-PyCH 24,5,6-Trimethyl-1-oxypyridin-2-ylH414ClNH 22-PyCH 24,6-Dimethyl-5-methoxy-pyridin-2-ylH415ClNH 22-PyCH 24,6-Dimethyl-5-methoxypyridin-3-ylH416ClNH 22-PyCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH417ClNH 22-PyCH 24,6-Dimethyl-5-bromopyridin-3-ylH418ClNH 22-PyCH 24,6-Dimethyl-5-chloropyridin-3-ylH419ClNH 22-PyCH 25,6-Dimethyl-4-bromopyridin-3-ylH420ClNH 22-PyCH 25,6-Dimethyl-4-chloropyridin-3-ylH421ClNH 22-PyCH 22,6-Dimethyl-3-methoxypyridin-4-ylH422ClNH 22-PyCH 22,6-Dimethyl-pyridin-4-ylH423ClNH 22-PyCH 22,3,6-Trimethyl-pyridin-4-ylH424ClNH 22-PyCH 22,3,6-Trimethoxy-pyridin-4-ylH425ClNH 22-PyCH 22,6-Dimethyl-3-bromopyridin-4-ylH426ClNH 22-PyCH 22,6-Dimethyl-3-chloropyridin-4-ylH427ClNH 22-PyCH 24,6-Dimethyl-5-iodopyridin-3-ylH428ClNH 22-PyCH 23,5-Dimethyl-4-aminopyridin-2-ylH429ClNH 2PhCH 23,5-Dimethyl-4-methoxypyridin-2-ylH430ClNH 2PhCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH431ClNH 2PhCH 23,5-Dimethyl-4-bromopyridin-2-ylH432ClNH 2PhCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH433ClNH 2PhCH 23,5-Dimethyl-4-chloropyridin-2-ylH434ClNH 2PhCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH435ClNH 2PhCH 23,5-Dimethyl-4-iodopyridin-2-ylH436ClNH 2PhCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH437ClNH 2PhCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH438ClNH 2PhCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH439ClNH 2PhCH 23,4,5-Trimethyl-pyridin-2-ylH440ClNH 2PhCH 23,4,5-Trimethyl-1-oxypyridin-2-ylH441ClNH 2PhCH 24,5,6-Trimethoxypyridin-2-ylH442ClNH 2PhCH 24,5,6-Trimethoxy-1-oxypyridin-2-ylH443ClNH 2PhCH 23,4,5-Trimethoxy-pyridin-2-ylH444ClNH 2PhCH 23,4,5-Trimethoxy-1-oxypyridin-2-ylH445ClNH 2PhCH 24,5,6-Trimethyl-pyridin-2-ylH446ClNH 2PhCH 24,5,6-Trimethyl-1-oxypyridin-2-ylH447ClNH 2PhCH 24,6-Dimethyl-5-methoxy-pyridin-2-ylH448ClNH 2PhCH 24,6-Dimethyl-5-methoxypyridin-3-ylH449ClNH 2PhCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH450ClNH 2PhCH 24,6-Dimethyl-5-bromopyridin-3-ylH451ClNH 2PhCH 24,6-Dimethyl-5-chloropyridin-3-ylH452ClNH 2PhCH 25,6-Dimethyl-4-bromopyridin-3-ylH453ClNH 2PhCH 25,6-Dimethyl-4-chloropyridin-3-ylH454ClNH 2PhCH 22,6-Dimethyl-3-methoxypyridin-4-ylH455ClNH 2PhCH 22,6-Dimethyl-pyridin-4-ylH456ClNH 2PhCH 22,3,6-Trimethyl-pyridin-4-ylH457ClNH 2PhCH 22,3,6-Trimethoxy-pyridin-4-ylH458ClNH 2PhCH 22,6-Dimethyl-3-bromopyridin-4-ylH459ClNH 2PhCH 22,6-Dimethyl-3-chloropyridin-4-ylH460ClNH 2PhCH 24,6-Dimethyl-5-iodopyridin-3-ylH461ClNH 2PhCH 23,5-Dimethyl-4-aminopyridin-2-ylH462ClNH 23-PyCH 23,5-Dimethyl-4-methoxypyridin-2-ylH463ClNH 23-PyCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH464ClNH 23-PyCH 23,5-Dimethyl-4-bromopyridin-2-ylH465ClNH 23-PyCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH466ClNH 23-PyCH 23,5-Dimethyl-4-chloropyridin-2-ylH467ClNH 23-PyCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH468ClNH 23-PyCH 23,5-Dimethyl-4-iodopyridin-2-ylH469ClNH 23-PyCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH470ClNH 23-PyCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH471ClNH 23-PyCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH472ClNH 23-PyCH 23,4,5-Trimethyl-pyridin-2-ylH473ClNH 23-PyCH 23,4,5-Trimethyl-1-oxypyridin-2-ylH474ClNH 23-PyCH 24,5,6-Trimethoxypyridin-2-ylH475ClNH 23-PyCH 24,5,6-Trimethoxy-1-oxypyridin-2-ylH476ClNH 23-PyCH 23,4,5-Trimethoxy-pyridin-2-ylH477ClNH 23-PyCH 23,4,5-Trimethoxy-1-oxypyridin-2-ylH478ClNH 23-PyCH 24,5,6-Trimethyl-pyridin-2-ylH479ClNH 23-PyCH 24,5,6-Trimethyl-1-oxypyridin-2-ylH480ClNH 23-PyCH 24,6-Dimethyl-5-methoxy-pyridin-2-ylH481ClNH 23-PyCH 24,6-Dimethyl-5-methoxypyridin-3-ylH482ClNH 23-PyCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH483ClNH 23-PyCH 24,6-Dimethyl-5-bromopyridin-3-ylH484ClNH 23-PyCH 24,6-Dimethyl-5-chloropyridin-3-ylH485ClNH 23-PyCH 25,6-Dimethyl-4-bromopyridin-3-ylH486ClNH 23-PyCH 25,6-Dimethyl-4-chloropyridin-3-ylH487ClNH 23-PyCH 22,6-Dimethyl-3-methoxypyridin-4-ylH488ClNH 23-PyCH 22,6-Dimethyl-pyridin-4-ylH489ClNH 23-PyCH 22,3,6-Trimethyl-pyridin-4-ylH490ClNH 23-PyCH 22,3,6-Trimethoxy-pyridin-4-ylH491ClNH 23-PyCH 22,6-Dimethyl-3-bromopyridin-4-ylH492ClNH 23-PyCH 22,6-Dimethyl-3-chloropyridin-4-ylH493ClNH 23-PyCH 24,6-Dimethyl-5-iodopyridin-3-ylH494ClNH 23-PyCH 23,5-Dimethyl-4-aminopyridin-2-ylH495ClNH 2CH 2 —CH 23,5-Dimethyl-4-methoxypyridin-2-ylHNMe 2496ClNH 2CH 2 —CH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylHNMe 2497ClNH 2CH 2 —CH 23,5-Dimethyl-4-bromopyridin-2-ylHNMe 2498ClNH 2CH 2 —CH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylHNMe 2499ClNH 2CH 2 —CH 23,5-Dimethyl-4-chloropyridin-2-ylHNMe 2500ClNH 2CH 2 —CH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylHNMe 2501ClNH 2CH 2 —CH 23,5-Dimethyl-4-iodopyridin-2-ylHNMe 2502ClNH 2CH 2 —CH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylHNMe 2503ClNH 2CH 2 —CH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylHNMe 2504ClNH 2CH 2 —CH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylHNMe 2505ClNH 2CH 2 —CH 23,4,5-Trimethyl-pyridin-2-ylHNMe 2506ClNH 2CH 2 —CH 23,4,5-Trimethyl-1-oxypyridin-2-ylHNMe 2507ClNH 2CH 2 —CH 24,5,6-Trimethoxypyridin-2-ylHNMe 2508ClNH 2CH 2 —CH 24,5,6-Trimethoxy-1-oxypyridin-2-ylHNMe 2509ClNH 2CH 2 —CH 23,4,5-Trimethoxy-pyridin-2-ylHNMe 2510ClNH 2CH 2 —CH 23,4,5-Trimethoxy-1-oxypyridin-2-ylHNMe 2511ClNH 2CH 2 —CH 24,5,6-Trimethyl-pyridin-2-ylHNMe 2512ClNH 2CH 2 —CH 24,5,6-Trimethyl-1-oxypyridin-2-ylHNMe 2513ClNH 2CH 2 —CH 24,6-Dimethyl-5-methoxy-pyridin-2-ylHNMe 2514ClNH 2CH 2 —CH 24,6-Dimethyl-5-methoxypyridin-3-ylHNMe 2515ClNH 2CH 2 —CH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylHNMe 2516ClNH 2CH 2 —CH 24,6-Dimethyl-5-bromopyridin-3-ylHNMe 2517ClNH 2CH 2 —CH 24,6-Dimethyl-5-chloropyridin-3-ylHNMe 2518ClNH 2CH 2 —CH 25,6-Dimethyl-4-bromopyridin-3-ylHNMe 2519ClNH 2CH 2 —CH 25,6-Dimethyl-4-chioropyridin-3-ylHNMe 2520ClNH 2CH 2 —CH 22,6-Dimethyl-3-methoxypyridin-4-ylHNMe 2521ClNH 2CH 2 —CH 22,6-Dimethyl-pyridin-4-ylHNMe 2522ClNH 2CH 2 —CH 22,3,6-Trimethyl-pyridin-4-ylHNMe 2523ClNH 2CH 2 —CH 22,3,6-Trimethoxy-pyridin-4-ylHNMe 2524ClNH 2CH 2 —CH 22,6-Dimethyl-3-bromopyridin-4-ylHNMe 2525ClNH 2CH 2 —CH 22,6-Dimethyl-3-chloropyridin-4-ylHNMe 2526ClNH 2CH 2 —CH 24,6-Dimethyl-5-iodopyridin-3-ylHNMe 2527ClNH 2CH 2 —CH 23,5-Dimethyl-4-aminopyridin-2-ylHNNe 2528ClNH 22-CH 23,5-Dimethyl-4-methoxypyridin-2-ylHfuranyl529ClNH 22-CH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylHfuranyl530ClNH 22-CH 23,5-Dimethyl-4-bromopyridin-2-ylHfuranyl531ClNH 22-CH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylHfuranyl532ClNH 22-CH 23,5 -Dimethyl-4-chloropyridin-2-ylHfuranyl533ClNH 22-CH 23,5 -Dimethyl-4-chloro-1-oxypyridin-2-ylHfuranyl534ClNH 22-CH 23,5-Dimethyl-4-iodopyridin-2-ylHfuranyl535ClNH 22-CH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylHfuranyl536ClNH 22-CH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylHfuranyl537ClNH 22-CH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylHfuranyl538ClNH 22-CH 23,4,5-Trimethyl-pyridin-2-ylHfuranyl539ClNH 22-CH 23,4,5-Trimethyl-1-oxypyridin-2-ylHfuranyl540ClNH 22-CH 24,5,6-Trimethoxypyridin-2-ylHfuranyl541ClNH 22-CH 24,5,6-Trimethoxy-1-oxypyridin-2-ylHfuranyl542ClNH 22-CH 23,4,5-Trimethoxy-pyridin-2-ylHfuranyl543ClNH 22-CH 23,4,5-Trimethoxy-1-oxypyridin-2-ylHfuranyl544ClNH 22-CH 24,5 ,6-Trimethyl-pyridin-2-ylHfuranyl545ClNH 22-CH 24,5,6-Trimethyl-1-oxypyridin-2-ylHfuranyl546ClNH 22-CH 24,6-Dimethyl-5-methoxy-pyridin-2-ylHfuranyl547ClNH 22-CH 24,6-Dimethyl-5-methoxypyridin-3 -ylHfuranyl548ClNH 22-CH24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylHfuranyl549ClNH 22-CH24,6-Dimethyl-5-bromopyridin-3 -ylHfuranyl550ClNH 22-CH24,6-Dimethyl-5-chloropyridin-3-ylHfuranyl551ClNH 22-CH25,6-Dimethyl-4-bromopyridin-3 -ylHfuranyl552ClNH 22-CH25,6-Dimethyl-4-chloropyridin-3-ylHfuranyl553ClNH 22-CH22,6-Dimethyl-3-methoxypyridin-4-ylHfuranyl554ClNH 22-CH22,6-Dimethyl-pyridin-4-ylHfuranyl555ClNH 22-CH22,3,6-Trimethyl-pyridin-4-ylHfuranyl556ClNH 22-CH22,3,6-Trimethoxy-pyridin-4-ylHfurany 1557ClNH 22-CH22,6-Dimethyl-3-bromopyridin-4-ylHfuranyl558ClNH 22-CH22,6-Dimethyl-3-chloropyridin-4-ylHfuranyl559ClNH 22-CH23,5-Dimethyl-4-aminopyridin-2-ylHfuranyl560ClNH 2ClCH 23,5-Dimethyl-4-methoxypyridin-2-ylH561ClNH 2ClCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH562ClNH 2ClCH 23,5-Dimethyl-4-bromopyridin-2-ylH563ClNH 2ClCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH564ClNH 2ClCH 23,5-Dimethyl-4-chloropyridin-2-ylH565ClNH 2ClCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH566ClNH 2ClCH 23,5-Dimethyl-4-iodopyridin-2-ylH567ClNH 2ClCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH568ClNH 2ClCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH569ClNH 2ClCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH570ClNH 2ClCH 23,4,5-Trimethyl-pyridin-2-ylH571ClNH 2ClCH 23,4,5-Trimethyl-1-oxypyridin-2-ylH572ClNH 2ClCH 24,6-Dimethyl-5-methoxypyridin-3-ylH573ClNH 2ClCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH574ClNH 2ClCH 23,5-Dimethyl-4-aminopyridin-2-ylH575ClNH 2BrCH 23,5-Dimethyl-4-methoxypyridin-2-ylH576ClNH 2BrCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH577ClNH 2BrCH 23,5-Dimethyl-4-bromopyridin-2-ylH578BrNH 2BrCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH579ClNH 2BrCH 23,5-Dimethyl-4-chloropyridin-2-ylH580BrNH 2BrCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH581ClNH 2BrCH 23,5-Dimethyl-4-iodopyridin-2-ylH582BrNH 2BrCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH583ClNH 2BrCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH584BrNH 2BrCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH585ClNH 2BrCH 23,4,5-Trimethyl-pyridin-2-ylH586BrNH 2BrCH 23,4,5-Trimethyl-1-oxypyridin-2-ylH587ClNH 2BrCH 24,6-Dimethyl-5-methoxypyridin-3-ylH588ClNH 2BrCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH589ClNH 2BrCH 23,5-Dimethyl-4-aminopyridin-2-ylH590ClNH 2ICH 23,5-Dimethyl-4-methoxypyridin-2-ylH591ClNH 2ICH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH592ClNH 2ICH 23,5-Dimethyl-4-bromopyridin-2-ylH593ClNH 2ICH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH594ClNH 2ICH 23,5-Dimethyl-4-chloropyridin-2-ylH595ClNH 2ICH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH596ClNH 2ICH 23,5-Dimethyl-4-iodopyridin-2-ylH597ClNH 2ICH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH598ClNH 2ICH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH599ClNH 2ICH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH600ClNH 2ICH 23,4,5-Trimethyl-pyridin-2-ylH601ClNH 2ICH 23,4,5-Trimethyl-1-oxypyridin-2-ylH602ClNH 2ICH 24,6-Dimethyl-5-methoxypyridin-3-ylH603ClNH 2ICH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH604ClNH 2ICH 23,5-Dimethyl-4-aminopyridin-2-ylH605ClNH 2CNCH 23,5-Dimethyl-4-methoxypyridin-2-ylH606ClNH 2CNCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH607ClNH 2CNCH 23,5-Dimethyl-4-bromopyridin-2-ylH608ClNH 2CNCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH609ClNH 2CNCH 23,5-Dimethyl-4-chloropyridin-2-ylH610ClNH 2CNCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH611ClNH 2CNCH 23,5-Dimethyl-4-iodopyridin-2-ylH612ClNH 2CNCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH613ClNH 2CNCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH614ClNH 2CNCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH615ClNH 2CNCH 23,4,5-Trimethyl-pyridin-2-ylH616ClNH 2CNCH 23,4,5-Trimethyl-1-oxypyridin-2-ylH617ClNH 2CNCH 24,6-Dimethyl-5-methoxypyridin-3-ylH618ClNH 2CNCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH619ClNH 2CNCH 23,5-Dimethyl-4-aminopyridin-2-ylH620ClNH 2HC(O)3,5-Dimethyl-4-methoxypyridin-2-ylH621ClNH 2HC(O)3,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH622ClNH 2HC(O)3,5-Dimethyl-4-bromopyridin-2-ylH623ClNH 2HC(O)3,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH624ClNH 2HC(O)3,5-Dimethyl-4-chloropyridin-2-ylH625ClNH 2HC(O)3,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH626ClNH 2HC(O)3,5-Dimethyl-4-iodopyridin-2-ylH627ClNH 2HC(O)3,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH628ClNH 2HC(O)3,5-Dimethyl-4-thiomethyl-pyridin-2-ylH629ClNH 2HC(O)3,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH630ClNH 2HC(O)3,4,5-Trimethyl-pyridin-2-ylH631ClNH 2HC(O)3,4,5-Trimethyl-1-oxypyridin-2-ylH632ClNH 2HC(O)4,6-Dimethyl-5-methoxypyridin-3-ylH633ClNH 2HC(O)4,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH634ClNH 2HC(O)3,5-Dimethyl-4-aminopyridin-2-ylH635ClNH 2HS(O)3,5-Dimethyl-4-methoxypyridin-2-ylH636ClNH 2HS(O)3,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH637ClNH 2HS(O)3,5-Dimethyl-4-bromopyridin-2-ylH638ClNH 2HS(O)3,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH639ClNH 2HS(O)3,5-Dimethyl-4-chloropyridin-2-ylH640ClNH 2HS(O)3,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH641ClNH 2HS(O)3,5-Dimethyl-4-iodopyridin-2-ylH642ClNH 2HS(O)3,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH643ClNH 2HS(O)3,5-Dimethyl-4-thiomethyl-pyridin-2-ylH644ClNH 2HS(O)3,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH645ClNH 2BrS(O)3,4,5-Trimethyl-pyridin-2-ylH646ClNH 2HS(O)3,4,5-Trimethyl-1-oxypyridin-2-ylH647ClNH 2BrS(O)4,6-Dimethyl-5-methoxypyridin-3-ylH648ClNH 2HS(O)4,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH649ClNH 2HSO 23,5-Dimethyl-4-methoxypyridin-2-ylH650ClNH 2HSO 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH651ClNH 2HSO 23,5-Dimethyl-4-bromopyridin-2-ylH652ClNH 2HSO 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH653ClNH 2BrSO 23,5-Dimethyl-4-chloropyridin-2-ylH654ClNH 2HSO 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH655ClNH 2HSO 23,5-Dimethyl-4-iodopyridin-2-ylH656ClNH 2HSO 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH657ClNH 2HSO 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH658ClNH 2HSO 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH659ClNH 2HSO 23,4,5-Trimethyl-pyridin-2-ylH660ClNH 2HSO 23,4,5-Trimethyl-1-oxypyridin-2-ylH661ClNH 2HSO 24,6-Dimethyl-5-methoxypyridin-3-ylH662ClNH 2HSO 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH663ClNH 2i-prC(O)3,5-Dimethyl-4-methoxypyridin-2-ylH664ClNH 2i-prC(O)3,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH665ClNH 2i-prC(O)3,5-Dimethyl-4-bromopyridin-2-ylH666ClNH 2i-prC(O)3,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH667ClNH 2i-prC(O)3,5-Dimethyl-4-chloropyridin-2-ylH668ClNH 2i-prC(O)3,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH669ClNH 2i-prC(O)3,5-Dimethyl-4-iodopyridin-2-ylH670ClNH 2i-prC(O)3,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH671ClNH 2i-prC(O)3,5-Dimethyl-4-thiomethyl-pyridin-2-ylH672ClNH 2i-prC(O)3,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH673ClNH 2i-prC(O)3,4,5-Trimethyl-pyridin-2-ylH674ClNH 2i-prC(O)3,4,5-Trimethyl-1-oxypyridin-2-ylH675ClNH 2i-prC(O)4,6-Dimethyl-5-methoxypyridin-3-ylH676ClNH 2i-prC(O)4,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH677ClNH 2i-prC(O)3,5-Dimethyl-4-aminopyridin-2-ylH678ClNH 2i-prS(O)3,5-Dimethyl-4-methoxypyridin-2-ylH679ClNH 2i-prS(O)3,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH680ClNH 2i-prS(O)3,5-Dimethyl-4-bromopyridin-2-ylH681ClNH 2i-prS(O)3,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH682ClNH 2i-prS(O)3,5-Dimethyl-4-chloropyridin-2-ylH683ClNH 2i-prS(O)3,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH684ClNH 2i-prS(O)3,5-Dimethyl-4-iodopyridin-2-ylH685ClNH 2i-prS(O)3,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH686ClNH 2i-prS(O)3,5-Dimethyl-4-thiomethyl-pyridin-2-ylH687ClNH 2i-prS(O)3,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH688ClNH 2i-prS(O)3,4,5-Trimethyl-pyridin-2-ylH689ClNH 2i-prS(O)3,4,5-Trimethyl-1-oxypyridin-2-ylH690ClNH 2i-prS(O)4,6-Dimethyl-5-methoxypyridin-3-ylH691ClNH 2i-prS(O)4,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH692ClNH 2i-prSO 23,5-Dimethyl-4-methoxypyridin-2-ylH693ClNH 2i-prSO 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH694ClNH 2i-prSO 23,5-Dimethyl-4-bromopyridin-2-ylH695ClNH 2i-prSO 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH696ClNH 2i-prSO 23,5-Dimethyl-4-chloropyridin-2-ylH697ClNH 2i-prSO 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH698ClNH 2i-prSO 23,5-Dimethyl-4-iodopyridin-2-ylH699ClNH 2i-prSO 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH700ClNH 2i-prSO 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH701ClNH 2i-prSO 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH702ClNH 2i-prSO 23,4,5-Trimethyl-pyridin-2-ylH703ClNH 2i-prSO 23,4,5-Trimethyl-1-oxypyridin-2-ylH704ClNH 2i-prSO 24,6-Dimethyl-5-methoxypyridin-3-ylH705ClNH 2i-prSO 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH706ClNH 2HC(O)3,4,5-TrimethoxyphenylH707ClNH 2HC(O)2-Chloro-3,4,5-trimethoxyphenylH708ClNH 2HC(O)2-Bromo-3,4,5-trimethoxyphenylH709ClNH 2HC(O)3,5-Dimethyl-4-methoxyphenylH710ClNH 2HC(O)2-Chloro-3,5-Dimethyl-4-methoxyphenylH711ClNH 2HC(O)2-Bromo-3,5-Dimethyl-4-methoxyphenylH712ClNH 2HSO 23,4,5-TrimethoxyphenylH713ClNH 2HSO 22-Chloro-3,4,5-trimethoxyphenylH714ClNH 2HSO 22-Bromo-3,4,5-trimethoxyphenylH715ClNH 2HSO 23,5-Dimethyl-4-methoxyphenylH716ClNH 2HSO 22-Chloro-3,5-Dimethyl-4-methoxyphenylH717ClNH 2HSO 22-Bromo-3,5-Dimethyl-4-methoxyphenylH718ClNH 2HCH 23,5-Dimethyl-4-methoxypyridin-2-ylBr719ClNH 2HCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylBr720ClNH 2HCH 23,5-Dimethyl-4-bromopyridin-2-ylBr721ClNH 2HCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylBr722ClNH 2HCH 23,5-Dimethyl-4-chloropyridin-2-ylBr723ClNH 2HCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylBr724ClNH 2HCH 23,5-Dimethyl-4-iodopyridin-2-ylBr725ClNH 2HCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylBr726ClNH 2HCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylBr727ClNH 2HCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylBr728ClNH 2HCH 23,4,5-Trimethyl-pyridin-2-ylBr729ClNH 2HCH 23,4,5-Trimethyl-1-oxypyridin-2-ylBr730ClNH 2HCH 24,6-Dimethyl-5-methoxypyridin-3-ylBr731ClNH 2HCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylBr732ClNH 2HCH 23,5-Dimethyl-4-methoxypyridin-2-ylCl733ClNH 2HCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylCl734ClNH 2HCH 23,5-Dimethyl-4-bromopyridin-2-ylCl735ClNH 2HCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylCl736ClNH 2HCH 23,5-Dimethyl-4-chloropyridin-2-ylCl737ClNH 2HCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylCl738ClNH 2HCH 23,5-Dimethyl-4-iodopyridin-2-ylCl739ClNH 2HCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylCl740ClNH 2HCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylCl741ClNH 2HCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylCl742ClNH 2HCH 23,4,5-Trimethyl-pyridin-2-ylCl743ClNH 2HCH 23,4,5-Trimethyl-1-oxypyridin-2-ylCl744ClNH 2HCH 24,6-Dimethyl-5-methoxypyridin-3-ylCl745ClNH 2HCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylCl746ClNH 2HCH 23,5-Dimethyl-4-methoxypyridin-2-ylCN747ClNH 2HCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylCN748ClNH 2HCH 23,5-Dimethyl-4-bromopyridin-2-ylCN749ClNH 2HCH 23,5-Dimethyl-4-bromo-1-oxypridin-2-y1CN750ClNH 2HCH 23,5-Dimethyl-4-chloropyridin-2-ylCN751ClNH 2HCH 23,5-Dimethy1-4-cMoro-1-ox˜yridin-2-y1CN752ClNH 2HCH 23,5-Dimethyl-4-iodopyridin-2-ylCN75325BrNH 2HCH 23,5-Dimethyl-4-methoxypyridin-2-ylH75420BrNH 2HCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH755BrNH 2HCH 26-Bromo-3,5-dimethyl-4-methoxypyridin-2-ylH756BrNH 2HCH 26-Chloro-3,5-dimethyl-4-methoxypyridin-2-ylH75723BrNH 2HCH 23,5-Dimethyl-4-bromopyridin-2-ylH75824BrNH 2HCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH75921BrNH 2HCH 23,5-Dimethyl-4-chloropyridin-2-ylH76022BrNH 2HCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH761BrNH 2HCH 23,5-Dimethyl-4-iodopyridin-2-ylH762BrNH 2HCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH763BrNH 2HCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH764BrNH 2HCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH765BrNH 2HCH 23,4,5-Trimethyl-pyridin-2-ylH766BrNH 2HCH 23,4,5-Trimethyl-1-oxypyridin-2-ylH767BrNH 2HCH 24,5,6-Trimethoxypyridin-2-ylH768BrNH 2HCH 24,5,6-Trimethoxy-1-oxypyridin-2-ylH769BrNH 2HCH 23-Bromo-4,5,6-trimethoxypyridin-2-ylH770BrNH 2HCH 23-Chloro-4,5,6-trimethoxypyridin-2-ylH771BrNH 2HCH 23,4,5-Trimethoxy-pyridin-2-ylH772BrNH 2HCH 23,4,5-Trimethoxy-1-oxypyridin-2-ylH773BrNH 2HCH 23-Bromo-3,4,5-trimethoxy-pyridin-2-ylH774BrNH 2HCH 23-Chloro-3,4,5-trimethoxy-pyridin-2-ylH775BrNH 2HCH 24,5,6-Trimethyl-pyridin-2-ylH776BrNH 2HCH 24,5,6-Trimethyl-1-oxypyridin-2-ylH777BrNH 2HCH 24,6-Dimethyl-5-methoxy-pyridin-2-ylH778BrNH 2HCH 24,6-Dimethyl-5-methoxypyridin-3-ylH779BrNH 2HCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH780BrNH 2HCH 24,6-Dimethyl-5-bromopyridin-3-ylH781BrNH 2HCH 24,6-Dimethyl-5-chloropyridin-3-ylH782BrNH 2HCH 25,6-Dimethyl-4-bromopyridin-3-ylH783BrNH 2HCH 25,6-Dimethyl-4-chloropyridin-3-ylH784BrNH 2HCH 22,6-Dimethyl-3-methoxypyridin-4-ylH785BrNH 2HCH 22,6-Dimethyl-pyridin-4-ylH786BrNH 2HCH 22,3,6-Trimethyl-pyridin-4-ylH787BrNH 2HCH 22,3,6-Trimethoxy-pyridin-4-ylH788BrNH 2HCH 22,6-Dimethyl-3-bromopyridin-4-ylH789BrNH 2HCH 22,6-Dimethyl-3-chloropyridin-4-ylH790BrNH 2HCH 22,6-Dimethyl-3-methoxy-1-oxy-pyridin-4-ylH791BrNH 2HCH 22,6-Dimethyl-1-oxy-pyridin-4-ylH792BrNH 2HCH 22,3,6-Trimethyl-1-oxy-pyridin-4-ylH793BrNH 2HCH 22,3,6-Trimethoxy-1-oxy-pyridin-4-ylH794BrNH 2HCH 22,6-Dimethyl-3-bromol-oxy-pyridin-4-ylH795BrNH 2HCH 22,6-Dimethyl-3-chlorol-oxy-pyridin-4-ylH796BrNH 2HCH 24,6-Dimethyl-5-iodopyridin-3-ylH797BrNH 2HCH 23,5-Dimethyl-4-aminopyridin-2-ylH798BrNH 2i-prCH 23,5-Dimethyl-4-methoxypyridin-2-ylH799BrNH 2i-prCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH800BrNH 2i-prCH 26-Bromo-3,5-dimethyl-4-methoxypyridin-2-ylH801BrNH 2i-prCH 26-Chloro-3,5-dimethyl-4-methoxypyridin-2-ylH802BrNH 2i-prCH 23,5-Dimethyl-4-bromopyridin-2-ylH803BrNH 2i-prCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH804BrNH 2i-prCH 23,5-Dimethyl-4-chloropyridin-2-ylH805BrNH 2i-prCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH806BrNH 2i-prCH 23,5-Dimethyl-4-iodopyridin-2-ylH807BrNH 2i-prCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH808BrNH 2i-prCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH809BrNH 2i-prCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH810BrNH 2i-prCH 23,4,5-Trimethyl-pyridin-2-ylH811BrNH 2i-prCH 23,4,5-Trimethyl-1-oxypyridin-2-ylH812BrNH 2i-prCH 24,5,6-Trimethoxypyridin-2-ylH813BrNH 2i-prCH 24,5,6-Trimethoxy-1-oxypyridin-2-ylH814BrNH 2i-prCH 23-Bromo-4,5,6-trimethoxypyridin-2-ylH815BrNH 2i-prCH 23-Chloro-4,5,6-trimethoxypyridin-2-ylH816BrNH 2i-prCH 23,4,5-Trimethoxy-pyridin-2-ylH817BrNH 2i-prCH 23,4,5-Trimethoxy-1-oxypyridin-2-ylH818BrNH 2i-prCH 23-Bromo-3,4,5-trimethoxy-pyridin-2-ylH819BrNH 2i-prCH 23-Chloro-3,4,5-trimethoxy-pyridin-2-ylH820BrNH 2i-prCH 24,5,6-Trimethyl-pyridin-2-ylH821BrNH 2i-prCH 24,5,6-Trimethyl-1-oxypyridin-2-ylH822BrNH 2i-prCH 24,6-Dimethyl-5-methoxy-pyridin-2-ylH823BrNH 2i-prCH 24,6-Dimethyl-5-methoxypyridin-3-ylH824BrNH 2i-prCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH825BrNH 2i-prCH 24,6-Dimethyl-5-bromopyridin-3-ylH826BrNH 2i-prCH 24,6-Dimethyl-5-chloropyridin-3-ylH827BrNH 2i-prCH 25,6-Dimethyl-4-bromopyridin-3-ylH828BrNH 2i-prCH 25,6-Dimethyl-4-chloropyridin-3-ylH829BrNH 2i-prCH 22,6-Dimethyl-3-methoxypyridin-4-ylH830BrNH 2i-prCH 22,6-Dimethyl-pyridin-4-ylH831BrNH 2i-prCH 22,3,6-Trimethyl-pyridin-4-ylH832BrNH 2i-prCH 22,3,6-Trimethoxy-pyridin-4-ylH833BrNH 2i-prCH 22,6-Dimethyl-3-bromopyridin-4-ylH834BrNH 2i-prCH 22,6-Dimethyl-3-chloropyridin-4-ylH835BrNH 2i-prCH 22,6-Dimethyl-3-methoxy-1-oxypyridin-4-ylH836BrNH 2i-prCH 22,6-Dimethyl-1-oxy-pyridin-4-ylH837BrNH 2i-prCH 22,3,6-Trimethyl-1-oxypyridin-4-ylH838BrNH 2i-prCH 22,3,6-Trimethoxy-1-oxypyridin-4-ylH839BrNH 2i-prCH 22,6-Dimethyl-3-bromol-oxypyridin-4-ylH840BrNH 2i-prCH 22,6-Dimethyl-3-chlorol-oxypyridin-4-ylH841BrNH 2i-prCH 24,6-Dimethyl-5-iodopyridin-3-ylH842BrNH 2i-prCH 23,5-Dimethyl-4-aminopyridin-2-ylH843BrNH 2PhCH 23,5-Dimethyl-4-methoxypyridin-2-ylH844BrNH 2PhCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH845BrNH 2PhCH 26-Bromo-3,5-dimethyl-4-methoxypyridin-2-ylH846BrNH 2PhCH 26-Chloro-3,5-dimethyl-4-methoxypyridin-2-ylH847BrNH 2PhCH 23,5-Dimethyl-4-bromopyridin-2-ylH848BrNH 2PhCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH849BrNH 2PhCH 23,5-Dimethyl-4-chloropyridin-2-ylH850BrNH 2PhCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH851BrNH 2PhCH 23,5-Dimethyl-4-iodopyridin-2-ylH852BrNH 2PhCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH853BrNH 2PhCH 23,5-Dimethyl-4-thiomethyl-pyridin-2-ylH854BrNH 2PhCH 23,5-Dimethyl-4-thiomethyl-1-oxypyridin-2-ylH855BrNH 2PhCH 23,4,5-Trimethyl-pyridin-2-ylH856BrNH 2PhCH 23,4,5-Trimethyl-1-oxypyridin-2-ylH857BrNH 2PhCH 24,5,6-Trimethoxypyridin-2-ylH858BrNH 2PhCH 24,5,6-Trimethoxy-1-oxypyridin-2-ylH859BrNH 2PhCH 23-Bromo-4,5,6-trimethoxypyridin-2-ylH860BrNH 2PhCH 23-Chloro-4,5,6-trimethoxypyridin-2-ylH861BrNH 2PhCH 24,6-Dimethyl-5-methoxypyridin-3-ylH862BrNH 2PhCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH863BrNH 2MeCH 23,5-Dimethyl-4-methoxypyridin-2-ylH864BrNH 2MeCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH865BrNH 2MeCH 26-Bromo-3,5-dimethyl-4-methoxypyridin-2-ylH866BrNH 2MeCH 26-Chloro-3,5-dimethyl-4-methoxypyridin-2-ylH867BrNH 2MeCH 23,5-Dimethyl-4-bromopyridin-2-ylH868BrNH 2MeCH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH869BrNH 2MeCH 23,5-Dimethyl-4-chloropyridin-2-ylH870BrNH 2MeCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH871BrNH 2MeCH 23,5-Dimethyl-4-iodopyridin-2-ylH872BrNH 2MeCH 23,5-Dimethyl-4-iodo-1-oxypyridin-2-ylH873BrNH 2MeCH 24,6-Dimethyl-5-methoxypyridin-3-ylH874BrNH 2MeCH 24,6-Dimethyl-5-methoxy-1-oxypyridin-3-ylH87539ClNH 2CH 2CH 23,5-Dimethyl-4-methoxypyridin-2-ylH(Bn) 287612ClNH 2HCH 22-Chloro-4,5-dimethoxylphenylH87716ClNH 2HCH 22-Nitro-4,5-dimethoxylphenylH87817ClNH 2HCH 23,4-DichlorophenylH87918ClNH 2HCH 23,5-DIMETHOXYLPHENYLH88019ClNH 2HCH 22,5-DIMETHOXYLPHENYLH88126BrNH 2HCH 23,5-DIMETHOXYLPHENYLH88227ClNH 2HCH 23-METHOXYLPHENYLH88328ClNH 2HCH 24-METHOXYLPHENYLH88429ClICH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH88530ClICH 23,5-Dimethyl-4-bromo-1-oxypyridin-2-ylH88631ClICH 23,5-Dimethyl-4-methoxypyridin-2-ylH88732ClHCH 23,5-DIMETHYL-4-BROMO-1-OXYPYRIDIN-2-YLH88833ClHCH 23,5-Dimethyl-4-methoxypyridin-2-ylH88934ClHCH 23,5-Dimethyl-4-methoxy-1-oxypyridin-2-ylH89035ClHCH 23,5-Dimethyl-4-chloropyridin-2-ylH89136ClICH 23,5-Dimethyl-4-chloropyridin-2-ylH89237ClHCH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH89338ClICH 23,5-Dimethyl-4-chloro-1-oxypyridin-2-ylH Compounds of interest in Table 1 are compounds 2, 3, 17, 18, 27, 28, 62, 63, 77, 78, 92, 93, 129, 130, 238, 239, 242,243, 245, 246, 247, 248, 249, 250, 251, 252, 253, 267, 268, 287, 288, 291, 292, 293, 294, 295, 296, 297, 298, 312, 313, 332, 333, 334, 335, 336, 337, 338, 339, 351, 352, 365, 366, 384, 385, 398, 399,400, 401, 402, 403, 404, 405, 417, 418, 431, 432, 433, 434, 435, 436, 437, 438, 450, 451, 464, 465, 483, 484, 497, 498, 530, 531, 549, 550, 562, 563, 574, 575, 577, 578, 589, 590, 592, 593, 604, 605, 607, 608, 619, 620, 755, 756, 759, 760, 761, 762, 763, 764, 765, 766, 780, 781, 800, 801, 804, 805, 806, 807, 808, 809, 810, 811, 825, 826, 845, 846, 863, 864, 865, 866, 875, and 876 with the selected ones being 17, 18, 27, 28, 62, 63, 77, 78, 242, 243, 245, 246, 247, 248, 249, 250, 251, 252, 253, 267, 268, 287, 288, 291, 292, 293, 294, 295, 296, 312, 313, 431, 432, 755, 756, 759, 760, 761, 762, 763, 764, 800, and 801. III. Synthesis of the Compounds of the Invention The compounds of Formula I of the present invention may be synthesized by various methods known in the art. The general strategy is outlined in Scheme 1 and consists of three parts: (1) constructing the bicyclic system, starting from either a pyridine or a pyrrole, or an acyclic precursor (2) appending the R 5 -R 4 -group, and (3) further elaborating the ring systems. Importantly, one skilled in the art will recognize that the sequence of events is not necessarily (1)-(2)-(3), and that these events may be interchanged, provided there be no incompatibility between the reagents and the functional groups specific to the case in point. Also, the starting materials or the intermediates of Formula 1, 4, 5, and I can exist in tautomeric forms as shown in FIG. 1, and both forms are indiscriminately used in this patent. 1. Assembly of the pyrrolo[2,3-d]pyrimidine 1.1. Assembly of the pyrrolo[2,3-d]pyrimidine Starting from a Pyrimidine The compounds of Formula 4 can be prepared from pyrimidines as outlined in Scheme 2. For instance: Methods 1.1.1 The compounds of Formula 4 can be made by intramolecular cyclization of an aldehyde or ketone, possibly protected, as in Formula 6. (See, J. Davoll, J. Chem. Soc. 1960, 131; J. A. Montgomery, J. Chem. Soc. 1967, 665; G. Cristalli, J. Med. Chem. 1988, 31, 390; T. Miwa, J. Org. Chem. 1993, 58, 1696; D. M. Williams, J. Chem. Soc., Perkin Trans 1, 1997, 1171). Method 1.1.2 The compounds of Formula 4, wherein R 3 is H, R 6 is Cl, and R 7 is NH 2 can be prepared by treating compounds of Formula 7 wherein R is a halogen or a leaving group with ammonia. Similarly, compounds of Formula I wherein R 3 is H, R 1 is Cl, R 2 is NH 2 can be prepared by treating the compound of Formula 7 wherein R is a halogen or leaving group with R 5 —R 4 —NH 2 in butanol at reflux in presence of a base such as K 2 CO 3 , Cs 2 CO 3 or iPrNEt 2 . (A. B. Reitz J. Med. Chem. 1994, 37, 3561). Compounds of Formula 7 can in turn be prepared as taught by G. W. Craig, J. Prakt. Chem. 2000, 342, 504 and M. Semonsky, Coll. Czech. Chem. Commun. 1980, 45, 3583). Method 1.1.3: The compounds of Formula 4 can be obtained by treatment of a α-haloketone of Formula 8 wherein X is a halogen with ammonia or a synthetic equivalent thereof. Method 1.1.4: The compounds of Formula 4 wherein R 0 is methyl can be obtained by a tandem Pd-mediated intramolecular cyclization/double-bond migration of alkenes of Formula 9 (S. E. Watson, Synth. Commun. 1998, 28, 3885). Method 1.1.5: The compounds of Formula 4 wherein R 3 is H can be obtained by Pd-mediated intramolecular cyclization of alkynes of Formula 10, wherein Z in as electron-withdrawing group such as, e.g., tosyl-, or —CO 2 Et. Method 1.1.6: The compounds of Formula 4 wherein R 3 is AcO— can be obtained by intramolecular Friedel-Crafts acylation of precursors of Formula 11 (E. D. Edstrom, J. Org. Chem. 1993, 58, 403). Method 1.1.7: The compound of Formula 4, wherein R 0 is H, R 6 is OH, and R 7 is NH 2 , can be prepared by treating the compound of Formula 12 with an α-haloaldehyde of the formula R 3 —CHX—CHO. See, D. M. Williams, J. Chem. Soc., Perkin Trans 1, 1997, 1171; C. J. Barnett, Org. Proc. Res. Devop. 1999, 3, 184; A. Gangjee, J. Med. Chem. 2001, 44, 1993. Method 1.1.8: The compounds of Formula 4, wherein R 6 is OH and R 7 is NH 2 can be obtained by treating the compound of Formula 13 with an aldehyde of the formula R 3 —CHO. See, A. Gangjee, J. Med. Chem. 2003, 46, 591; E. C. Taylor, Heterocycles 1996, 43, 323. 1.2: Assembly of the pyrrolo[2,3-d]pyrimidine Starting from a Pyrrole The compounds of Formula 4 can also be made from pyrroles of Formula 2. There is a variety of methods by which the 6-membered ring can be formed (e.g. R. J. Bontems, J. Med Chem, 1990, 33, 2174 and references therein). For instance: Compounds of Formula 2 wherein R 13 is —CN and R 14 is R—NH—CR 7 ═N— can be cyclized and rearranged to give compounds of Formula 4 where R 6 is R—NH—. See, E. C. Taylor, J. Am. Chem. Soc. 1965, 87, 1995. Compounds of Formula 2 wherein R 13 is —CN and R 14 is NH 2 can be treated with thiourea, guanidine, or chloroformamidine to give compounds of Formula 4 in which R 6 is —NH 2 and R 7 is —NH 2 . See, H. Kosaku, Heterocycles, 2001, 55, 2279; A. Gangjee, U.S. Pat. No. 5,939,420 (1999). Compounds of Formula 2 wherein R 13 is —CN and R 14 is NH 2 can be treated with formamidine acetate to give compounds of Formula 4 wherein R 6 is NH 2 and R 7 is H (J. A. Montgomery, J. Chem. Soc. 1967, 665). The same transformation can be accomplished by treatment with DMF-DMA or an orthoester such as (EtO) 3 CH, followed by treatment with ammonia. See, E. C. Taylor, J. Am. Chem. Soc, 1965, 87, 1995. Compounds of Formula 2 wherein R 13 is —CN and R 14 is NH 2 can be treated with formic acid to give compounds of Formula 4 wherein R 6 is OH and R 7 is H (K. A. M. El-Bayouki, J. Chem. Res. Miniprint, 1995, 1901). Compounds of Formula 2 wherein R 13 is —CO 2 NH 2 and R 14 is —NH 2 can be treated under Vilsmeyer-Haack conditions (DMF/POCl 3 ) to give compounds of Formula 4 wherein R 6 is OH or Cl and R 7 is H. See, K. A. M. El-Bayouki, J. Chem. Res. Miniprint, 1995, 1901. Compounds of Formula 2 wherein R 13 is —CONH 2 and R 14 is —NH 2 can be treated with CS 2 or EtOCS 2 K to give compounds of Formula 4 in which R 6 is —OH and R 7 is —SH. See, S. M. Bennett, J. Med. Chem. 1990, 33, 2162. 1.3. Assembly of the pyrrolo[2,3-d]pyrimidine Starting from an Acyclic Precursor The compounds of Formula 14 can be prepared from an acyclic precursor as outlined in Scheme 4 (T. Miwa, J. Med. Chem. 1991, 34, 555). 2. Incorporation of the —R 4 —R 5 Fragment. 2.1. Alkylation of Compounds of Formula 4. Compounds of Formula 4 can be alkylated in the presence of a base such as K 2 CO 3 , NaH, Cs 2 CO 3 , DBU etc. with/without the presence of a catalyst such as NaI, KI, (Bu) 4 NI etc., and in a polar solvent such as DMF, THF, DMSO etc. using electrophiles such as L 1 -R 4 —R 5 where L 1 is a leaving group. See Scheme 5. Leaving groups include but are not limited to, e.g., halogen, triflate, tosylate, mesylate, triphenylphosphonium (generated under Mitsunobu conditions, e.g. PPh 3 /DEAD) etc. See Kasibhatla, PCT publication number WO 03/037860. 2.2. Preparation of Electrophiles L 1 -R 4 —R 5 wherein L 1 is a Leaving Group 2.2.1. Synthesis of Benzyl Type Electrophile: The electrophiles can be prepared from the substituted benzene derivatives using various methods reported in the literature, see Jerry March, Advanced Organic Chemistry, 4 th edition; Larock, Comprehensive Organic Transformations, 1989, VCH, New York. For example the compounds wherein L 1 is Br can be prepared by reduction of the corresponding benzoic acid or benzaldehyde, followed by halogenation. These benzyl derivatives can also be prepared by benzylic oxidation or benzylic halogenation. Further modification of the benzyl ring can be done before or after the pyrrolo[2,3-d]pyrimidine alkylation step. 2.2.2. Synthesis of Pyridyl Methyl Type Electrophile: These compounds can be prepared by many methods reported in the literature. Morisawa, J. Med. Chem. 1974,17, 1083; Klaus, W., J. Med. Chem. 1992, 35, 438; Abramovitch, R. A.; Smith, E. M. “Pyridine-1-oxide in Pyridine and its Derivatives,” in The Chemistry of Heterocyclic Compounds ; Weissberger, A., Taylor, E. C., Eds.; John Wiley, New York, 1974, Pt. 2, pp 1–261; Jeromin, G. E., Chem. Ber. 1987,120, 649. Blanz, E. J., J. Med. Chem. 1970, 13, 1124; Smith, Kline and French, EP Application EP 0184322, 1986; Abblard, J., Bull. Soc. Chim. Fr. 1972, 2466; Fisher, B. E., The Structure of Isomaltol. J. Org. Chem. 1964, 29, 776. De Cat, A., Bull. Soc. Chim. Belg. 1965, 74, 270; Looker, J. H., J. Org. Chem. 1979, 44, 3407. Ackerman, J. F. Ph.D. Dissertation, University of Notre Dame, June, 1949. These methods can be applied to the synthesis of quinoline and isoquinoline type compounds. 2.3. Incorporation of the —R 4 —R 5 Fragment by Nucleophilic Substitution. In some cases, the —R 4 —R 5 group can be appended before the bicyclic pyrrolo[2,3-d]pyrimidine bicyclic ring is constructed, and this is further detailed below (paragraph 4, schemes 8 and 9). In these cases the —R 4 —R 5 group can be appended by an aromatic nucleophilic substitution using NH 2 —R 4 —R 5 . The compound NH 2 —R 4 —R 5 is obtained by treating L 1 -R 4 —R 5 with ammonia at temperatures of 20–160° C. in a pressure vessel. The corresponding amines where L 1 is —NH 2 can be prepared by a variety of methods, for instance from compounds where L 1 is leaving group such as chloride, bromide, tosylate, mesylate etc. using ammonia, or with sodium azide followed by hydrogenation. 3. Further Elaboration of the Ring Systems. 3.1. Functional Group Interconversions of R 0 : Compounds of Formula I, wherein R 0 is H can be oxidized to compounds of Formula I wherein R 0 is OH with pyridinium tribromide or polymer supported pyridinium tribromide in tert-butanol/acetic acid mixture followed by zinc reduction. See, C. Liang, U.S. Pat. No. 6,610,688 (2000); L. Sun, Bioorg. Med. Chem Lett., 2002, 12, 2153. Compounds of Formula I, wherein R 0 is H can be treated under Mannich conditions (HCHO+HNRR′) to give compounds Formula I wherein R 0 is —CH—NRR′. See, F. Seela, Synthesis, 1997, 1067. Compounds of Formula I, wherein R 0 is H can be lithiated and treated with electrophiles (e.g., I 2 , ArCHO) to provide compounds of Formula I wherein R 0 is, e.g. —I or —CH(OH)Ar. See, E. Bisagni, Tetrahedron, 1983, 39, 1777; T, Sakamoto, Tetrahedron Lett. 1994, 35, 2919; T. Sakamoto, J. Chem. Soc., Perkin Trans 1, 1996, 459. 3.2. Functional Group Interconversions of R 1 : Compounds of Formula I, wherein R 1 is OH, can be converted to halides using standard conditions POCl 3 , POBr 3 etc. with/without a base such as Et 3 N, N,N-dimethylaniline, (iPr) 2 NEt etc. and with/without a catalyst such as BnEt 3 N + Cl − , in polar solvents such as CH 3 CN, CH 2 Cl 2 etc. Related methods include, but are not limited to, SOCl 2 /DMF (M. J. Robins, Can. J. Chem. 1973, 12, 3161), PPh 3 /CCl 4 (L. De Napoli , J. Chem. Soc. Perkin Trans 1, 1994, 923), HMPT/CCl 4 or HMPT/NBS (E. A. Veliz, Tetrahedron Lett, 2000, 41, 1695) or PPh 3 /I 2 (X. Lin, Org. Letters, 2000, 2, 3497). Compounds of Formula I, wherein R 1 is NH 2 , can be converted to halides by a Balz-Schiemann (F) or Sandmeyer reaction (Cl, Br, I) by means of a nitrosylating agent (NaNO 2 /H + , NOBF 4 , RONO) and a halogen donor (BF 4 − , CuX 2 , SbX 3 ). Compounds of Formula I, wherein R 1 is alkyl can be prepared from compounds of Formula 4 where R 1 is halogen and trialkyl aluminum or dialkyl zinc (A. Holy, J. Med. Chem. 1999, 42, 2064). Compounds of Formula I, wherein R 1 is a halide can be converted to compounds wherein R 1 is —NH 2 , —OH, —SH, —OR 8 , —SR 8 with standard reagents, e.g., NH 3 , NaOH, thiourea, R 8 O − , R 8 S − , with or without a catalyst (e.g. Pd, Ni, Cu, Lewis acid, H + ) (e.g., B. G. Ugarkar, J. Med. Chem. 2000, 43, 2883–2893 and 2894–2905). Compounds of Formula I, wherein R 1 is halogen or another leaving group can be treated with ammonia to provide compounds of Formula I wherein R 1 is NH 2 (F. Seela, Liebigs. Ann. Chem. 1985, 315). 3.2. Functional Group Interconversions of R 2 : Compounds of Formula I, wherein R 2 is NH 2 can be temporarily protected, e.g. as an amide (Ac 2 O, PivCl), a carbamate (tBoc) 2 O) or amidine (DMF-DMA). Compounds of Formula I, wherein R 2 is NH 2 can be converted to halides by a Balz-Schiemann (F) or Sandmeyer reaction (Cl, Br, I) by means of a nitrosylating agent (NaNO 2 /H + , NOBF 4 , RONO) and a halogen donor (BF4 − , CuX 2 , SbX 3 ). Compounds of Formula I, wherein R 2 is a halide can be converted to compounds wherein R 2 is NH 2 , OH, SH, OR 8 , SR 8 with standard reagents, e.g. NH 3 , NaOH, thiourea, R 8 O − , R 8 S − , with or without a catalyst (e.g. Pd, Ni, Cu, Lewis acid, H + ). Compounds of Formula I, wherein R 2 is SH can be converted to halides (Br 2 ). They can also be oxidized (e.g, H 2 O 2 ) and treated with ammonia to give a NH 2 group (S. M. Bennett, J. Med. Chem. 1990, 33, 2162). Compounds of Formula I, wherein R 2 is a sulfide, e.g., MeS—, can be converted to a sulfone, e.g. MeSO 2 —, and displaced with a nucleophile, e.g. NH 3 or NH 2 —NH 2 , N 3 —, CN—. 3.3. Functional Group Interconversions of R 3 : Compounds of Formula I, wherein R 3 is H can be halogenated (J. F. Gerster, J. Chem. Soc. 1969, 207) and further functionalized by Pd-catalyzed reactions ((a) Sonogashira coupling: E. C. Taylor et al, Tetrahedron, 1992, 48, 8089; (b) carboxylation: J. W. Pawlik, J. Heterocycl. Chem. 1992, 29, 1357; (c) Suzuki coupling: T. Y. I. Wu, Org. Lett., 2003, 5, 3587) or by addition of nucleophiles (e.g. hydrazine, B. M. Lynch, Can. J. Chem. 1988, 66, 420). Compounds of Formula I wherein R 3 is —CHO can be subjected to a Bayer-Villiger oxidation to provide compounds of Formula I wherein R 3 is —O—CHO. The latter can be hydrolyzed to R 3 is —OH. (A. S. Bourlot, E. Desarbre, J. Y. Mérour Synthesis 1994, 411) Compounds of Formula I, wherein R 3 is H can be treated under Mannich condition (HCHO+HNRR′) to give compounds Formula I wherein R 3 is —CH—NRR′ (F. Seela, Synthesis, 1997, 1067) Compounds of Formula I, wherein R 3 is —CH 2 —NBn 2 can be obtained by Mannich reaction and further treated with an aniline of Formula NH 2 —Ar to give compounds of Formula I wherein R 3 is —CH 2 —NH—Ar (D. C. Miller, J. Med. Chem. 2002, 45, 90). Compounds of Formula I, wherein R 3 is Br can be metallated with BuLi, and treated with an electrophile such as MeI to give a compound of Formula I, wherein R 3 is Me. Compounds of Formula I, wherein R 1 is Cl and R 3 is Br can undergo selective metallation at R 3 (J. S. Pudlo, J. Med. Chem. 1990, 33, 1984). Compounds of Formula I, wherein R 0 is OH and R 3 is H can be be monalkylated or bis-alkylated to give compounds of Formula III, wherein R 1 is an alkyl group. The alkylation can be effected in the presence of a base such as KHMDS, LHMDS, LDA etc. with/without the presence of a catalyst such as NaI, KI, (Bu) 4 NI etc., and in a polar solvent such as THF, DMSO etc. using electrophiles such as L 1 -R 3 where L 1 is a leaving group. Leaving groups include but are not limited to, e.g., halogen, triflate, tosylate or mesylate. Compounds of Formula I, wherein R 0 is H and R 3 is H can be oxidized to compounds of Formula 16/IV, with an oxidizing reagent such as ruthenium tetroxide in a binary solvent such as acetonitrile/water. (G. W. Gribble Org. Prep. Proced. Int. 2001, 33(6), 615). Compounds of Formula I, wherein R 0 is OH and R 3 is H can be oxidized to compounds of Formula II, (wherein R 3 , R 3 is an oxo group) with an oxidizing reagent such as selenium dioxide or oxygen in presence of a cobalt (III) catalyst. (SeO 2 oxidation: Romeo Helv. Chim. Acta. 1955, 38, 463, 465. Oxygen oxidation: A. Inada Heterocycles 1982, 19, 2139). 3.4. Further Elaboration of R 5 : R 5 , especially when it is aryl or heteroaryl, can be further modified as needed, for example by halogenation, nitration, palladium coupling of halogen, Friedel-Crafts alkylation/acylation, etc. or these modifications can also be done before alkylation, see Jerry March, Advanced Organic Chemistry . The heteroaromatic rings can also be oxidized to their corresponding N-oxides using various oxidizing agents such as H 2 O 2 , O 3 , MCPBA etc. in polar solvents such as CH 2 Cl 2 , CHCl 3 , CF 3 COOH etc. See Jerry March, Advanced Organic Chemistry, 4th edition, Chapter 19. Examples of modifications are suggested in Scheme 6. 4. Permutations of the Order of Events As mentioned above, the events (1) assembly of the bicyclic system (2) appendage of the R 5 —R 4 -moiety, and (3) further elaboration of the ring systems do not necessarily have to be made in the sequence (1)-(2)-(3), and it may be beneficial to proceed in a different sequence. Method 4.1. Scheme 8 shows a synthesis in which the order of events is not (1)-(2)-(3), but is (2)-(1)-(3). First R 5 is appended via an aromatic nucleophilic substitution, then the bicyclic system is constructed, and finally it is elaborated. Method 4.1.1 The compound of Formula 18, wherein R 1 is Cl and R 2 is NH 2 , can be prepared by treating the compound of Formula 17 wherein R 2 =NH 2 , and R 1 =X=Cl, with R 5 —R 4 —NH 2 in butanol at reflux in presence of a base such as K 2 CO 3 , Cs 2 CO 3 or iPrNEt 2 . (A. B. Reitz J. Med. Chem. 1994, 37, 3561). Method 4.1.2 The compound of Formula 19, wherein R 1 is Cl and R 2 is NH 2 and L 1 =Br on I, can be prepared by refluxing the compound of Formula 18 in chloroform or dichloroethane in presence of an halogenating reagent such as bromine, N-bromosuccinimide, iodine or N-iodosuccinimide and an acid such as acetic acid or p-toluenesulfonic acid. (A. P. Phillips J. Am. Chem. Soc. 1952, 74, 3922). Method 4.1.3 The compound of Formula 20, wherein R 1 is Cl and R 2 is NH 2 , can be prepared by coupling the compound of Formula 19 with trimethylsilylacetylene under Sonogashira conditions followed by hydroboration using dicylohexylborane and oxidation using hydrogen peroxide in presence of sodium hydroxide. (Sonogashira coupling: E. C. Taylor Tetrahedron, 1992, 48, 8089. Hydroboration/oxidation: G. Zweifel J. Am. Chem. Soc. 1976, 98, 3184). Method 4.1.4 The compound of Formula 21, wherein R 1 is Cl and R 2 is NH 2 , can be prepared by heating the compound of Formula 20 in a polar aprotic solvent such as THF, DME or dioxane in presence of oxalyl chloride, thionyl chloride, mesyl chloride or alkyl chloroformate and a base such as iPrNEt 2 or pyridine. It can also be prepared by treating the compound of Formula 20 with coupling reagents such DCC/HOBt, DCC/DMAP or EDCI/HOBt. (R. C. Larock Comprehensive Organic Transformations , Second Edition, p. 1870). Method 4.2 Again, as mentioned above, the events (1) assembly of the bicyclic system (2) appendage of the R 5 —R 4 -moiety, and (3) further elaboration of the ring systems do not necessarily have to be made in the sequence (1)-(2)-(3), and it may be beneficial to proceed in a different sequence. For illustrative purposes, Scheme 9 shows a putative synthesis in which the order of events is not (1)-(2)-(3), but is (2)-(1)-(3). First R 5 is appended via an aromatic nucleophilic substitution, then the bicyclic system is constructed, and finally it is elaborated. Method 4.3 For illustrative purposes, Scheme 10 shows a putative synthesis in which the order of events is not (1)-(2)-(3), but is (1)-(3)-(2)-(3). First the bicyclic ring is constructed, then it is elaborated, then the R 4 —R 5 moiety is appended, and finally the bicyclic ring system is further elaborated (deprotection). Also, if R 5 is for instance a pyridine, it can be converted to a N-oxide either before or after alkylation. IV. Pharmaceutical Compositions, Dosaging, and Modes of Administration The present invention is directed to the clinical use of the heterocyclics, in particular, the pyrazolopyrimidines and their related analogs of Formulae A, I, II, III and IV, and their polymorphs, solvates, esters, tautomers, diastereomers, enantiomers, pharmaceutically acceptable salts and prodrugs thereof, for use in treatment or prevention of diseases that are HSP90-dependent. Examples of such diseases include disorders such as inflammatory diseases, infections, autoimmune disorders, stroke, ischemia, cardiac disorder, neurological disorders, fibrogenetic disorders, proliferative disorders, tumors, leukemias, neoplasms, cancers, carcinomas, metabolic diseases, and malignant disease. The fibrogenetic disorders include but are not limited to scleroderma, polymyositis, systemic lupus, rheumatoid arthritis, liver cirrhosis, keloid formation, interstitial nephritis and pulmonary fibrosis. The present invention features pharmaceutical compositions comprising the compound of Formulae A, I, II, III and IV, or a polymorph, solvate, ester, tautomer, enantiomer, diastereomer, pharmaceutically acceptable salt thereof, or prodrug thereof, of any of the preceding aspects and embodiments and one or more pharmaceutical excipients. Those of ordinary skill in the art are familiar with formulation and administration techniques that can be employed with the compounds and methods of the invention, e.g., as discussed in Goodman and Gilman, The Pharmacological Basis of Therapeutics , current ed.; Pergamon; and Remington's, Pharmaceutical Sciences (current edition), Mack Publishing Co., Easton, Pa. The compounds utilized in the methods of the instant invention may be administered either alone or in combination with pharmaceutically acceptable carriers, excipients or diluents, in a pharmaceutical composition, according to standard pharmaceutical practice. The compounds can be administered orally or parenterally, including the intravenous, intramuscular, intraperitoneal, subcutaneous, rectal and topical routes of administration. For example, the therapeutic or pharmaceutical compositions of the invention can be administered locally to the area in need of treatment. This may be achieved by, for example, but not limited to, local infusion during surgery, topical application, e.g., cream, ointment, injection, catheter, or implant, said implant made, e.g., out of a porous, non-porous, or gelatinous material, including membranes, such as sialastic membranes, or fibers. The administration can also be by direct injection at the site (or former site) of a tumor or neoplastic or pre-neoplastic tissue. Still further, the compounds or compositions of the invention can be delivered in a vesicle, e.g., a liposome (see, for example, Langer, Science 1990, 249,1527–1533; Treat et al., Liposomes in the Therapy of Infectious Disease and Cancer , Lopez-Bernstein and Fidler, Ed., Liss, N.Y., pp. 353–365, 1989). The compounds and pharmaceutical compositions used in the methods of the present invention can also be delivered in a controlled release system. In one embodiment, a pump may be used (see, Sefton, 1987, CRC Crit. Ref. Biomed. Eng. 14:201; Buchwald et al. Surgery, 1980 88, 507; Saudek et al. N. Engl. J. Med. 1989, 321, (574). Additionally, a controlled release system can be placed in proximity of the therapeutic target. (See, Goodson, Medical Applications of Controlled Release, 1984, Vol. 2, pp. 115–138). The pharmaceutical compositions used in the methods of the instant invention can also contain the active ingredient in a form suitable for oral use, for example, as tablets, troches, lozenges, aqueous or oily suspensions, dispersible powders or granules, emulsions, hard or soft capsules, or syrups or elixirs. Compositions intended for oral use may be prepared according to any method known in the art for the manufacture of pharmaceutical compositions, and such compositions may contain one or more agents selected from the group consisting of sweetening agents, flavoring agents, coloring agents and preserving agents in order to provide pharmaceutically elegant and palatable preparations. Tablets contain the active ingredient in admixture with non-toxic pharmaceutically acceptable excipients which are suitable for the manufacture of tablets. These excipients may be, for example, inert diluents, such as calcium carbonate, sodium carbonate, lactose, calcium phosphate or sodium phosphate; granulating and disintegrating agents, such as microcrystalline cellulose, sodium crosscarmellose, corn starch, or alginic acid; binding agents, for example starch, gelatin, polyvinyl-pyrrolidone or acacia, and lubricating agents, for example, magnesium stearate, stearic acid or talc. The tablets may be un-coated or coated by known techniques to mask the taste of the drug or delay disintegration and absorption in the gastrointestinal tract and thereby provide a sustained action over a longer period. For example, a water soluble taste masking material such as hydroxypropylmethyl-cellulose or hydroxypropylcellulose, or a time delay material such as ethyl cellulose, or cellulose acetate butyrate may be employed as appropriate. Formulations for oral use may also be presented as hard gelatin capsules wherein the active ingredient is mixed with an inert solid diluent, for example, calcium carbonate, calcium phosphate or kaolin, or as soft gelatin capsules wherein the active ingredient is mixed with water soluble carrier such as polyethyleneglycol or an oil medium, for example peanut oil, liquid paraffin, or olive oil. Aqueous suspensions contain the active material in admixture with excipients suitable for the manufacture of aqueous suspensions. Such excipients are suspending agents, for example sodium carboxymethylcellulose, methylcellulose, hydroxypropylmethyl-cellulose, sodium alginate, polyvinyl-pyrrolidone, gum tragacanth and gum acacia; dispersing or wetting agents may be a naturally-occurring phosphatide, for example lecithin, or condensation products of an alkylene oxide with fatty acids, for example polyoxyethylene stearate, or condensation products of ethylene oxide with long chain aliphatic alcohols, for example heptadecaethylene-oxycetanol, or condensation products of ethylene oxide with partial esters derived from fatty acids and a hexitol such as polyoxyethylene sorbitol monooleate, or condensation products of ethylene oxide with partial esters derived from fatty acids and hexitol anhydrides, for example polyethylene sorbitan monooleate. The aqueous suspensions may also contain one or more preservatives, for example ethyl, or n-propyl p-hydroxybenzoate, one or more coloring agents, one or more flavoring agents, and one or more sweetening agents, such as sucrose, saccharin or aspartame. Oily suspensions may be formulated by suspending the active ingredient in a vegetable oil, for example arachis oil, olive oil, sesame oil or coconut oil, or in mineral oil such as liquid paraffin. The oily suspensions may contain a thickening agent, for example beeswax, hard paraffin or cetyl alcohol. Sweetening agents such as those set forth above, and flavoring agents may be added to provide a palatable oral preparation. These compositions may be preserved by the addition of an anti-oxidant such as butylated hydroxyanisol or alpha-tocopherol. Dispersible powders and granules suitable for preparation of an aqueous suspension by the addition of water provide the active ingredient in admixture with a dispersing or wetting agent, suspending agent and one or more preservatives. Suitable dispersing or wetting agents and suspending agents are exemplified by those already mentioned above. Additional excipients, for example sweetening, flavoring and coloring agents, may also be present. These compositions may be preserved by the addition of an anti-oxidant such as ascorbic acid. The compounds and pharmaceutical compositions used in the methods of the instant invention may also be in the form of an oil-in-water emulsion. The oily phase may be a vegetable oil, for example olive oil or arachis oil, or a mineral oil, for example liquid paraffin, or mixtures of these. Suitable emulsifying agents may be naturally-occurring phosphatides, for example soybean lecithin, and esters or partial esters derived from fatty acids and hexitol anhydrides, for example sorbitan monooleate, and condensation products of the said partial esters with ethylene oxide, for example polyoxyethylene sorbitan monooleate. The emulsions may also contain sweetening agents, flavoring agents, preservatives and antioxidants. Syrups and elixirs may be formulated with sweetening agents, for example glycerol, propylene glycol, sorbitol or sucrose. Such formulations may also contain a demulcent, a preservative, flavoring and coloring agents and antioxidant. The pharmaceutical compositions may be in the form of a sterile injectable aqueous solution. Among the acceptable vehicles and solvents that may be employed are water, Ringer's solution and isotonic sodium chloride solution. The sterile injectable preparation may also be a sterile injectable oil-in-water microemulsion where the active ingredient is dissolved in the oily phase. For example, the active ingredient may be first dissolved in a mixture of soybean oil and lecithin. The oil solution may then be introduced into a water and glycerol mixture and processed to form a microemulsion. The injectable solutions or microemulsions may be introduced into a patient's blood-stream by local bolus injection. Alternatively, it may be advantageous to administer the solution or microemulsion in such a way as to maintain a constant circulating concentration of the instant compound. In order to maintain such a constant concentration, a continuous intravenous delivery device may be utilized. An example of such a device is the Deltec CADD-PLUS™ model 5400 intravenous pump. The pharmaceutical compositions may be in the form of a sterile injectable aqueous or oleagenous suspension for intramuscular and subcutaneous administration. This suspension may be formulated according to the known art using those suitable dispersing or wetting agents and suspending agents which have been mentioned above. The sterile injectable preparation may also be a sterile injectable solution or suspension in a non-toxic parenterally-acceptable diluent or solvent, for example as a solution in 1,3-butanediol. In addition, sterile, fixed oils are conventionally employed as a solvent or suspending medium. For this purpose any bland fixed oil may be employed including synthetic mono- or diglycerides. In addition, fatty acids such as oleic acid find use in the preparation of injectables. The compounds of the present invention used in the methods of the present invention may also be administered in the form of suppositories for rectal administration of the drug. These compositions can be prepared by mixing the inhibitors with a suitable nonirritating excipient which is solid at ordinary temperatures but liquid at the rectal temperature and will therefore melt in the rectum to release the drug. Such materials include cocoa butter, glycerinated gelatin, hydrogenated vegetable oils, mixtures of polyethylene glycols of various molecular weights and fatty acid esters of polyethylene glycol. For topical use, creams, ointments, jellies, solutions or suspensions, etc., containing a compound or composition of the invention can be used. As used herein, topical application can include mouth washes and gargles. The compounds used in the methods of the present invention can be administered in intranasal form via topical use of suitable intranasal vehicles and delivery devices, or via transdermal routes, using those forms of transdermal skin patches well known to those of ordinary skill in the art. To be administered in the form of a transdermal delivery system, the dosage administration will, of course, be continuous rather than intermittent throughout the dosage regimen. The methods, compounds and compositions of the instant invention may also be used in conjunction with other well known therapeutic agents that are selected for their particular usefulness against the condition that is being treated. For example, the instant compounds may be useful in combination with known anti-cancer and cytotoxic agents. Further, the instant methods and compounds may also be useful in combination with other inhibitors of parts of the signaling pathway that links cell surface growth factor receptors to nuclear signals initiating cellular proliferation. The methods of the present invention may also be useful with other agents that inhibit angiogenesis and thereby inhibit the growth and invasiveness of tumor cells, including, but not limited to VEGF receptor inhibitors, including ribozymes and antisense targeted to VEGF receptors, angiostatin and endostatin. Examples of antineoplastic agents that can be used in combination with the compounds and methods of the present invention include, in general, and as appropriate, alkylating agents, anti-metabolites, epidophyllotoxins, an antineoplastic enzyme, a topoisomerase inhibitor, procarbazine, mitoxantrone, platinum coordination complexes, biological response modifiers and growth inhibitors, hormonal/anti-hormonal therapeutic agents and haematopoietic growth factors. Exemplary classes of antineoplastic include the anthracyclines, vinca drugs, mitomycins, bleomycins, cytotoxic nucleosides, epothilones, discodermolide, pteridines, diynenes and podophyllotoxins. Particularly useful members of those classes include, for example, carminomycin, daunorubicin, aminopterin, methotrexate, methopterin, dichloromethotrexate, mitomycin C, porfiromycin, 5-fluorouracil, 6-mercaptopurine, gemcitabine, cytosine arabinoside, podophyllotoxin or podo-phyllotoxin derivatives such as etoposide, etoposide phosphate or teniposide, melphalan, vinblastine, vincristine, leurosidine, vindesine, leurosine, paclitaxel and the like. Other useful antineoplastic agents include estramustine, carboplatin, cyclophosphamide, bleomycin, gemcitibine, ifosamide, melphalan, hexamethyl melamine, thiotepa, cytarabin, idatrexate, trimetrexate, dacarbazine, L-asparaginase, camptothecin, CPT-11, topotecan, ara-C, bicalutamide, flutamide, leuprolide, pyridobenzoindole derivatives, interferons and interleukins. When a compound or composition of the invention is administered into a human subject, the daily dosage will normally be determined by the prescribing physician with the dosage generally varying according to the age, weight, and response of the individual patient, as well as the severity of the patient's symptoms. In one exemplary application, a suitable amount of compound is administered to a mammal undergoing treatment for cancer, for example, breast cancer. Administration typically occurs in an amount of between about 0.01 mg/kg of body weight to about 100 mg/kg of body weight per day (administered in single or divided doses), more preferably at least about 0.1 mg/kg of body weight per day. A particular therapeutic dosage can include, e.g., from about 0.01 mg to about 1000 mg of compound, and preferably includes, e.g., from about 1 mg to about 1000 mg. The quantity of active compound in a unit dose of preparation may be varied or adjusted from about 0.1 mg to 1000 mg, preferably from about 1 mg to 300 mg, more preferably 10 mg to 200 mg, according to the particular application. The amount administered will vary depending on the particular IC 50 value of the compound used and the judgment of the attending clinician taking into consideration factors such as health, weight, and age. In combinational applications in which the compound is not the sole active ingredient, it may be possible to administer lesser amounts of compound and still have therapeutic or prophylactic effect. Preferably, the pharmaceutical preparation is in unit dosage form. In such form, the preparation is subdivided into unit doses containing appropriate quantities of the active component, e.g., an effective amount to achieve the desired purpose. The actual dosage employed may be varied depending upon the requirements of the patient and the severity of the condition being treated. Determination of the proper dosage for a particular situation is within the skill of the art. Generally, treatment is initiated with smaller dosages which are less than the optimum dose of the compound. Thereafter, the dosage is increased by small amounts until the optimum effect under the circumstances is reached. For convenience, the total daily dosage may be divided and administered in portions during the day if desired. The amount and frequency of administration of the compounds and compositions of the present invention used in the methods of the present invention, and if applicable other chemotherapeutic agents and/or radiation therapy, will be regulated according to the judgment of the attending clinician (physician) considering such factors as age, condition and size of the patient as well as severity of the disease being treated. The chemotherapeutic agent and/or radiation therapy can be administered according to therapeutic protocols well known in the art. It will be apparent to those skilled in the art that the administration of the chemotherapeutic agent and/or radiation therapy can be varied depending on the disease being treated and the known effects of the chemotherapeutic agent and/or radiation therapy on that disease. Also, in accordance with the knowledge of the skilled clinician, the therapeutic protocols (e.g., dosage amounts and times of administration) can be varied in view of the observed effects of the administered therapeutic agents (i.e., antineoplastic agent or radiation) on the patient, and in view of the observed responses of the disease to the administered therapeutic agents. Also, in general, the compounds of the invention need not be administered in the same pharmaceutical composition as a chemotherapeutic agent, and may, because of different physical and chemical characteristics, be administered by a different route. For example, the compounds/compositions may be administered orally to generate and maintain good blood levels thereof, while the chemotherapeutic agent may be administered intravenously. The determination of the mode of administration and the advisability of administration, where possible, in the same pharmaceutical composition, is well within the knowledge of the skilled clinician. The initial administration can be made according to established protocols known in the art, and then, based upon the observed effects, the dosage, modes of administration and times of administration can be modified by the skilled clinician. The particular choice of compound (and where appropriate, chemotherapeutic agent and/or radiation) will depend upon the diagnosis of the attending physicians and their judgment of the condition of the patient and the appropriate treatment protocol. The compounds/compositions of the invention (and where appropriate chemotherapeutic agent and/or radiation) may be administered concurrently (e.g., simultaneously, essentially simultaneously or within the same treatment protocol) or sequentially, depending upon the nature of the proliferative disease, the condition of the patient, and the actual choice of chemotherapeutic agent and/or radiation to be administered in conjunction (i.e., within a single treatment protocol) with the compound/composition. In combinational applications and uses, the compound/composition and the chemotherapeutic agent and/or radiation need not be administered simultaneously or essentially simultaneously, and the initial order of administration of the compound/composition, and the chemotherapeutic agent and/or radiation, may not be important. Thus, the compounds/compositions of the invention may be administered first followed by the administration of the chemotherapeutic agent and/or radiation; or the chemotherapeutic agent and/or radiation may be administered first followed by the administration of the compounds/compositions of the invention. This alternate administration may be repeated during a single treatment protocol. The determination of the order of administration, and the number of repetitions of administration of each therapeutic agent during a treatment protocol, is well within the knowledge of the skilled physician after evaluation of the disease being treated and the condition of the patient. For example, the chemotherapeutic agent and/or radiation may be administered first, especially if it is a cytotoxic agent, and then the treatment continued with the administration of the compounds/compositions of the invention followed, where determined advantageous, by the administration of the chemotherapeutic agent and/or radiation, and so on until the treatment protocol is complete. Thus, in accordance with experience and knowledge, the practicing physician can modify each protocol for the administration of a compound/composition for treatment according to the individual patient's needs, as the treatment proceeds. The attending clinician, in judging whether treatment is effective at the dosage administered, will consider the general well-being of the patient as well as more definite signs such as relief of disease-related symptoms, inhibition of tumor growth, actual shrinkage of the tumor, or inhibition of metastasis. Size of the tumor can be measured by standard methods such as radiological studies, e.g., CAT or MRI scan, and successive measurements can be used to judge whether or not growth of the tumor has been retarded or even reversed. Relief of disease-related symptoms such as pain, and improvement in overall condition can also be used to help judge effectiveness of treatment. V. Assays for Determining HSP90 Binding and Downstream Effect A variety of in vitro and in vivo assays are available to test the effect of the compounds of the invention on HSP90. HSP90 competitive binding assays and functional assays can be performed as known in the art by substituting in the compounds of the invention. Chiosis et al. Chemistry & Biology 2001, 8, 289–299, describe some of the known ways in which this can be done. For example, competition binding assays using, e.g., geldanamycin or 17-AAG as a competitive binding inhibitor of HSP90 can be used to determine relative HSP90 affinity of the compounds of the invention by immobilizing the compound of interest or other competitive inhibitor on a gel or solid matrix, preincubating HSP90 with the other inhibitor, passing the preincubated mix over the gel or matrix, and then measuring the amount of HSP90 that retains or does not retain on the gel or matrix. Downstream effects can also be evaluated based on the known effect of HSP90 inhibition on function and stability of various steroid receptors and signaling proteins including, e.g., Raf1 and HER2. Compounds of the present invention induce dose-dependent degradation of these molecules, which can be measured using standard techniques. Inhibition of HSP90 also results in up-regulation of HSP90 and related chaperone proteins that can similarly be measured. Antiproliferative activity on various cancer cell lines can also be measured, as can morphological and functional differentiation related to HSP90 inhibition. Many different types of methods are known in the art for determining protein concentrations and measuring or predicting the level of proteins within cells and in fluid samples. Indirect techniques include nucleic acid hybridization and amplification using, e.g., polymerase chain reaction (PCR). These techniques are known to the person of skill and are discussed, e.g., in Sambrook, Fritsch & Maniatis Molecular Cloning: A Laboratory Manual, 2nd ed., Cold Spring Harbor Laboratory, Cold Spring Harbor, N.Y., 1989; Ausubel, et al. Current Protocols in Molecular Biology , John Wiley & Sons, NY, 1994, and, as specifically applied to the quantification, detection, and relative activity of HER2/Neu in patient samples, e.g., in U.S. Pat. Nos. 4,699,877, 4,918,162, 4,968,603, and 5,846,749. A brief discussion of two generic techniques that can be used follows. The determination of whether cells overexpress or contain elevated levels of HER2 can be determined using well known antibody techniques such as immunoblotting, radioimmunoassays, western blotting, immunoprecipitation, enzyme-linked immunosorbant assays (ELISA), and derivative techniques that make use of antibodies directed against HER2. As an example, HER2 expression in breast cancer cells can be determined with the use of an immunohistochemical assay, such as the Dako Hercep™ test (Dako Corp., Carpinteria, Calif.). The Hercep™ test is an antibody staining assay designed to detect HER2 overexpression in tumor tissue specimens. This particular assay grades HER2 expression into four levels: 0, 1, 2, and 3, with level 3 representing the highest level of HER2 expression. Accurate quantitation can be enhanced by employing an Automated Cellular Imaging System (ACIS) as described, e.g., by Press, M. et al. Modern Pathology 2000, 13, 225A. Antibodies, polyclonal or monoclonal, can be purchased from a variety of commercial suppliers, or may be manufactured using well-known methods, e.g., as described in Harlow et al. Antibodies: A Laboratory Manual, 2nd ed; Cold Spring Harbor Laboratory, Cold Spring Harbor, N.Y., 1988. HER2 overexpression can also be determined at the nucleic acid level since there is a reported high correlation between overexpression of the HER2 protein and amplification of the gene that codes for it. One way to test this is by using RT-PCR. The genomic and cDNA sequences for HER2 are known. Specific DNA primers can be generated using standard, well-known techniques, and can then be used to amplify template already present in the cell. An example of this is described in Kurokawa, H. et al. Cancer Res. 2000, 60, 5887–5894. PCR can be standardized such that quantitative differences are observed as between normal and abnormal cells, e.g, cancerous and noncancerous cells. Well known methods employing, e.g., densitometry, can be used to quantitate and/or compare nucleic acid levels amplified using PCR. Similarly, fluorescent in situ hybridization (FISH) assays and other assays can be used, e.g., Northern and/or Southern blotting. These rely on nucleic acid hybridization between the HER2 gene or mRNA and a corresponding nucleic acid probe that can be designed in the same or a similar way as for PCR primers, above. See, e.g., Mitchell M S, and Press M. F. Oncol., Suppl. 1999, 12, 108–116. For FISH, this nucleic acid probe can be conjugated to a fluorescent molecule, e.g., fluorescein and/or rhodamine, that preferably does not interfere with hybridization, and which fluorescence can later be measured following hybridization. See, e.g., Kurokawa, H et al, Cancer Res. 2000, 60, 5887–5894 (describing a specific nucleic acid probe having sequence 5′-FAM-NucleicAcid-TAMRA-p-3′ sequence). ACIS-based approaches as described above can be employed to make the assay more quantitative (de la Torre-Bueno, J., et al. Modern Pathology 2000, 13, 221A). Immuno and nucleic acid detection can also be directed against proteins other than HSP90 and HER2, which proteins are nevertheless affected in response to HSP90 inhibition. The following examples are offered by way of illustration only and are not intended to be limiting of the full scope and spirit of the invention. EXAMPLES I. Materials and Methods The chemical reagents used to create the novel products of the invention below are all available commercially, e.g., from Aldrich Chemical Co., Milwaukee, Wis., USA. Otherwise their preparation is facile and known to one of ordinary skill in the art, or it is referenced or described herein. The final compounds were usually purified by preparative TLC (silica gel 60 Å, Whatman Partisil PK6F) or flash chromatography (silica gel 60 Å, EMD Chemicals) using EtOAc/hexane or MeOH/CH 2 Cl 2 as eluents. Rf's were measured using silica gel TLC plates (silica gel 60 Å, EMD Chemicals). Analytical HPLC chromatograms were obtained using a C18 column (Agilent Zorbax 300SB-C18; 5 microns; 4.6 mm×150 mm). A gradient was applied between solvent A (0.1% TFA in H 2 O) and solvent B (0.5% TFA in CH 3 CN) increasing the proportion of A linearly from 5% (t=0) to 100% (t=7.00 min), with a constant flow rate of 1 mL/min. The samples were diluted to typically 0.1–1 mg/mL in MeOH or CH 3 CN and the injection volumes were typically 10 μL. The column was not heated, and UV detection was effected at 254 mn. 1 H-NMR spectra were recorded on a Bruker Avance 400 MHz spectrometer. The chemical names were generated using the Beilstein Autonom 2.1 software. II. General Procedures 1. General procedures to prepare and manipulate the pyrrolo[2,3-d]pyrimidine ring General procedure 1.1: Preparation of pyrrolo[2,3-d]pyrimidines (R 0 ≠OH) A suspension of 4-diamino-6-hydroxypyrimidine (6 mmol), AcONa (12 mmol) and α-haloaldehyde (6 mmol ) in CH 3 CN (20 mL) and H 2 O (20 mL) was stirred at 22–40° C. overnight whereupon the starting materials gradually dissolved and the desired pyrrolo[2,3-d]pyrimidine precipitated. The precipitate was collected by filtration and washed (water, acetontrile, ether) and air-dried ((a) C. J. Barnett, Org. Proc. Res. Develop. 1999, 3, 184. (b) F. Seela, Liebigs Ann. Chem. 1987, 15). General Procedure 1.2: Preparation of pyrrolo[2,3-d]pyrimidines (R 0 =OH) A suspension of (2-amino-4,6-dichloro-pyrimidin-5-yl)-acetic acid ethyl ester, R 5 —R 4 —NH 2 and EtN(i-Pr) 2 in BuOH was heated at reflux for 24 h whereupon the solvent was removed under reduced pressure. The residue was then dissolved in CH 2 Cl 2 and washed with sat. NaHCO 3 solution and dried with Na 2 SO 4 . The crude material was purified by preparative TLC or flash chromatography (EtOAc/hexane or MeOH/CH 2 Cl 2 ) to give the pure pyrrolo[3,4-d]pyrimidin-6-one. General Procedure 1.3: Alkylation of pyrrolo[2,3-d]pyrimidines at N-7 A suspension of the 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine (1 mmol), benzyl halide (1 mmol) and K 2 CO 3 or Cs 2 CO 3 (1–5 mmol) in dry DMF (5 mL) was heated to 40° C. for 3 to 10 h. Work-up (EtOAc) and purification by preparative TLC or flash chromatography (EtOAc/hexane or MeOH/CH 2 Cl 2 ) yielded the pure N-7 alkylated product. General Procedure 1.4: Aminomethylation of pyrrolo[2,3-d]pyrimidines at C-5 A solution of 2-amino-7H-pyrrolo[2,3-d]pyrimidin-4-ol, formaldehyde (2–5 equiv.) and HNR 9 R 9 (2–5 equiv.) in 80% aq. acetic acid was heated in a sealed tube at 60° C. overnight, concentrated, extracted in MeOH:CH 2 Cl 2 (1:10), washed with sat. NaHCO 3 and concentrated. See H. Akimoto, J. Chem. Soc. Perkin Trans 1. 1998, 1637. General Procedure 1.5: Alkylation of pyrrolo[2,3-d]pyrimidin-6-one at C-5 To a solution of pyrrolo[2,3-d]pyrimidin-6-one in THF at −78° C. was added a base such as LDA, LHMDS or KHMDS and after 30 min, the alkyl halide was further added to give monoalkylated and bisalkylated pyrrolo[2,3-d]pyrimidin-6-ones which were purified by preparative TLC or flash chromatography (EtOAc/hexane or MeOH/CH 2 Cl 2 ). General Procedure 1.6: Oxidation of pyrrolo[2,3-d]pyrimidines at C-5 A solution of 2-amino-4-chloro-pyrrolo[3,4-d]pyrimidin-6-one and SeO 2 in dioxane was heated at reflux until completion of the reaction, (1 h) whereupon the solvent was removed under reduced pressure. The crude was purified by preparative TLC or flash chromatography (EtOAc/hexane or MeOH/CH 2 Cl 2 ) to give the pure 4-chloro-5-hydroxy-2-imino-2,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one. 2. General Procedures to Manipulate the Pyridine Ring General Procedure 2.1: Preparation of Pyridine N-Oxides A solution of the pyridine derivative (1 mmol) in dichloromethane or chloroform (5 mL) was cooled by means of an ice-bath, treated with m-CPBA (1.1 to 3 mmol) in three portions, and allowed to warm to r.t. The mixture was extracted with dichloromethane and washed with aqueous NaOH, followed by water. Drying (Na 2 SO 4 ) and concentration afforded the pyridine N-oxide. General Procedure 2.2: Preparation of 2-(acetoxymethyl)-pyridines A solution of the 2-methylpyridine N-oxide (1.0 mmol) in acetic anhydride (5 mL) was heated to reflux for 0.5 h. Work-up (EtOAc), drying (MgSO 4 ), evaporation and purification by preparative TLC or flash chromatography afforded the 2-(acetoxymethyl) pyridine. General Procedure 2.3: Preparation of 2-(hydroxymethyl)-pyridines A suspension of 2-acetoxymethyl-pyridine derivative and solid K 2 CO 3 in methanol was heated to 50° C. for 5–30 min. Evaporation, work-up (EtOAc), and drying (MgSO 4 ) afforded the 2-(hydroxymethyl)-pyridine. General Procedure 2.4: Preparation of 2-(bromomethyl)-pyridines A solution of 2-(hydroxymethyl)-pyridine (1.0 mmol) and triphenyl phosphine (1.2 mmol) in dichloromethane or chloroform (5 mL) was cooled to 0° C. A solution of CBr 4 (1.5 mmol) in dichloromethane or chloroform was added dropwise, and the resulting mixture was stirred at 0° C. for 0.5–1 h. Work-up and purification by flash chromatography afforded the 2-(bromomethyl)-pyridine. General Procedure 2.5: Preparation of 2-(aminomethyl)-pyridines The 2-(chloromethyl)-pyridine derivative in a solution of ammonia in MeOH was heated at 100° C. overnight whereupon it was concentrated under reduced pressure and purified by flash chromatography (MeOH/CH 2 Cl 2 ) to afford the 2-(aminomethyl)-pyridine derivative. General Procedure 2.6: Preparation of 2-chloropyridines A suspension of 2-(hydroxymethyl)-pyridine (10 g) in POCl 3 (30 mL) was stirred at 110° C. for 1.5 h. The resulting viscous oil was cooled to r.t. and poured onto ice water (500 g). The pH was adjusted to 10 with solid KOH. Work-up (CHCl 3 ), drying (MgSO 4 ) and evaporation gave the 2-chloropyridine, which was used without purification. General Procedure 2.7: Preparation of Pyridinium Salts. A solution of the pyridine was heated in MeOH until it dissolved. A methanolic solution of acid (1.0 equiv of e.g. HCl, MsOH) was added, and the solvent was evaporated to give the pyridinium salt. 3. General Procedure to Manipulate Benzene Rings General Procedure 3.1: Halogenation of Benzene Rings. Variant 1: A solution of the aromatic compound in MeOH/THF/acetate buffer (1N in each AcOH and AcONa) was treated with Br 2 (1.3-equiv) at r.t. for 5 min. The excess bromine and solvent were removed on a rotary evaporator. Work-up (CHCl 3 ) and flash chromatography afforded the desired bromobenzene. Variant 2: A solution of the aromatic compound (7 mmol) and N-halosuccinimide (NCS, NBS, or NIS, 1.06 equiv) in acetic acid (40 mL) was heated to 40–90° C. for 0.3–1 h. Evaporation, work-up (EtOAc) and flash chromatography afforded the desired halogenated benzene. Preparation of Intermediates Example 1 2-Chloro-1-chloromethyl-3,4,5-trimethoxy-benzene The title compound was obtained by chlorination of 5-chloromethyl-1,2,3-trimethoxy-benzene with NCS according to the general procedure 3.1. 1 H-NMR (CDCl 3 ): δ 6.82 (s, 1H), 4.70 (s, 1H), 3.93 (s, 3H), 3.90 (s, 3H) 3.87 (s, 3H). Example 2 2-Chloro-6-chloromethyl-4-methoxy-3,5-dimethyl-pyridine Step 1: 2-Chloromethyl-4-methoxy-3,5-dimethylpyridine-1-oxide The title compound was obtained by oxidation of 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine according to the general procedure 2.1. HPLC Rt: 4.46 min. 1 H-NMR (CDCl 3 ): δ 8.05 (s, 1H), 4.93 (s, 2H), 3.77 (s, 3H), 2.37 (s, 3H), 2.24 (s, 3H). Step 2: 2-Chloro-6-chloromethyl-4-methoxy-3,5-dimethylpyridine The title compound was obtained by treating 2-chloromethyl-4-methoxy-3,5-dimethylpyridine-1-oxide with POCl 3 according to the general procedure 2.6. HPLC Rt: 6.757 min. 1 H-NMR (CDCl 3 ): δ 4.64 (s, 2H), 3.79 (s, 3H), 2.35 (s, 3H), 2.33 (s, 3H). Example 3 4-Chloro-2-chloromethyl-3,5-dimethyl-pyridine The title compound was obtained by treating 2-chloromethyl-3,5-dimethyl-pyridin-4-ol (Tarbit, et al. WO 99/10326) with POCl 3 in the same manner as in the general procedure 2.6 (74% yield). HPLC Rt: 5.54 min. 1 H-NMR (CDCl 3 ): 8.24 (s, 1H), 4.71 (s, 2H), 2.48 (s, 3H), 2.36 (s, 3H). Example 4 4-Bromo-2-bromomethyl-3,5-dimethyl-pyridine 4-Bromo-2-bromomethyl-3,5-dimethyl-pyridine was prepared by any of the following three methods: Step 1: 2,3,5-Collidine-N-oxide 2,3,5-Collidine-N-oxide was obtained by oxidation of 2,3,5-collidine according to the general procedure 2.1 in 70% yield. HPLC Rt: 3.96 min. 1 H-NMR (CDCl 3 ): δ 8.03 (s, 1H), 6.90 (s, 1H), 2.47 (s, 3H), 2.31 (s, 3H), 2.24 (s, 3H). m/z (%) 138.2 (M+1, 100%). Rf (20% MeOH/EtOAc): 0.35. Step 2: 4-Bromo-2,3,5-collidine-N-oxide 2,3,5-collidine-N-oxide (1.3 g, 10 mmol) and K 2 CO 3 (2.9 g, 20 mmol) were suspended in 10 mL of CCl 4 . Bromine (1 mL, 20 mmol) was added dropwise, and the reaction mixture was heated to reflux for 2 h. Work-up (EtOAc) and flash chromatography (10% MeOH/EtOAc) afforded the title compound as a solid (1.05 g, 51% yield). HPLC Rt: 5.24 min. 1 H-NMR (CDCl 3 ): δ 8.06 (s, 1 H), 2.56 (s, 3H), 2.43 (s, 3H), 2.31 (s, 3H). m/z (%) 216.2 (M+1, 100%), 218.2 (M+3, 100%). Rf (20% MeOH/EtOAc): 0.45. Step 3: Acetic acid 4-bromo-3,5-dimethyl-pyridin-2-yl methyl ester 4-Bromo-2,3,5-collidine-N-oxide (0.25 g, 11 mmol) was dissolved in acetic anhydride (5 mL) and the solution was heated to reflux for 30 min. Work-up and flash chromatography (50% Hexane/EtOAc) afforded the title compound (0.27 g, 96% yield). Rf (50% Hexane/EtOAc): 0.70. HPLC Rt: 4.76 min. 1 H-NMR (CDCl 3 ): δ 8.26 (s, 1H), 5.27 (s, 2H), 2.46 (s, 3H), 2.41 (s, 3H), 2.14 (s, 3H). Step 4: 4-Bromo-3,5-dimethyl-pyridin-2-yl methanol A suspension of acetic acid 4-bromo-3,5-dimethyl-pyridin-2-yl methyl ester (0.26 g, 1.0 mmol) and K 2 CO 3 (excess) in MeOH (5 mL) was heated to 50° C. for 15 min. Work-up (CHCl 3 ), evaporation, and filtration through a silica gel pad (eluent: 100% EtOAc) gave the title compound as a white solid (0.19 g, 88% yield). Rf (50% Hexane/EtOAc): 0.5. HPLC Rt: 3.80 min. 1 H-NMR (CDCl 3 ): δ 8.23 (s, 1H), 4.70 (s, 2H), 2.46 (s, 3H), 2.30 (s, 3H). Step 5: 4-Bromo-2-bromomethyl-3,5-dimethyl-pyridine The title compound was obtained from 4-bromo-3,5-dimethyl-pyridin-2-yl methanol according to the general procedure 2.4. HPLC Rt: 6.32 min. 1 H-NMR (CDCl 3 ): δ 8.22 (s, 1H), 4.63 (s, 2H), 2.52 (s, 3H), 2.40 (s, 3H). Step 1: 2-chloromethyl-3,5-dimethyl-pyridin-4-ol The title compound was obtained by heating 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine hydrochloride in toluene as described in the patent by Tarbit, et al. WO 99/10326. Step 2: 4-bromo-2-chloromethyl-3,5-dimethyl pyridine A mixture of 2-chloromethyl-3,5-dimethyl-pyridin-4-ol (8.2 g, 47.8 mmol) and POBr 3 (60 g, 209 mmol) was stirred at 130° C. for 3 h. The resulting viscous oil was cooled to r.t. and poured onto ice water. The pH was adjusted to 10 with solid KOH. Work-up (CHCl 3 ), drying (MgSO 4 ) and evaporation afforded the title compound as a purple solid (8.7 g, 78% yield) which was used without purification. HPLC Rt: 6.03 min. 1 H-NMR (CDCl 3 ): 8.20 (s, 1H), 4.62 (s, 2H), 2.50 (s, 3H), 2.38 (s, 3H). Step 1: 4-bromo-2-chloromethyl-3,5-dimethyl pyridine A suspension of 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine (3.24 g, 14.6 mmol) in PBr 3 (8.0 mL, 85.1 mmol, 5.8 equiv.) was heated to 80° C. under nitrogen. A catalytic amount of DMF (0.50 mL, 6.4 mmol, 0.44 equiv.) was added, whereupon the suspension rapidly turned into an orange solution. After 40 min., the reaction was still incomplete as judged by HPLC. The temperature was raised to 110° C. and the reaction was prolonged for 30 min, at which point it was complete. The mixture was poured over ice, made basic with conc. aq. NH 4 OH and extracted into EtOAc. Washing with water, drying (brine, MgSO 4 ) and concentration gave the title compound as a pink solid (1.51 g, 44%) containing 10% of an impurity by 1 H-NMR. The crude was used without further purification. 1 H-NMR (CDCl 3 ): δ 8.19 (s, 1H), 4.59 (s, 2H), 2.48 (s, 3H), 2.37 (s, 3H). Preparation of Final Compounds Example 5 4-Chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine (F. Seela, Liebigs Ann. Chem. 1987, 15) with 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine hydrochloride according to the general procedure 1.3. HPLC Rt: 4.709 min. 1 H-NMR (CDCl 3 ): δ 8.23 (s, 1H), 6.90 (m, 1H), 6.38 (m 1H), 5.35 (s, 2H), 4.99 (s, 2H), 3.75 (s, 3H), 2.26 (s, 3H), 2.21 (s, 3H). Example 6 7-(2-Bromo-3,4,5-trimethoxy-benzyl)-4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 2-bromo-1-chloromethyl-3,4,5-trimethoxy-benzene according to the general procedure 1.3. HPLC Rt: 6.937 min. 1 H-NMR (DMSO-d6): δ 7.11 (m 1H), 6.73(s, 2H), 6.42 (s, 1H), 6.37 (m 1H), 5.23 (s, 2H), 3.79 (s, 3H), 3.75 (s, 3H), 3.61 (s, 3H). Example 7 4-Chloro-7-(2-iodo-3,4,5-trimethoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 1-chloromethyl-2-iodo-3,4,5-trimethoxy-benzene according to the general procedure 1.3. HPLC Rt: 7.069 min. 1 H-NMR (DMSO-d6): δ 7.08 (m, 1H), 6.74 (s, 2H), 6.38 (m, 1H), 6.36 (s, 1H), 5.19 (s, 2H), 3.80 (s, 3H), 3.77 (s, 3H), 3.60 (s, 3H). Example 8 4-Chloro-7-(4-methoxy-3,5-dimethyl-1-oxy-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine 1-oxide according to the general procedure 1.3. HPLC Rt: 5.079 min. 1 H-NMR (DMSO-d6): δ 8.18 (s, 1H), 7.29 (m, 1H), 6.68(s, 2H), 6.24 (m, 1H), 5.38 (s, 2H), 3.70 (s, 3H), 2.42 (s, 3H), 2.17 (s, 3H). ESI-MS 334.2 (M+1). Example 9 4-Chloro-7-(3,4,5-trimethoxy-benzyl)-7H-pyrrolo [2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 5-chloromethyl-1,2,3-trimethoxy-benzene according to the general procedure 1.3. HPLC Rt: 6.036 min. 1 H-NMR (CDCl 3 ): δ 6.82 (m, 1H), 6.41 (s, 2H), 6.40 (m, 1H), 5.36 (s, 2H), 5.16 (s, 2H), 3.81 (s, 3H), 3.78 (s, 6H). Example 10 4-Chloro-7-(6-chloro-4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo [2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 2-chloro-6-chloromethyl-4-methoxy-3,5-dimethyl-pyridine according to the general procedure 1.3. HPLC Rt: 6.880 min. 1 H-NMR (DMSO-d6): δ 7.06 (m, 1H), 6.63(s, 2H), 6.32 (m, 1H), 5.29 (s, 2H), 3.74 (s, 3H), 2.25 (s, 3H), 2.21 (s, 3H). Example 11 4-Chloro-7-(4-chloro-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 4-chloro-2-chloromethyl-3,5-dimethyl-pyridine according to the general procedure 1.3. HPLC Rt: 5.878 min. 1 H-NMR (CDCl 3 ): δ 8.27 (s, 1H), 6.89 (m, 1H), 6.40 (m, 1H), 5.40(s, 2H), 4.94 (s, 2H), 2.39 (s, 3H), 2.37 (s, 3H). Example 12 4-Chloro-7-(2-chloro-4,5-dimethoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 1-bromomethyl-2-chloro-4,5-dimethoxy-benzene according to the general procedure 1.3. HPLC Rt: 6.635 min. 1 H-NMR (CDCl 3 ): δ 6.91 (m, 1H), 6.90 (s, 1H), 6.71 (s, 1H), 6.42 (m, 1H), 5.30 (s, 2H), 4.97 (s, 2H), 3.88 (s, 3H), 3.75 (s, 3H). Example 13 7-(4-Bromo-3,5-dimethyl-pyridin-2-ylmethyl)-4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 4-bromo-2-chloromethyl-3,5-dimethyl-pyridine according to the general procedure 1.3. HPLC Rt: 6.072 min. 1 H-NMR (DMSO-d6): δ 8.15 (s, 1H), 7.10 (m, 1H), 6.60(s, 1H), 6.30 (m, 1H), 5.40 (s, 2H), 2.46 (s, 3H), 2.30 (s, 3H). Example 14 4-Chloro-7-(4-chloro-3,5-dimethyl-1-oxy-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 4-chloro-2-chloromethyl-3,5-dimethyl-pyridine 1-oxide according to the general procedure 1.3. HPLC Rt: 5.610 min. 1 H-NMR (DMSO-d6): δ 8.36 (s, 1H), 7.26 (m, 1H), 6.69(s, 1H), 6.21 (m, 1H), 5.43(s, 2H), 2.60 (s, 3H), 2.27 (s, 3H). Example 15 7-(4-Bromo-3,5-dimethyl-1-oxy-pyridin-2-ylmethyl)-4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 4-bromo-2-chloromethyl-3,5-dimethyl-pyridine 1-oxide according to the general procedure 1.3. HPLC Rt: 5.734 min. 1 H-NMR (DMSO-d6): δ 8.33 (s, 1H), 7.24 (m, 1H), 6.69 (s, 1H), 6.25 (m, 1H), 5.47(s, 2H), 2.65 (s, 3H), 2.29 (s, 3H). Example 16 4-Chloro-7-(3,5-dimethoxy-2-nitro-benzyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2ylamine with 1-bromomethyl-4,5-dimethoxy-2-nitro-benzene according to the general procedure 1.3. HPLC Rt: 6.345 min. 1 H-NMR (DMSO-d6): δ 7.73 (s, 1H), 7.16 (m, 1H), 6.72 (s, 2H), 6.41 (s, 1H), 6.40 (m, 1H), 5.58(s, 2H), 3.92 (s, 3H), 3.62 (s, 3H). Example 17 4-Chloro-7-(3,4-dichloro-benzyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 4-bromomethyl-1,2-dichloro-benzene according to the general procedure 1.3. HPLC Rt: 7.148 min. 1 H-NMR (DMSO-d6): δ 7.60 (m, 1H), 7.59 (m, 1H), 7.25(q, 1H), 7.12(m, 1H), 6.71 (s, 2H), 6.37 (q, 1H), 5.26(s, 2H). Example 18 4-Chloro-7-(3,5-dimethoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 1-chloromethyl-3,5-dimethoxy-benzene according to the general procedure 1.3. HPLC Rt: 6.423 min. 1 H-NMR (DMSO-d6): δ 7.21(m, 1H), 6.69 (s, 2H), 6.40 (m, 3H), 6.34 (m, 1H), 5.34 (s, 2H), 3.68 (s, 6H). Example 19 4-Chloro-7-(2,5-dimethoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 2-chloromethyl-1,4-dimethoxy-benzene according to the general procedure 1.3. HPLC Rt: 6.537 min. 1 H-NMR (DMSO-d6): δ 7.13 (m, 1H), 6.85 (d, 1H), 6.82 (m, 1H), 6.68 (s, 2H), 6.35 (m, 1H), 6.22 (d, 1H), 3.78 (s, 3H), 3.60 (s, 3H). Example 20 4-Bromo-7-(4-methoxy-3,5-dimethyl-1-oxy-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-bromo-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine (obtained as described in F. Seela, Liebigs Ann. Chem. 1987, 15 for 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine, but replacing POCl 3 with POBr 3 ) with 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine-1-oxide according to the general procedure 1.3. HPLC Rt: 5.158 min. 1 H-NMR (DMSO-d6): δ 8.18 (s, 1H), 7.29 (m, 1H), 6.69 (s, 2H), 6.15 (m, 1H), 5.37(s, 2H), 3.70 (s, 3H), 2.42 (s, 3H), 2.17 (s, 3H). Example 21 4-Bromo-7-(4-chloro-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-bromo-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 4-chloro-2-chloromethyl-3,5-dimethyl-pyridine according to the general procedure 1.3. HPLC Rt: 5.803 min. 1 H-NMR (DMSO-d6): δ 8.20 (s, 1H), 7.04 (m, 1H), 6.61 (s, 2H), 6.21 (m, 1H), 5.38(s, 2H), 2.42 (s, 3H), 2.28 (s, 3H). Example 22 4-Bromo-7-(4-chloro-3,5-dimethyl-1-oxy-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-bromo-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 4-chloro-2-chloromethyl-3,5-dimethyl-pyridine-1-oxide according to the general procedure 1.3. HPLC Rt: 5.688 min. 1 H-NMR (DMSO-d6): δ 8.35 (s, 1H), 7.25 (m, 1H), 6.70 (s, 2H), 6.15 (m, 1H), 5.43 (s, 2H), 2.60 (s, 3H), 2.27 (s, 3H). Example 23 4-Bromo-7-(4-bromo-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-bromo-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 4-bromo-2-chloromethyl-3,5-dimethyl-pyridine according to the general procedure 1.3. HPLC Rt: 5.996 min. 1 H-NMR (DMSO-d6): δ 8.15 (s, 1H), 7.05 (m, 1H), 6.61 (s, 2H), 6.21 (m, 1H), 5.43 (s, 2H), 2.46 (s, 3H), 2.30 (s, 3H). Example 24 4-Bromo-7-(4-bromo-3,5-dimethyl-1-oxy-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-bromo-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 4-bromo-2-chloromethyl-3,5-dimethyl-pyridine-1-oxide according to the general procedure 1.3. HPLC Rt: 5.798 min. 1 H-NMR (DMSO-d6): δ 8.33 (s, 1H), 7.24 (m, 1H), 6.71 (s, 2H), 6.15 (m, 1H), 5.46 (s, 2H), 2.64 (s, 3H), 2.29 (s, 3H). Example 25 4-Bromo-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-bromo-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine according to the general procedure 1.3. HPLC Rt: 4.847 min. 1 H-NMR (DMSO-d6): δ 8.07 (s, 1H), 7.03 (m, 1H), 6.60 (s, 2H), 6.20 (m, 1H), 5.29 (s, 2H), 3.72 (s, 3H), 2.24 (s, 3H), 2.17 (s, 3H). Example 26 4-Bromo-7-(3,5-dimethoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-bromo-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 1-cloromethyl-3,5-dimethoxy-benzene according to the general procedure 1.3. HPLC Rt: 6.490 min. 1 H-NMR (CDCl 3 ): δ 7.20 (m, 1H), 6.70 (s, 2H), 6.40 (s, 1H), 6.34 (s, 2H), 6.23 (m, 1H), 5.16 (s, 2H), 3.69 (s, 6H). Example 27 4-Chloro-7-(3-methoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 1-chloromethyl-3-methoxy-benzene according to the general procedure 1.3. HPLC Rt: 7.177 min. 1 H-NMR (DMSO-d6): δ 7.26–7.18 (m, 2H), 6.82–6.80 (m, 1H), 6.67 (s, 1H), 6.70–6.67 (m, 3H), 6.32–6.30 (m, 1H), 5.20 (s, 2H), 3.68 (s, 3H). Example 28 4-Chloro-7-(4-methoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 1-chloromethyl-4-methoxy-benzene according to the general procedure 1.3. HPLC Rt: 6.889 min. 1 H-NMR (DMSO-d6): δ 7.19–7.16 (m, 3H), 6.90–6.88 (m, 2H), 6.69 (s, 2H), 6.32–6.30 (m, 1H), 5.18 (s, 2H), 3.71 (s, 3H). Example 29 N-[4-Chloro-5-iodo-7-(4-methoxy-3,5-dimethyl-1-oxy-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]-2,2-dimethyl-propionamide The title compound was obtained by alkylation of N-(4-chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-2,2-dimethyl-propionamide with 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine-1-oxide according to the general procedure 1.3. HPLC Rt: 6.812 min. 1 H-NMR (DMSO-d6): δ 10.20 (s, 1H), 8.13(s, 1H), 7.97 (s, 1H), 5.50 (s, 2H), 3.72 (s, 3H), 2.50 (s, 3H), 2.16 (s, 3H), 1.22 (s, 9H). Example 30 N-[7-(4-Bromo-3,5-dimethyl-1-oxy-pyridin-2-ylmethyl)-4-chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-2-yl]-2,2-dimethyl-propionamide The title compound was obtained by alkylation of N-(4-chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-2,2-dimethyl-propionamide with 4-bromo-2-chloromethyl-3,5-dimethyl-pyridine-1-oxide according to the general procedure 1.3. HPLC Rt: 7.630 min. 1 H-NMR (DMSO-d6): δ 10.21 (s, 1H), 8.30(s, 1H), 7.91 (s, 1H), 5.59 (s, 2H), 2.72 (s, 3H), 2.28 (s, 3H), 1.22 (s, 9H). Example 31 N-[4-Chloro-5-iodo-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]-2,2-dimethyl-propionamide The title compound was obtained by alkylation of N-(4-chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-2,2-dimethyl-propionamide (A. Gangjee, J. Med. Chem. 2003, 46, 591) with 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine according to the general procedure 1.3. HPLC Rt: 6.627 min. 1 H-NMR (DMSO-d6): δ 10.15 (s, 1H), 8.05(s, 1H), 7.73 (s, 1H), 5.46 (s, 2H), 3.74 (s, 3H), 2.33 (s, 3H), 2.16 (s, 3H), 1.21 (s, 9H). Example 32 N-[7-(4-Bromo-3,5-dimethyl-1-oxy-pyridin-2-ylmethyl)-4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-yl]-2,2-dimethyl-propionamide The title compound was obtained by alkylation of N-(4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-2,2-dimethyl-propionamide with 4-bromo-2-chloromethyl-3,5-dimethyl-pyridine-1-oxide according to the general procedure 1.3. HPLC Rt: 6.806 min. 1 H-NMR (DMSO-d6): δ 10.13 (s, 1H), 8.30(s, 1H), 7.74 (m, 1H), 6.52 (m, 1H), 5.62 (s, 2H), 2.73 (s, 3H), 2.28 (s, 3H), 1.23 (s, 9H). Example 33 N-[4-Chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]-2,2-dimethyl-propionamide The title compound was obtained by alkylation of N-(4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-2,2-dimethyl-propionamide with 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine according to the general procedure 1.3. HPLC Rt: 6.087 min. 1 H-NMR (CDCl3): δ 8.18 (s, 1H), 8.13(s, 1H), 7.18 (m, 1H), 6.49 (m, 1H), 5.50 (s, 2H), 3.72 (s, 3H), 2.26 (s, 3H), 2.22 (s, 3H), 1.34 (s, 9H). Example 34 N-[4-Chloro-7-(4-methoxy-3,5-dimethyl-1-oxy-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]-2,2-dimethyl-propionamide The title compound was obtained by alkylation of N-(4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-2,2-dimethyl-propionamide with 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine-1-oxide according to the general procedure 1.3. HPLC Rt: 6.115 min. 1 H-NMR (CDCl3): δ 8.12 (s, 1H), 8.02(s, 1H), 7.93 (m, 1H), 6.49 (m, 1H), 5.71 (s, 2H), 3.76 (s, 3H), 2.70 (s, 3H), 2.22 (s, 3H), 1.36 (s, 9H). Example 35 N-[4-Chloro-7-(4-chloro-3,5-dimethyl-pyridin-2-ylmethyl)-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-2-yl]-2,2-dimethyl-propionamide The title compound was obtained by alkylation of N-(4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-2,2-dimethyl-propionamide with 4-chloro-2-chloromethyl-3,5-dimethyl-pyridine according to the general procedure 1.3. HPLC Rt: 6.761 min. 1 H-NMR (CDCl3): δ 8.23 (s, 1H), 8.11(s, 1H), 7.15 (m, 1H), 6.50 (m, 1H), 5.71 (s, 2H), 2.43 (s, 3H), 2.33 (s, 3H), 1.35 (s, 9H). Example 36 N-[4-Chloro-7-(4-chloro-3,5-dimethyl-pyridin-2-ylmethyl)-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-2-yl]-2,2-dimethyl-propionamide The title compound was obtained by alkylation of N-(4-chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-2,2-dimethyl-propionamide with 4-chloro-2-chloromethyl-3,5-dimethyl-pyridine according to the general procedure 1.3. HPLC Rt: 7.508 min. 1 H-NMR (CDCl3): δ 8.17 (s, 1H), 8.11 (s, 1H), 8.07 (s, 1H), 5.77 (s, 2H), 2.81 (s, 3H), 2.33 (s, 3H), 1.37 (s, 9H). Example 37 N-[4-Chloro-7-(4-chloro-3,5-dimethyl-1-oxy-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]-2,2-dimethyl-propionamide The title compound was obtained by alkylation of N-(4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-2,2-dimethyl-propionamide with 4-chloro-2-chloromethyl-3,5-dimethyl-pyridine-1-oxide according to the general procedure 1.3. HPLC Rt: 6.688 min. 1 H-NMR (CDCl3): δ 8.15 (s, 1H), 8.09 (s, 1H), 7.87 (m, 1H), 6.47 (m, 1H), 5.77 (s, 2H), 2.84 (s, 3H), 2.31 (s, 3H), 1.37 (s, 9H). Example 38 N-[4-Chloro-7-(4-chloro-3,5-dimethyl-1-oxy-pyridin-2-ylmethyl)-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-2-yl]-2,2-dimethyl-propionamide The title compound was obtained by alkylation of N-(4-chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-2,2-dimethyl-propionamide with 4-chloro-2-chloromethyl-3,5-dimethyl-pyridine-1-oxide according to the general procedure 1.3. HPLC Rt: 7.619 min. 1 H-NMR (CDCl3): δ 8.25 (s, 1H), 8.13 (s, 1H), 7.33 (s, 1H), 5.55 (s, 2H), 2.47 (s, 3H), 2.36 (s, 3H), 1.36 (s, 9H). Example 39 4-Chloro-5-[(dibenzylamino)-methyl]-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine Step 1. Octanoic acid (4-chloro-5-[(dibenzylamino)-methyl]-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-amide A solution of octanoic acid {5-[(dibenzylamino)-methyl]-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-2-yl}-amide (1.0 g, 2 mmol; J. Chem. Soc. Perkin Trans. 1 1998, 1637), BnNEt 3 Cl (1.4 g, 4 mmol), PhNMe 2 (0.5 mL) and POCl 3 (1.73 mL, 12 mmol) in CH 3 CN (9.2 mL) was heated to 100° C. for 40 min and concentrated. The residue was poured into ice water and neutralized with 2N NaOH, extracted with EtOAc (50 mL×3), and evaporated, to give the title compound (0.80 g, 76%). HPLC Rt: 6.868 min. 1 H-NMR (DMSO-d 6 ): δ 12.19 (s, 11H), 10.49 (s, 1H), 1.45–7.21 (m, 1H), 3.80 (s, 2H), 3.59 (s, 4H), 2.41 (t, 2H), 1.56 (m, 2H), 1.27 (br s 8H), 0.85 (t, 3H). Step 2. 4-Chloro-5-[(dibenzylamino)-methyl]-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine A suspension of octanoic acid {4-chloro-5-[(dibenzylamino)-methyl]-7H-pyrrolo[2,3-d]pyrimidin-2-yl}-amide (150 mg, 0.30 mmol), 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine (56 mg, 0.30 mmol) and K 2 CO 3 (84 mg, 0.60 mmol) in dry DMF (1 mL) was heated to 45° C. overnight. After work-up (EtOAc) and evaporation, the residue was taken up in methanolic 4N HCl (1 mL), stirred at room temperature for 1 h, and neutralized to pH 7 with 2N NaOH. Extraction with EtOAc (10 mL×3), evaporation and purification by preparative TLC (MeOH/CH 2 Cl 2 10:1) gave the title compound (70.5 mg, 45%). HPLC Rt: 5.362 min. 1 H-NMR (DMSO-d 6 ): δ 8.05 (s, 1H), 7.30–7.22 (m, 10H), 6.99(s, 1H), 6.57 (s, 2H), 5.27 (s 2H), 3.70 (s, 2H), 3.65 (s, 3H), 3.54 (s, 4H), 2.17 (s, 3H), 2.15 (s, 3H). Example 40 4-Chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-5-phenylaminomethyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine Step 1. Octanoic acid (4-chloro-5-phenylaminomethyl-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-amide A solution of octanoic acid {5-[(dibenzylamino)-methyl]-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-2-yl}-amide (2.42 g, 3 mmol) and aniline (10 mL) was heated to 90° C. in a sealed tube overnight, concentrated, filtered, and washed with MeOH (2 mL×3) to give the title compound (1.1 g, 57%). HPLC Rt: 6.327 min. 1 H-NMR (DMSO-d 6 ): δ 11.77 (s, 1H), 11.47 (s, 1H), 11.37 (s, 1H), 7.05 (m, 2H), 6.85 (s, 1H), 6.62 (m, 2H), 6.52 (m, 1H), 5.58 (t, 1H), 4.31 (d, 2H), 2.43 (t, 2H), 1.58 (m, 2H), 1.27 (m, 8H), 0.86 (t, 3H). Step 2. 4-Chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-5-phenylaminomethyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine A solution of octanoic acid (4-chloro-5-phenylaminomethyl-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-amide (270 mg, 0.68 mmol), BnNEt 3 Cl (0.48 g, 1.36 mmol), PhNMe 2 (0.17 mL) and POCl 3 (0.59 mL, 4.08 mmol) in CH 3 CN (3 mL) was heated to 100° C. for 40 min and concentrated. The residue was poured into ice water and neutralized with 2N NaOH, extracted with EtOAc (20 mL×3), evaporated, to give 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine as a crude oil (282 mg) which was used without purification. A suspension of this crude (282 mg, 0.68 mmol), 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine (140 mg, 0.68 mmol) and Cs 2 CO 3 (266 mg, 0.68 mmol) in dry DMF (1 mL) was heated to 45° C. overnight. After work-up (EtOAc) and evaporation, the residue was taken up in methanolic 4N HCl (1 mL), stirred at room temperature for 1 h, and neutralized to pH 7 with 2N NaOH. Extraction with EtOAc (10 mL×3), evaporation and purification by preparative TLC (MeOH/CH 2 Cl 2 10:1) gave the title compound (4.8 mg, 1.6%). HPLC Rt: 4.785 min. 1 H-NMR (CDCl 3 ): δ 8.12 (s, 1H), 7.18(m, 2H), 6.75(m, 2H), 6.60 (s, 1H), 5.26(s, 2H), 4.93 (s, 2H), 4.74 (s, 2H), 3.70 (s, 3H), 3.00 (s, 3H), 2.23 (s, 3H), 2.16 (s, 3H). Example 41 4-Chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-5-[(methyl-phenyl-amino)-methyl]-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine Step 1: Octanoic acid (4-chloro-5-[(methyl-phenyl-amino)-methyl]-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-amide The title compound was obtained by treating octanoic acid {5-[(dibenzylamino)-methyl]-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-2-yl}-amide (2.42 g, 3 mmol) and N-methylaniline (10 mL) as in step 1 of the previous example. HPLC Rt: 6.325 min. 1 H-NMR (DMSO-d 6 ): δ 11.73 (s, 1H), 11.47 (s, 1H), 11.35 (s, 1H), 7.13 (m, 2H), 6.78 (s, 2H), 6.60 (m, 2H), 4.64(s, 2H), 2.98 (s, 3H), 2.43 (t, 2H), 1.58 (m, 2H), 1.27 (m, 8H), 0.86 (t, 3H). Step 2: 4-Chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-5-[(methyl-phenyl-amino)-methyl]-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of octanoic acid {4-chloro-5-[(methyl-phenyl-amino)-methyl]-7H-pyrrolo[2,3-d]pyrimidin-2-yl}-amide with 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine and deprotection with 4N HCl as in step 2 of the previous example. HPLC Rt: 4.844 min. 1 H-NMR (CDCl 3 ): δ 8.20 (s, 1H), 7.16 (m, 2H), 6.87 (s, 1H), 6.70–6.64 (m, 2H), 5.28 (s, 2H), 5.13 (s, 2H), 4.46 (s, 2H), 4.15 (br s, 1H), 3.73 (s, 3H), 2.25 (s, 3H), 2.18 (s, 3H). Example 42 4-Chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-6-pyrrolidin-1-ylmethyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine Step 1. Octanoic acid (4-chloro-6-pyrrolidin-1-ylmethyl-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-amide A solution of octanoic acid (4-oxo-6-pyrrolidin-1-ylmethyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-2-yl)-amide (0.36 g 1 mmol; J. Chem. Soc. Perkin Trans. 1 1998, 1637), BnNEt 3 Cl (0.70 g, 2 mmol), PhNMe 2 (0.25 mL) and POCl 3 (0.86 mL, 6 mmol) in CH 3 CN (5 mL) was heated to 100° C. for 40 min and concentrated. The residue was poured into ice water and neutralized with 2N NaOH, extracted with EtOAc (50 mL×3), and evaporated to give octanoic acid (4-chloro-6-pyrrolidin-1-ylmethyl-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-amide as a crude (0.33 g) which was used without purification. HPLC Rt: 6.737 min. 1 H-NMR (CDCl 3 ): δ 11.60 (br s, 1H), 10.20 (br s, 1H), 6.38 (s, 1H), 3.86 (s, 2H), 2.90 (m, 2H), 2.70 9s, 4H), 1.86 (s, 4H), 1.78 (t, 2H), 1.32–1.29 (m, 8H), 0.90 (t, 3H). Step 2. 4-Chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-6-pyrrolidin-1-ylmethyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine A suspension of the crude octanoic acid (4-chloro-6-pyrrolidin-1-ylmethyl-7H-pyrrolo[2,3-d]pyrimidin-2-yl)-amide (330 mg, 0.87 mmol), 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine (162 mg, 0.87 mmol) and K 2 CO 3 (121 mg, 0.87 mmol) in dry DMF (1 mL) was heated to 45° C. overnight. After work-up (EtOAc) and evaporation, the residue was taken up in 6N methanolic HCl (1 mL), stirred at room temperature for 1 h, and neutralized to pH 7 with 2N NaOH. Extraction with EtOAc (10 mL×3), evaporation and purification by preparative TLC (MeOH/CH 2 Cl 2 10:1) yielded 4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-6-pyrrolidin-1-ylmethyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine (4.1 mg, yield 1.0%). HPLC Rt: 6.092 min. 1 H-NMR (CDCl 3 ): δ 8.09 (s, 1H), 6.31(s, 1H), 5.55(s, 2H), 4.85(s, 2H), 3.77 (s, 3H), 3.52(brs, 2H), 2.43 (m, 4H), 1.76–1.71 (m, 4H). Example 43 4-Chloro-5-isopropyl-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine Step 1. 3-Bromo-4-methyl-pentanal A mixture of 4-methyl-pentanal (8.60 g, 0.10 mol), 5,5-dibromobarbituric acid (DBBA, 17.15 g, 0.06 mol), 40% HBr (2 mL) and HOAc (1 mL) in CH 2 Cl 2 (180 mL) was stirred at 25° C. for 5 h. after filtration, the filtrate was washed with 1N Na 2 SO 3 , Na 2 CO 3 , and brine, dried with Na 2 SO 4 , and evaporated to give 3-bromo-4-methyl-pentanal (8.76 g, 53%). 1 H-NMR (CDCl 3 ): δ 9.40 (s, 1H), 4.40 (t, 1H), 2.10 (m, 1H), 1.06 (s, 3H), 1.05 (s, 3H). Step 2. 2-Amino-5-isopropyl-3,7-dihydro-pyrrolo[2,3-d]pyrimidin-4-one A suspension of 2,4-diamino-6-hydroxypyrimidine (6.68 g, 50 mmol), AcONa (8.3 g 100 mmol) and 3-bromo-4-methyl-pentanal (8.76 g, 50 mmol) in CH 3 CN (100 mL) and H 2 O (100 mL) was stirred at 25° C. overnight whereupon the starting materials gradually dissolved and the desired pyrrolo[2,3-d]pyrimidine precipitated. The precipitate was collected by filtration and washed with MeOH to give 2-amino-5-isopropyl-3,7-dihydro-pyrrolo[2,3-d]pyrimidin-4-one (3.80 g, 40%). HPLC Rt: 4.408 min. 1 H-NMR (DMSO-d 6 ): δ 10.58 (s, 1H), 10.10 (s, 1H), 6.30 (s, 1H), 5.97 (s, 2H), 3.03 (7, 1H), 1.20 (s, 3H), 1.19 (s, 3H). Step 3. 4-Chloro-5-isopropyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine A mixture of 2-amino-5-isopropyl-3,7-dihydro-pyrrolo[2,3-d]pyrimidin-4-one and acetic anhydride (20 mL) was heated to reflux for 3 h and evaporated. The residue was treated with BnNEt 3 Cl (8.99 g, 40 mmol), PhNMe 2 (4.9 mL) and POCl 3 (17 mL, 120 mmol) in CH 3 CN (100 mL) at 100° C. for 40 min and concentrated. The residue was poured into ice water and neutralized with 2N NaOH, extracted with EtOAc (80 mL×3), and evaporated to give an oil which was digested with methanolic 4N HCl (50 mL) at 50° C. for 2 h. After cooling, and neutralization to pH 7 with 2N NaOH, the solid was collected by filtration and dried to give 4-chloro-5-isopropyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine (1.88 g, 45%). HPLC Rt: 5.796 min. 1 H-NMR (DMSO-d 6 ): δ 11.170 (s, 1H), 6.82 (s, 1H), 6.42 (s, 2H), 3.24 (7, 1H), 1.25 (s, 3H), 1.23 (s, 3H). Step 4. 4-Chloro-5-isopropyl-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine A suspension of 4-chloro-5-isopropyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine (105 mg, 0.5 mmol), 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine (93 mg, 0.5 mmol) and K 2 CO 3 (85 mg, 0.6 mmol) in dry DMF (1 mL) was heated to 45° C. overnight, Work-up (EtOAc), evaporation, and purification by preparative TLC (MeOH/CH 2 Cl 2 10:1) gave 4-chloro-5-isopropyl-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine (36 mg). HPLC Rt: 5.867 min. 1 H-NMR (DMSO-d 6 ): δ 8.07 (s, 1H), 6.74(s, 1H), 6.51 (s, 2H), 5.22 (s, 2H), 3.70 0s, 3H), 3.23 (7, 1H), 2.21 (s, 3H), 2.15 (s, 3H). Example 44 4-chloro-7-(4-chloro-3-methyl-pyridin-2-ylmethyl)-5-isopropyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-5-isopropyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 4-chloro-2-chloromethyl-3,5-dimethyl-pyridine according to the general procedure 1.3. HPLC Rt: 6.997 min. 1 H-NMR (CDCl 3 ): δ 8.27 (s, 1H), 6.61 (s, 1H), 5.33 (s, 2H), 5.09 (s, 2H), 3.35 (7, 1H), 2.35 (s, 6H), 1.25 (s, 3H), 1.23 (s, 3H). Example 45 4-Chloro-7-(4-chloro-3-methyl-1-oxy-pyridin-2-ylmethyl)-5-isopropyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The title compound was obtained by alkylation of 4-chloro-5-isopropyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine with 2-chloromethyl-3,5-dimethyl-pyridine-1-oxide according to the general procedure 1.3. HPLC Rt: 6.753 min. 1 H-NMR (DMSO-d 6 ): δ 8.37 (s, 1H), 7.03 (s, 1H), 6.63 (s, 2H), 5.40 (s, 2H), 3.20 (7, 1H), 2.59 (s, 3H), 2.27 (s, 3H), 1.20 (s, 3H), 1.19 (s, 3H). Example 46 4-Chloro-5-(2-isobutylamino-ethyl)-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine Step 1. 4-(tert-Butyl-diphenyl-silanyloxy)-butan-1-ol A mixture of tBuPh 2 SiCl (25 mL, 98 mmol), 1,4-butanediol (25 mL, 281 mmol), iPrNEt 2 (50 mL, 303 mmol) and CH 2 Cl 2 (50 mL) was stirred at rt for 14 h, concentrated, diluted with diethyl ether, washed with water (3×) and brine. Drying (Na 2 SO 4 ) and concentration afforded the title compound as a clear oil (29.8 g, 93%) which was used without further purification. Rf (EtOAc:hexane 1:4) 0.3. 1 H-NMR (CDCl 3 ): δ 7.71 (dd, 4H), 7.43 (m, 6H), 3.74 (t, 2H), 3.70 (q, 2H), 2.10 (br. t, 1H), 1.69 (m, 4H), 1.08 (s, 9H). Step 2. 4-(tert-Butyl-diphenyl-silanyloxy)-butyraldehyde A solution of 4-(tert-butyl-diphenyl-silanyloxy)-butan-1-ol (29.8 g, 91 mmol) in CH 2 Cl 2 (70 mL) was added to a slurry of PCC (21.5 g, 100 mmol), celite (50 g) and CH 2 Cl 2 (300 mL). The mixture was stirred for 2 h at rt, and the celite was removed by filtration and washed with CH 2 Cl 2 (300 mL). Concentration and chromatography (EtOAc/hexane 1:4) afforded the title compound as a clear oil (22.2 g, 75%). Rf (EtOAc:hexane 1:4) 0.7. 1 H-NMR (CDCl 3 ): δ 9.82 (t, 1H), 7.68 (dd, 4H), 7.41 (m, 6H), 3.71 (t, 2H), 2.57 (t, 2H), 1.91 (q, 2H), 1.07 (s, 9H). Step 3. 2-Bromo-4-(tert-butyl-diphenyl-silanyloxy)-butyraldehyde A mixture of 4-(tert-butyl-diphenyl-silanyloxy)-butyraldehyde (22.2 g, 68 mmol), 5,5-dibromobarbituric acid (12.1 g, 43 mmol) and CH 2 Cl 2 (80 mL) was treated with 70% aq HBr (1 mL, 14 mmol) and stirred at rt for 1 h. The by-product (barbituric acid) was removed by filtration and washed with CH 2 Cl 2 (100 mL). The combined organic layers were washed (1N Na 2 S 2 O 3 , 5% NaHCO 3 , half-sat. brine) and dried (Na 2 SO 4 ). Concentration gave the title compound as a clear oil (25.3 g, 92%) which was used without further purification. Rf (EtOAc:hexane 1:4) 0.7. 1 H-NMR (CDCl 3 ): δ 9.55 (d, 1H), 7.68 (dd, 4H), 7.41 (m, 6H), 4.60 (ddd, 1H), 3.84 (m, 2H), 2.35 (m, 1H), 2.10 (m, 1H), 1.07 (s, 9H). Step 4. 2-Amino-5-[2-(tert-butyl-diphenyl-silanyloxy)-ethyl]-3,7-dihydro-pyrrolo[2,3-d]pyrimidin-4-one The title compound was obtained by treating 2-bromo-4-(tert-butyl-diphenyl-silanyloxy)-butyraldehyde (25.3 g, 62 mmol) with 2,4-diamino-6-hydroxypyrimidine (10.2 g, 124 mmol) according to the general procedure 1.1 (23.4 g, 87%). HPLC Rt: 6.981 min. 1 H-NMR (CDCl 3 ): δ 10.67 (s, 1H), 10.14 (s, 1H), 7.55 (m, 4H), 7.38 (m, 6H), 6.37 (s, 1H), 5.98 (s, 2H), 3.86 (t, 2H), 2.86 (t, 2H), 0.95 (s, 9H). Step 5. N-{7-Acetyl-5-[2-(tert-butyl-diphenyl-silanyloxy)-ethyl]-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-2-yl}-acetamide A solution of 2-amino-5-[2-(tert-butyl-diphenyl-silanyloxy)-ethyl]-3,7-dihydro-pyrrolo[2,3-d]pyrimidin-4-one (22.7 g, 52 mmol) in Ac 2 O (200 mL) was heated to 110° C. for 2.5 h, concentrated, diluted with toluene (300 mL) and concentrated again to afford the title compound to afford the title compound as a crude brown oil (27 g) which was used without further purification. An aliquot was purified by chromatography for characterization. HPLC Rt: 8.349 min. 1 H-NMR (CDCl 3 ): δ 11.77 (s, 1H), 8.81 (s, 1H), 7.61 (dd, 4H), 7.30 (m, 7H), 6.37 (s, 1H), 4.00 (t, 2H), 3.02 (t, 2H), 2.70 (s, 3H), 2.23 (s, 3H), 1.04 (s, 9H). Step 6. N-{7-Acetyl-5-[2-(tert-butyl-diphenyl-silanyloxy)-ethyl]-4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-yl}-acetamide A solution of crude N-{7-acetyl-5-[2-(tert-butyl-diphenyl-silanyloxy)-ethyl]-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-2-yl}-acetamide (26.4 g, 51 mmol), BnNEt 3 Cl (23.2 g, 102 mmol), PhNMe 2 (19.6 mL, 153 mmol) and POCl 3 (9.3 mL, 77 mmol) in CH 3 CN (100 mL) was heated to 80° C. for 1.5 h. The mixture was diluted with EtOAc (800 mL), washed (sat. NaHCO 3 , brine) and concentrated to afford the title compound as an oil (46 g) which was used without further purification. An aliquot was purified by chromatography for characterization. HPLC Rt: 8.562 min. 1 H-NMR (CDCl 3 ): δ 8.05 (s, 1H), 7.68 (s, 1H), 7.57 (dd, 4H), 7.40 (m, 6H), 3.99 (t, 2H), 3.06 (t, 2H), 2.98 (s, 3H), 2.52 (s, 3H), 1.04 (s, 9H). Step 7. N-{5-[2-(tert-Butyl-diphenyl-silanyloxy)-ethyl]-4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-yl}-acetamide A solution of crude N-{7-acetyl-5-[2-(tert-butyl-diphenyl-silanyloxy)-ethyl]-4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-yl}-acetamide (46 g) in MeOH (150 mL) was treated with K 2 CO 3 (8.0 g, 58 mmol) at rt for 15 min. Filtration, concentration, and chromatography (EtOAc/hexane 1:1) afforded the title compound as an oil contaminated with residual PhNMe2 from step 6. The oil was diluted with EtOAc (40 mL) and treated with hexane (40 mL) to obtained the desired product as a pale yellow precipitate (4.2 g, 16% over 3 steps). HPLC Rt: 8.558 min. 1 H-NMR (CDCl 3 ): δ 11.75 (br. s, 1H), 11.35 (br. s, 1H), 7.60 (dd, 4H), 7.37 (m, 6H), 3.97 (t, 2H), 3.10 (t, 2H), 2.57 (s, 3H), 1.06 (s, 9H). Step 8. N-[5-[2-(tert-Butyl-diphenyl-silanyloxy)-ethyl]-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]-acetamide A mixture of N-{5-[2-(tert-butyl-diphenyl-silanyloxy)-ethyl]-4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-yl}-acetamide (344 mg, 0.70 mmol), 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine hydrochloride (175 mg, 0.77 mmol), K 2 CO 3 (516 mg, 3.7 mmol) and DMF (3.0 mL) was stirred at rt overnight. Work-up (EtOAc/water; brine) afforded the title compound as an off-white solid which was used without further purification (516 mg, “115%”). HPLC Rt: 8.419 min. 1 H-NMR (CDCl 3 ): δ 8.20 (s, 1H), 7.95 (s, 1H), 7.55 (dd, 4H), 7.32 (m, 6H), 7.04 (s, 1H), 5.37 (s, 2H), 3.91 (t, 2H), 3.73 (s, 3H), 3.06 (t, 2H), 2.57 (s, 3H), 2.26 (s, 3H), 2.25 (s, 3H), 0.97 (s, 9H). Step 9. 5-[2-(tert-Butyl-diphenyl-silanyloxy)-ethyl]-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine A solution of N-[5-[2-(tert-Butyl-diphenyl-silanyloxy)-ethyl]-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]-acetamide (511 mg) in THF (3 mL) and MeOH (3 mL) was treated with NaOH 2M (3 mL) at 45° C. for 1.5 h. Work-up and chromatography (EtOAc/hexane 1:1) afforded the title compound as a white powder (290 mg, 69% over 2 steps). HPLC Rt: 8.198 min. 1 H-NMR (CDCl 3 ): δ 8.20 (s, 1H), 7.57 (dd, 4H), 7.40 (m, 2H), 7.32 (m, 4H), 6.69 (s, 1H), 5.26 (s, 2H), 4.90 (s, 2H), 3.98 (t, 2H), 3.66 (s, 3H), 3.00 (t, 2H), 2.24 (s, 3H), 2.18 (s, 3H), 0.96 (s, 9H). Step 10. 2-[2-Amino-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-ethanol A solution of 5-[2-(tert-butyl-diphenyl-silanyloxy)-ethyl]-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine (246 mg, 0.41 mmol) in THF (5 mL) was treated with TBAF (1N in THF, 0.5 mL, 0.50 mmol) at rt for 1 h. Work-up (EtOAc/water, brine) gave the crude product as an oil, which was diluted with diethyl ether (15 mL) whereupon the desired product precipitated out of solution as a white powder (110 mg, 74%). HPLC Rt: 4.474 min. 1 H-NMR (CDCl 3 ): δ 8.21 (s, 1H), 6.78 (s, 1H), 5.30 (s, 2H), 4.93 (s, 2H), 3.87 (t, 2H), 3.76 (s, 3H), 3.03 (t, 2H), 2.26 (s, 3H), 2.23 (s, 3H). Step 11. Methanesulfonic acid 2-[2-amino-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-ethyl ester A solution of 2-[2-amino-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-ethanol (11.6 mg, 0.031 mmol) and Et 3 N (30 ul, 0.22 mmol) in THF (2 mL) was treated with MsCl (11 uL, 0.14 mmol) at rt for 15 min to give a solution of the title compound which was used without further purification. In a separate experiment, the material was purified by preparative TLC (EtOAc 100%). HPLC Rt: 4.765 min. 1 H-NMR (CDCl 3 ): δ 8.22 (s, 1H), 6.80 (s, 1H), 5.31 (s, 2H), 4.93 (s, 2H), 4.42 (t, 2H), 3.77 (s, 3H), 2.98 (t, 2H), 2.85 (s, 3H), 2.23 (s, 3H), 2.07 (s, 3H). Step 12. 4-Chloro-5-(2-isobutylamino-ethyl)-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamine The solution of methanesulfonic acid 2-[2-amino-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-ethyl ester in THF obtained from step 11 was diluted with i-BuNH 2 (4 mL) and heated to 50° C. for 15 h. Concentration, work-up (EtOAc/NaHCO 3 sat.; brine) and preparative TLC (MeOH:Et 3 N:CH 2 Cl 2 7:3:100) gave the title compound as a colorless oil (6 mg, 50%). HPLC Rt: 4.263 min. 1 H-NMR (CDCl 3 ): δ 8.20 (s, 1H), 6.79 (s, 1H), 5.29 (s, 2H), 4.97 (s, 2H), 3.76 (s, 3H), 3.04 (t, 2H), 2.96 (t, 2H), 2.53 (d, 2H), 2.26 (s, 3H), 2.22 (s, 3H), 1.85 (oct., 1H), 0.90 (d, 6H). Example 47 2-Amino-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one The title compound was obtained by condensation between (2-amino-4,6-dichloro-pyrimidin-5-yl)-acetic acid ethyl ester and (4-methoxy-3,5-dimethyl-pyridin-2-yl)-methylamine according to the general procedure 1.2. HPLC Rt: 4.893 min. 1 H-NMR (CDCl 3 ): δ 8.07 (s, 1H), 5.03 (s, 2H), 4.92 (s, 2H), 3.77 (s, 3H), 3.57 (s, 2H), 2.31 (s, 3H), 2.20 (s, 3H). Example 48 2-Amino-4-chloro-7-(4-chloro-3,5-dimethyl-pyridin-2-ylmethyl)-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one The title compound was obtained by alkylation of 4-chloro-pyrrolo[2,3-d]pyrimidin-6-one with 2-chloromethyl-4-chloro-3,5-dimethyl-pyridine according to the general procedure 1.3. HPLC Rt: 5.367 min. 1 H-NMR (CDCl 3 ): δ 8.09 (s, 1H), 5.02 (s, 2H), 4.96 (s, 2H), 3.57 (s, 2H), 2.45 (s, 3H), 2.29 (s, 3H). Example 49 2-Amino-4-chloro-7-(3,5-dimethyl-4-methoxy-1-oxy-pyridin-2-ylmethyl)-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one The title compound was obtained by oxidation of 2-amino-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one with m-CPBA according to the general procedure 2.1. HPLC Rt: 4.763 min. 1 H-NMR (DMSO-d6): δ 8.01 (s, 1H), 7.01 (s, 2H), 4.93 (s, 2H), 3.73 (s, 3H), 3.46 (s, 2H), 2.40 (s, 3H), 2.19 (s, 3H). Example 50 2-Amino-4-chloro-7-(4-chloro-3,5-dimethyl-1-oxy-pyridin-2-ylmethyl)-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one The title compound was obtained by oxidation of 2-amino-4-chloro-7-(4-chloro-3,5-dimethyl-pyridin-2-ylmethyl)-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one with m-CPBA according to the general procedure 2.1. HPLC Rt: 4.90 min. 1 H-NMR (CDCl 3 /CD 3 OD): δ 7.96 (s, 1H), 5.12 (s, 2H), 3.38 (s, 2H), 2.47 (s, 3H), 2.27 (s, 3H). Example 51 2-Amino-4-chloro-7-(3,4,5-trimethoxy-benzyl)-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one The title compound was obtained by condensation between (2-Amino-4,6-dichloro-pyrimidin-5-yl)-acetic acid ethyl ester and 3,4,5-Trimethoxy-benzylamine according to the general procedure 1.2. HPLC Rt: 6.391 min. 1 H-NMR (CDCl 3 ): δ 6.70 (s, 2H), 5.14 (s, 2H), 4.77 (s, 2H), 3.84 (s, 6H), 3.81 (s, 3H), 3.47 (s, 2H). Example 52 2-Amino-4-chloro-7-(2-bromo-3,4,5-trimethoxy-benzyl)-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one The title compound was obtained by treating 2-amino-4-chloro-7-(3,4,5-trimethoxy-benzyl)-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one with bromine in acetic acid according to the general procedure 3.1. HPLC Rt: 7.150 min. 1 H-NMR (CDCl 3 ): δ 6.49 (s, 1H), 5.14 (s, 2H), 4.94 (s, 2H), 3.90 (s, 3H), 3.86 (s, 3H), 3.75 (s, 3H), 3.55 (s, 2H). Example 53 2-Amino-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-5-methyl-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one The title compound was obtained by alkylation of 2-amino-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one with iodomethane according to the general procedure 1.5. HPLC Rt: 4.091 min. 1 H-NMR (CDCl 3 ): δ 8.01 (s, 1H), 5.15 (s, 2H), 4.93 (d, 1H), 4.87 (d, 1H), 3.76 (s, 3H), 3.51 (s, 1H), 2.29 (s, 3H), 2.20 (s, 3H), 1.78 (s, 3H). Example 54 2-Amino-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-5,5-dimethyl-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one The title compound was obtained by alkylation of 2-amino-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one with iodomethane according to the general procedure 1.5. HPLC Rt: 5.002 min. 1 H-NMR (CDCl 3 ): δ 8.02 (s, 1H), 5.02 (s, 2H), 4.90 (s, 2H), 3.75 (s, 3H), 2.29 (s, 3H), 2.18 (s, 3H), 1.53 (s, 6H). Example 55 2-Amino-4-chloro-7-(2-bromo-3,4,5-trimethoxy-benzyl)-5,5-dimethyl-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one The title compound was obtained by alkylation of 2-amino-4-chloro-7-(3,4,5-trimethoxy-benzyl)-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one with iodomethane according to the general procedure 1.5. HPLC Rt: 6.944 min. 1 H-NMR (CDCl 3 ): δ 6.34 (s, 1H), 5.09 (s, 2H), 4.93 (s, 2H), 3.90 (s, 3H), 3.86 (s, 3H), 3.71 (s, 3H), 1.52 (s, 6H). Example 56 4-Chloro-5-hydroxy-2-imino-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-2,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one The title compound was obtained by oxidation of 2-amino-4-chloro-7-(4-methoxy-3,5-dimethyl-pyridin-2-ylmethyl)-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one with selenium dioxide according to the general procedure 1.6. HPLC Rt: 4.294 min. 1 H-NMR (CDCl 3 ): δ 8.04 (s, 1H), 5.93 (s, 1H), 5.76 (s, 1H), 4.97 (s, 2H), 3.765 (s, 3H), 2.29 (s, 3H), 2.20 (s, 3H). Example 57 4-Chloro-5-hydroxy-2-imino-7-(3,4,5-trimethoxy-benzyl)-2,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one The title compound was obtained by oxidation of 2-amino-4-chloro-7-(3,4,5-trimethoxy-benzyl)-5,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one with selenium dioxide according to the general procedure 1.6. HPLC Rt: 6.156 min. 1 H-NMR (CDCl 3 ): δ 6.68 (s, 2H), 6.12 (s, 1H), 5.93 (s, 1H), 4.84 (s, 2H), 3.86 (s, 6H), 3.83 (s, 3H). Example 58 4-Chloro-5-hydroxy-2-imino-7-(2-bromo-3,4,5-trimethoxy-benzyl)-2,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one The title compound was obtained by oxidation of 4-chloro-5-hydroxy-2-imino-7-(2-bromo-3,4,5-trimethoxy-benzyl)-2,7-dihydro-pyrrolo[2,3-d]pyrimidin-6-one according to the general procedure 1.6. HPLC Rt: 6.230 min. 1 H-NMR (CDCl 3 ): δ 6.57 (s, 1H), 6.14 (s, 1H), 5.91 (s, 1H), 5.01 (s, 2H), 3.90 (s, 3H), 3.87 (s, 3H), 3.78 (s, 3H). BIOLOGY EXAMPLES Example A rHSP90 Competitive Binding Assay Five microgram of purified rHSP90 protein (Stressgen, BC, Canada, #SPP-770) in phosphate buffered saline (PBS) was coated on 96 well plates by incubating overnight at 4° C. Unbound protein was removed and the coated wells were washed twice with 200 μL PBS. DMSO controls (considered as untreated samples) or test compounds were then added at 100-30-10-3-1-0.3 μM dilutions (in PBS), the plates mixed for 30 seconds on the plate shaker, and then incubated for 60 min. at 37° C. The wells were washed twice with 200 μL PBS, and 10 μM biotinylated-geldanamycin (biotin-GM) was added and incubated for 60 min. at 37° C. The wells were washed again twice with 200 μL PBS, before the addition of 20 μg/mL streptavidin-phycoerythrin (streptavidin-PE) (Molecular Probes, Eugene, Oreg.) and incubation for 60 min. at 37° C. The wells were washed again twice with 200 μL PBS. Relative fluorescence units (RFU) was measured using a SpectraMax Gemini XS Spectrofluorometer (Molecular Devices, Sunnyvale, Calif.) with an excitation at 485 nm and emission at 580 nm; data was acquired using SOFTmax®PRO software (Molecular Devices Corporation, Sunnyvale, Calif.). The background was defined as the RFU generated from wells that were not coated with HSP90 but were treated with the biotin-GM and streptavidin-PE. The background measurements were subtracted from each sample treated with biotin-GM and streptavidin-PE measurements before other computation. Percent inhibition of binding for each sample was calculated from the background subtracted values as follows: % binding inhibition=[(RFU untreated−RFU treated)/RFU untreated]×100. Example B Cell Lysate Binding Assay MCF7 breast carcinoma cell lysates were prepared by douncing in lysing buffer (20 mM HEPES, pH 7.3, 1 mM EDTA, 5 mM MgCl 2 , 100 mM KCl), and then incubated with or without test compound for 30 mins at 4° C., followed by incubation with biotin-GM linked to BioMag™ streptavidin magnetic beads (Qiagen) for 1 hr at 4° C. The tubes were placed on a magnetic rack, and the unbound supernatant removed. The magnetic beads were washed three times in lysis buffer and boiled for 5 mins at 95° C. in SDS-PAGE sample buffer. Samples were analyzed on SDS protein gels, and Western blots were done for rHSP90. Bands in the Western Blots were quantitated using the Bio-rad Fluor-S MultiImager, and the % inhibition of binding of rHSP90 to the biotin-GM was calculated. The lysate binding ability of selected compounds of the invention based on the above assay is summarized in Table 2. The IC 50 reported is the concentration of test compound needed to achieve 50% inhibition of the biotin-GM binding to rHSP90 in the MCF7 cell lysates. Example C HER2 Degradation Assay MCF7 breast carcinoma cells (ATCC) were grown in Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal bovine serum (FBS) and 10 mM HEPES, and plated in 24 well plates (50% confluent). Twenty-four hrs later (cells are 65–70% confluent), test compounds were added and incubated overnight for 16 h. For the less potent compounds, the amounts added were 100 μM, 30 μM, 10 μM and 1 μM, and for more potent compounds, the amounts added were 1 μM, 0.3 μM, 0.1 μM, 0.03 μM, 0.01 μM and 0.003 μM. The wells were washed with 1 mL phosphate buffered saline (PBS), and 200 μL trypsin was added to each well. After trypsinization was complete, 50 μL of FBS was added to each well. Then 200 μL cells was transferred to 96 well plates. The cells were pipetted up and down to obtain a single cell suspension. The plates were centrifuged at 2,500 rpm for 1 min using a Sorvall Legend RT™ tabletop centrifuge (Kendro Laboratory Products, Asheville, N.C.). The cells were then washed once in PBS containing 0.2% BSA and 0.2% sodium azide (BA buffer). Phycoerythrin (PE) conjugated anti HER2/Neu antibody (Becton Dickinson, #340552), or PE conjugated anti-keyhole limpet hemocyanin [KLH] (Becton Dickinson, #340761) control antibody was added at a dilution of 1:20 and 1:40 respectively (final concentration was 1 μg/mL) and the cells were pipeted up and down to form a single cell suspension, and incubated for 15 mins. The cells were washed twice with 200 μL BA buffer, and resuspended in 200 μL BA buffer, and transferred to FACSCAN tubes with an additional 250 μL BA buffer. Samples were analyzed using a FACSCalibur™ flow cytometer (Becton Dickinson, San Jose, Calif.) equipped with Argon-ion laser that emits 15 mW of 488 nm light for excitation of the PE fluorochrome. 10,000 events were collected per sample. A fluorescence histogram was generated and the mean fluorescence intensity (MFI) of each sample was determined using Celiquest software. The background was defined as the MFI generated from cells incubated with control IgG-PE, and was subtracted from each sample stained with the HER2/Neu antibody. Cells incubated with DMSO were used as untreated controls since the compounds were resuspended in DMSO. Percent degradation of HER2 was calculated as follows: % HER2 degraded=[(MF1 untreated cells−MF1 treated cells)/MF1 untreated cell]×100 The HER2 degradation ability of selected compounds of the invention based on this assay is summarized in Table 2. IC 50 is defined as the concentration at which there was 50% degradation of the HER2/Neu protein. Example D MTS Assay MTS assays measure the cytotoxicity of geldanamycin derivatives. MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) is a tetrazolium dye that is converted to a formazan product by dehydrogenase enzymes of metabolically active cells (Corey, A. et al. “Use of an aqueous soluble tetrazolium/formazan assay for cell growth assays in culture,” Cancer Commun. 1991, 3, 207–212). Cells were seeded in 96 well plates at 2000 cells/well and allowed to adhere overnight in Dulbecco's modified Eagle's medium supplemented with 10% fetal bovine serum. The final culture volume was 100 μl. Viable cell number was determined by using the Celltiter 96 AQ ueous Non-radioactive Cell Proliferation Assay (Promega, Madison Wis.). The MTS /PMS (phenazine methosulfate) solution was mixed at a ratio of 20:1, and 20 μL was added per well to 100 μl of culture medium. After 2–4 hours, the formation of the formazan product was measured at 490 nm absorbance using a multiwell plate spectrophotometer. Background was determined by measuring the Abs 490 nm of cell culture medium and MTS-PMS in the absence of cells and was subtracted from all values. Percent viable cells was calculated as follows: % viable cells=(Abs at 490 nm treated cells/Abs at 490 nm untreated cells)×100 The effect of selected compounds of the invention on MCF7 breast carcinoma cells according to the MTS assay is summarized in Table 2. IC 50 was defined as the concentration of the compound which gave rise to 50% reduction in viable cell number. TABLE 2Biological Activities of Selected Compoundsof the InventionLysateHER2MTSbindingIC 50IC 50S. NoEx #Structure(μM)(μM)(μM)18ND0.0230.1210ND0.250.63110.090.080.2450.150.0950.35130.090.051.06140.050.0381.07150.030.0150.023820ND0.0421.0921ND0.17>10.01022ND0.0651.01123ND0.13>10.01224ND0.0250.31325ND0.15>10.01446ND0.07ND1645ND0.02ND1743ND0.13ND1847ND0.45ND1948ND1.5ND2052ND0.410.02149ND0.180.9ND, not determined. The foregoing examples are not limiting and are merely illustrative of various aspects and embodiments of the present invention. All documents cited herein are indicative of the levels of skill in the art to which the invention pertains and are incorporated by reference herein in their entireties. None, however, is admitted to be prior art. One skilled in the art will readily appreciate that the present invention is well adapted to carry out the objects and obtain the ends and advantages mentioned, as well as those inherent therein. The methods and compositions described illustrate preferred embodiments, are exemplary, and are not intended as limitations on the scope of the invention. Certain modifications and other uses will occur to those skilled in the art, and are encompassed within the spirit of the invention, as defined by the scope of the claims. The invention illustratively described herein suitably may be practiced in the absence of any element or elements, limitation or limitations which is not specifically disclosed herein. The terms and expressions which have been employed are used as terms of description and not of limitation, and there is no intention in the use of such terms and expressions of excluding any equivalents of the features shown and described, or portions thereof. It is recognized that various modifications are possible within the scope of the invention claimed. Thus, it should be understood that although the present invention has been specifically disclosed by preferred embodiments, optional features, modifications and variations of the concepts herein disclosed may be resorted to by those skilled in the art, and that such modifications and variations are considered to be within the scope of this invention as defined by the description and the appended claims. In addition, where features or aspects of the invention are described in terms of Markush groups or other grouping of alternatives, e.g., genuses, those skilled in the art will recognize that the invention is also thereby described in terms of any individual member or subgroup of members of the Markush group or subgenus, and exclusions of individual members as appropriate, e.g., by proviso. Other embodiments are within the following claims.","lang":"en","source":"USPTO_FULLTEXT","data_format":"ORIGINAL"}},"description_lang":["en"],"has_description":true,"has_docdb":true,"has_inpadoc":true,"has_full_text":true,"biblio_lang":"en"},"jurisdiction":"US","collections":[],"usersTags":[],"lensId":"110-917-847-905-650","publicationKey":"US_7138402_B2","displayKey":"US 7138402 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R0 is selected from hydrogen, halogen, lower alkyl, —SR8, —OR8, —CN, and —NHR8,\n
R1 is halogen, or lower alkyl;\n
R2 is —NHR8;\n
R3 is selected from the group consisting of hydrogen, halogen, —SR8, —OR8, —CN, —C(O)R9, —C(O)OH, —NO2, —NR8R10, lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic and heterocyclic, all optionally substituted, wherein:\n\nthe aryl, heteroaryl, alicyclic and heterocyclic groups are optionally mono-, bi- or tri-cyclic,\nR8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N, and\nthe optional substituents on R3 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR8, —OR8, —CN, —C(O)OH, —C(O)R9, —NO2, —NR8R10, lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
When R0 or R3 is —OH or —SH, the compound may exist as the corresponding (thio)keto tautomer or a mixture of keto-enol tautomers;\n
R4 is —CHR12—, —C(O)—, —C(S)—, —S(O)— or —SO2—;\n
R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein\n\nthe aryl group is substituted with 3 to 5 substituents,\nthe heteroaryl group is substituted with 2 to 5 substituents,\nthe alicyclic group is substituted with 3 to 5 substituents,\nthe heterocyclic group is substituted with 3 to 5 substituents, and\nthe substituents are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR8, —OR8, —CN, —C(O)OH, —C(O)R9, —NO2, —NR8R10, lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R8 is hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R9;\n
R9 is H, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, —NR10R10, or —OR11, wherein R10 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R10 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl or lower heteroaryl;\n
R11 is lower alkyl, lower alkenyl, or lower alkynyl, lower heteroaryl or lower aryl; and\n
R12 is hydrogen or lower alkyl."],"number":1,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 1, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein each of said aryl, heteroaryl, alicyclic or heterocyclic group is monocyclic or bicyclic."],"number":2,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 1 or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein:\n
R0 is hydrogen, halogen, —SH, —OH, or —CN;\n
R1 is halogen; and\n
R2 is —NHR8, where R8 is hydrogen or —C(O)R9."],"number":3,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 1, or a polymorph, ester, tautomer, enantiomer pharmaceutically acceptable salt or prodrug thereof, wherein:\n
R1 is chloro or bromo,\n
R2 is —NHR8, where R8 is hydrogen or —C(O)R9; and\n
R3 is hydrogen, halogen, —OR8, —SR8, —NR8R10, lower alkyl, lower alkenyl, or lower alkynyl, lower perhaloalkyl, lower aryl, or lower heteroaryl."],"number":4,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 1, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein:\n
R0 is hydrogen, halogen or —CN;\n
R2 is —NHR8, where R8 is hydrogen or —C(O)R9; and\n
R4 is —CH2—."],"number":5,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 1, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein:\n
R0 is hydrogen, halogen, —SH, —OH or —CN;\n
R1 is halogen;\n
R2 is —NH2;\n
R3 is hydrogen, halogen, —OR8, —SR8, —NR8R10, lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, lower aryl, or lower heteroaryl, wherein R8 is hydrogen, lower alkyl, lower aryl, or —C(O)R9;\n
R4 is —CH2—; and\n
R5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents."],"number":6,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1 is chloro or bromo, R2 is —NH2, and R5 is a phenyl having at least three substituents."],"number":7,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1 is chloro or bromo, R2 is —NH2 and R5 is a pyridyl having at least two substituents."],"number":8,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1 is chloro or bromo, R2 is —NH2, and R5 is 1-oxy-pyridyl (N-oxy-pyridyl) having at least two substituents."],"number":9,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":10,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":11,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein the compound is a member selected from the group of compounds below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":12,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":13,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":14,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":15,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":16,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":17,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":18,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":19,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":20,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":21,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is a member selected from the group below wherein Py is pyridinyl, a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":22,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":23,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":24,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":25,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":26,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":27,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":28,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":29,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":30,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":31,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":32,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":33,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":34,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":35,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":36,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":37,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":38,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":39,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":40,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":41,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is represented by the formula below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":42,"annotation":false,"claim":true,"title":false},{"lines":["A pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and at least one compound represented by Formula I below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:\nwherein:\n
R0 is selected from hydrogen, halogen, lower alkyl, —SR8, —OR8, —CN, and —NHR8,\n
R1 is halogen, or lower alkyl;\n
R2 is —NHR8;\n
R3 is selected from the group consisting of hydrogen, halogen, —SR8, —OR8, —CN, —C(O)R9, —C(O)OH, —NO2, —NR8R10, lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic and heterocyclic, all optionally substituted, wherein:\n\nthe aryl, heteroaryl, alicyclic and heterocyclic groups are optionally mono-, bi- or tri-cyclic,\nR8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N, and\nthe optional substituents on R3 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR8, —OR8, —CN, —C(O)OH, —C(O)R9, —NO2, —NR8R10 lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
When R0 or R3 is —OH or —SH, the compound may exist as the corresponding (thio)keto tautomer or a mixture of keto-enol tautomers;\n
R4 is —CHR12—, —C(O)—, —C(S)—, —S(O)— or —SO2—;\n
R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein\n\nthe aryl group is substituted with 3 to 5 substituents,\nthe heteroaryl group is substituted with 2 to 5 substituents,\nthe alicyclic group is substituted with 3 to 5 substituents,\nthe heterocyclic group is substituted with 3 to 5 substituents, and\nthe substituents are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR8, —OR8, —CN, —C(O)OH, —C(O)R9, —NO2, —NR8R10, lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R8 is hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R9;\n
R9 is H, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, —NR10R10, or —OR11, wherein R10 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R10 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl or lower heteroaryl;\n
R11 is lower alkyl, lower alkenyl, or lower alkynyl, lower heteroaryl or lower aryl; and\n
R12 is hydrogen or lower alkyl."],"number":43,"annotation":false,"claim":true,"title":false},{"lines":["The pharmaceutical composition of claim 43, wherein:\n
R0 is hydrogen, halogen, —SH, —OH, or —CN,\n
R1 is halogen; and\n
R2 is —NHR8, where R8 is hydrogen or —C(O)R9."],"number":44,"annotation":false,"claim":true,"title":false},{"lines":["The pharmaceutical composition of claim 43, wherein:\n
R0 is hydrogen, halogen or —CN,\n
R2 is —NHR8, where R8 is hydrogen or —C(O)R9; and\n
R4 is —CH2—."],"number":45,"annotation":false,"claim":true,"title":false},{"lines":["The pharmaceutical composition of claim 43, wherein:\n
R0 is hydrogen, halogen, —SH, —OH or —CN,\n
R1 is halogen;\n
R2 is —NH2,\n
R3 is hydrogen, halogen, OR8, SR8, NR8R10, lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, lower aryl, or lower heteroaryl, wherein R8 is hydrogen, lower alkyl, lower aryl, or —C (O)R9;\n
R4 is —CH2—; and\n
R5 is aryl or heteroaryl, wherein each of the aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents."],"number":46,"annotation":false,"claim":true,"title":false},{"lines":["The pharmaceutical composition of claim 43, wherein:\n
R1 is chloro or bromo;\n
R2 is —NH2; and\n
R5 is a phenyl having at least three substituents, a pyridyl having at least two substituents, or 1-oxy-pyridyl (N-oxy-pyridyl), each of which has at least two substituents."],"number":47,"annotation":false,"claim":true,"title":false},{"lines":["A compound represented by Formula II, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:\nwherein:\n
R0 is hydrogen, halogen, lower alkyl, —SR8, —OR8, —CN or —NHR8;\n
R1 is halogen, or lower alkyl;\n
R2 is —NH2;\n
R4 is —CHR12—, —C(O)—, —C(S)—, —S(O)— or —SO2—;\n
R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein:\n\nthe aryl group is substituted with 3 to 5 substituents,\nthe heteroaryl group is substituted with 2 to 5 substituents,\nthe alicyclic group is substituted with 3 to 5 substituents,\nthe heterocyclic group is substituted with 3 to 5 substituents, and\nthe substituents on R5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR8, —OR8, —CN, —C(O)OH, —C(O)R9, —NO2, —NR8R10, lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R9;\n
R9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR10R10, or —OR11, wherein R10 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl;\n
R11 is lower alkyl, lower alkenyl, or lower alkynyl, lower heteroaryl or lower aryl;\n
R12 is hydrogen or lower alkyl; and\n
R0 and R10 taken together optionally form an exocyclic double bond which is optionally substituted, or optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N."],"number":48,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 48, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein:\n
R1 is halogen or lower alkyl;\n
R4 is —CHR12—; and\n
R5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents."],"number":49,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 49, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein\n
R0 is hydrogen or —NHR8;\n
R1 is halogen, or lower alkyl;\n
R10 is hydrogen or lower alkyl."],"number":50,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 49, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein:\n
R0 is hydrogen;\n
R1 is halogen;\n
R4 is —CH2—;\n
R5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents; and\n
R10 is hydrogen."],"number":51,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 51, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R1 is chloro or bromo; R5 is phenyl, pyridyl or 1-oxy-pyridyl (N-oxy-pyridyl), each R5 has at least two substituents."],"number":52,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 51, wherein said compound is a member selected from the group below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":53,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 51, wherein said compound is a member selected from the group below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":54,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 51, wherein said compound is a member selected from the group below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":55,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 51, wherein said compound is a member selected from the group below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:"],"number":56,"annotation":false,"claim":true,"title":false},{"lines":["A pharmaceutical composition comprising one or more pharmaceutical acceptable excipients and at least one compound represented by Formula II below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:\nwherein:\n
R0 is hydrogen, halogen, lower alkyl, —SR8, —OR8, —CN or —NHR8;\n
R1 is halogen, or lower alkyl;\n
R2 is —NH2;\n
R4 is —CHR12—, —C(O)—, —C(S)—, —S(O)— or —SO2—;\n
R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein:\n\nthe aryl group is substituted with 3 to 5 substituents,\nthe heteroaryl group is substituted with 2 to 5 substituents,\nthe alicyclic group is substituted with 3 to 5 substituents,\nthe heterocyclic group is substituted with 3 to 5 substituents, and\nthe substituents on R5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR8, —OR8, —CN, —C(O)OH, —C(O)R9, —NO2, —NR8R10, lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R9.\n
R9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR10R10, or —OR11, wherein R10 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl,\n
R11 is lower alkyl, lower alkenyl, lower alkynyl, lower heteroaryl or lower aryl;\n
R12 is hydrogen or lower alkyl; and\n
R0 and R10 taken together optionally form an exocyclic double bond which is optionally substituted, or optionally form a ring of 3–7 ring atoms and optionally 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N."],"number":57,"annotation":false,"claim":true,"title":false},{"lines":["A compound represented by Formula III, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:\nwherein:\n
R1 is halogen, or lower alkyl;\n
R2 is —NH2;\n
R3 is selected from the group consisting of hydrogen, halogen, —SR8, —OR8, —CN, —C(O)R9, —C(O)OH, —NO2, —NR8R10, lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic, heterocyclic, all optionally substituted, wherein:\n\nthe aryl, heteroaryl, alicyclic and heterocyclic groups are optionally mono-, bi- or tri-cyclic,\nR8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N, and\nthe optional substituents on R3 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR8, —OR8, —CN, —C(O)OH, —C(O)R9, —NO2, —NR8R10, lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R8 and R10 with the N to which they are attached together optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R4 is —CHR12—, —C(O)—, —C(S)—, —S(O)— or —SO2—;\n
R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein\n\nthe aryl group is substituted with 3 to 5 substituents,\nthe heteroaryl group is substituted with 2 to 5 substituents,\nthe alicyclic group is substituted with 3 to 5 substituents,\nthe heterocyclic group is substituted with 3 to 5 substituents, and\nthe substituents on R5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR8, —OR8, —CN, —C(O)OH, —C(O)R9, —NO2, —NR8R10, lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R9;\n
R9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR10R10, or —OR11, wherein R10 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl,\n
R11 is lower alkyl, lower alkenyl, lower alkynyl, lower heteroaryl or lower aryl;\n
R12 is hydrogen or lower alkyl; and\n
R3 and R10 taken together optionally form an exocyclic double bond which is optionally substituted, or optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N."],"number":58,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 58, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein:\n
R1 is halogen;\n
R3 is hydrogen, halogen, —OR8, —SR8, —NR8R10, lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, lower aryl, or lower heteroaryl, wherein R8 is hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R9;\n
R4 is —CH2—;\n
R5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents, and\n
R10 is hydrogen or lower alkyl."],"number":59,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 58, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein:\n
R1 is halogen;\n
R4 is —CH2—;\n
R5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents; and\n
R10 is hydrogen."],"number":60,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 58, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein:\n
R1 is halogen;\n
R3 is hydrogen;\n
R4 is —CH2—;\n
R5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents; and\n
R10 is hydrogen."],"number":61,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 61, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein: R1 is chloro or bromo; and R5 is phenyl, pyridyl or 1-oxy-pyridyl (N-oxy-pyridyl), wherein each R5 has at least two substituents."],"number":62,"annotation":false,"claim":true,"title":false},{"lines":["A pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and at least one compound represented by Formula III below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:\nwherein:\n
R1 is halogen, or lower alkyl;\n
R2 is —NH2;\n
R3 is selected from the group consisting of hydrogen, halogen, —SR8, —OR8—CN, —C(O)R9, —C(O)OH, —NO2, —NR8R10, lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic, heterocyclic, all optionally substituted, wherein:\n\nthe aryl, heteroaryl, alicyclic and heterocyclic groups are optionally mono-, bi- or tri-cyclic,\nR8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N, and\nthe optional substituents on R3 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR8, —OR8, —CN, —C(O)OH, —C(O)R9, —NO2, —NR8R10, lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R4 is —CHR12—, —C(O)—, —C(S)—, —S(O)— or —SO2—;\n
R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein\n\nthe aryl group is substituted with 3 to 5 substituents,\nthe heteroaryl group is substituted with 2 to 5 substituents,\nthe alicyclic group is substituted with 3 to 5 substituents,\nthe heterocyclic group is substituted with 3 to 5 substituents, and\nthe substituents on R5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR8, —OR8, —CN, —C(O)OH, —C(O)R9, —NO2 and —NR8R10 lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R9;\n
R9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR10R10, or —OR11, wherein R10 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl,\n
R11 is lower alkyl, lower alkenyl, lower alkynyl, lower heteroaryl or lower aryl;\n
R12 is hydrogen or lower alkyl; and\n
R3 and R10 taken together optionally form an exocyclic double bond which is optionally substituted, or optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N."],"number":63,"annotation":false,"claim":true,"title":false},{"lines":["A compound represented by Formula IV, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:\nwherein:\n
R1 is halogen, or lower alkyl;\n
R2 is —NH2;\n
R4 is —CHR12—, —C(O)—, —C(S)—, —S(O)— or —SO2—;\n
R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein\n\nthe aryl group is substituted with 3 to 5 substituents,\nthe heteroaryl group is substituted with 2 to 5 substituents,\nthe alicyclic group is substituted with 3 to 5 substituents,\nthe heterocyclic group is substituted with 3 to 5 substituents, and\nthe substituents on R5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR8, —OR8, —CN, —C(O)OH, —C(O)R9, —NO2, —NR8R10, lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R9;\n
R9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR10R10, or —OR11, wherein R10 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl,\n
R11 is lower alkyl, lower alkenyl, lower alkynyl, lower heteroaryl or lower aryl; and\n
R12 is hydrogen or lower alkyl."],"number":64,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 64, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein:\n
R1 is halogen;\n
R4 is —CH2—; and\n
R5 is aryl or heteroaryl, wherein each of said aryl and heteroaryl is monocyclic or bicyclic and is substituted with 3 to 5 substituents."],"number":65,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 65, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1 is chloro or bromo, R5 is phenyl, pyridyl or 1-oxy-pyridyl (N-oxy-pyridyl), wherein each R5 has at least two substituents."],"number":66,"annotation":false,"claim":true,"title":false},{"lines":["A pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and at least one compound represented by Formula IV below, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof:\nwherein:\n
R1 is halogen, or lower alkyl;\n
R2 is —NH2;\n
R4 is —CHR12—, —C(O)—, —C(S)—, —S(O)— or —SO2—;\n
R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein\n\nthe aryl group is substituted with 3 to 5 substituents,\nthe heteroaryl group is substituted with 2 to 5 substituents,\nthe alicyclic group is substituted with 3 to 5 substituents,\nthe heterocyclic group is substituted with 3 to 5 substituents, and\nthe substituents on R5 are selected from the group consisting of halogen, lower alkyl, lower alkenyl, lower alkynyl, —SR8, —OR8, —CN, —C(O)OH, —C(O)R9, —NO2 and —NR8R10 lower aryl, heteroaryl, alicyclic, lower heterocyclic, arylalkyl, heteroarylalkyl, amino, alkylamino, dialkylamino, oxo, perhaloalkyl, perhaloalkoxy, perhaloacyl, guanidinyl, pyridinyl, thiophenyl, furanyl, indolyl, and indazolyl, wherein R8 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R8 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aryl, lower heteroaryl, or —C(O)R9;\n
R9 is H, lower alkyl, lower aryl, lower heteroaryl, —NR10R10, or —OR11, wherein R10 and R10 taken together with the N to which they are attached optionally form a ring of 3–7 ring atoms and 1–3 of the ring atoms are heteroatoms selected from the group of O, S and N;\n
R10 is hydrogen, lower alkyl, lower heteroaryl, lower aryl, lower alkenyl, or lower alkynyl,\n
R11 is lower alkyl, lower alkenyl, lower alkynyl, lower heteroaryl or lower aryl; and\n
R12 is hydrogen or lower alkyl."],"number":67,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 6, wherein said compound is a member selected from the group below, or a polymorph, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof"],"number":68,"annotation":false,"claim":true,"title":false}]}},"filters":{"npl":[],"notNpl":[],"applicant":[],"notApplicant":[],"inventor":[],"notInventor":[],"owner":[],"notOwner":[],"tags":[],"dates":[],"types":[],"notTypes":[],"j":[],"notJ":[],"fj":[],"notFj":[],"classIpcr":[],"notClassIpcr":[],"classNat":[],"notClassNat":[],"classCpc":[],"notClassCpc":[],"so":[],"notSo":[],"sat":[]},"sequenceFilters":{"s":"SEQIDNO","d":"ASCENDING","p":0,"n":10,"sp":[],"si":[],"len":[],"t":[],"loc":[]}}