{"search_session":{},"preferences":{"l":"en","queryLanguage":"en"},"patentId":"174-512-600-608-431","frontPageModel":{"patentViewModel":{"ref":{"entityRefType":"PATENT","entityRefId":"174-512-600-608-431"},"entityMetadata":{"linkedIds":{"empty":true},"tags":[],"collections":[{"id":8906,"type":"PATENT","title":"Univ Pennsylvania Patent Portfolio","description":"","access":"OPEN_ACCESS","displayAvatar":true,"attested":false,"itemCount":24238,"tags":[],"user":{"id":91044780,"username":"Cambialens","firstName":"","lastName":"","created":"2015-05-04T00:55:26.000Z","displayName":"Cambialens","preferences":"{\"usage\":\"public\",\"beta\":false}","accountType":"PERSONAL","isOauthOnly":false},"notes":[{"id":8221,"type":"COLLECTION","user":{"id":91044780,"username":"Cambialens","firstName":"","lastName":"","created":"2015-05-04T00:55:26.000Z","displayName":"Cambialens","preferences":"{\"usage\":\"public\",\"beta\":false}","accountType":"PERSONAL","isOauthOnly":false},"text":"
Search applicants and owners= \"Univ Pennsylvania\", \"Pennsylvania Univ\", \"Univ Penns*\", \"Penn* Univ\", \"University of Pennsylvania\", \"Pennsylvania University\".
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Search applicants and owners= \"Univ Pennsylvania\", \"Pennsylvania Univ\", \"Univ Penns*\", \"Penn* Univ\", \"University of Pennsylvania\", \"Pennsylvania University\".
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\n\nR1-x-A1-x-y-A2-y-x-A1-x-R2 (IIa)\n\nor an acceptable salt or solvate thereof,wherein:\n
x is NR8, O, S, or —N(R8)N(R8)—; and y is C═O, C═S, or O═S═O; wherein R8 is hydrogen;\n
A1 and A2 are independently arylene or heteroarylene, wherein A1 is substituted with one or more polar (PL) groups and is optionally substituted with one or more non-polar (NPL) groups and A2 is independently optionally substituted with one or more polar (PL) group(s), one or more non-polar (NPL) group(s), or a combination of one or more polar (PL) group(s) and one or more non-polar (NPL) group(s);\n
R1 is a polar group (PL) or a non-polar group (NPL); and R2 is R1;\n
NPL is a nonpolar group independently selected from the group consisting of —B(OR4)2 and —(NR3′)q1NPL—UNPL—(CH2)pNPL—(NR3″)q2NPL—R4′, wherein:\n
R3, R3′, and R3″ are independently selected from the group consisting of hydrogen, alkyl, and alkoxy;\n
R4 and R4′ are independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, and heteroaryl, any of which is optionally substituted with one or more alkyl or halo groups;\n
UNPL is absent or selected from the group consisting of O, S, S(═O), S(═O)2, NR3, —C(═O)—, —C(═O)—N═N—NR3—, —C(═O)—NR3—N═N—, —N═N—NR3—, —C(═N—N(R3)2)—, —C(═NR3)—, —C(═O)O—, —C(═O)S—, —C(═S)—, —O—P(═O)2O—, —R3O—, —R3S—, —S—C═N— and —C(═O)—NR3—O—, wherein groups with two chemically nonequivalent termini can adopt both possible orientations;\n
the —(CH2)pNPL— alkylene chain is optionally substituted with one or more amino or hydroxy groups, or is unsaturated;\n
pNPL is 0 to 8;\n
q1NPL and q2NPL are independently 0, 1 or 2;\n
PL is a polar group selected from the group consisting of halo, hydroxyethoxymethyl, methoxyethoxymethyl, polyoxyethylene, and —(NR5′)q1PL—UPL—(CH2)pPL—(NR5′)q2PL—V, wherein:\n
R5 and R5′ are independently selected from the group consisting of hydrogen, alkyl, and alkoxy;\n
UPL is absent or selected from the group consisting of O, S, S(═O), S(═O)2, NR5, —C(═O)—, —C(═O)—N═N—NR5—, —C(═O)—NR5—N═N—, —N═N—NR5—, —C(═N—N(R5)2)—, —C(═NR5)—, —C(═O)O—, —C(═O)S—, —C(═S)—, —O—P(═O)2O—, —R5O—, —R5S—, —S—C═N— and —C(═O)—NR5—O—, wherein groups with two chemically nonequivalent termini can adopt both possible orientations;\n
V is selected from the group consisting of nitro, cyano, amino, hydroxy, alkoxy, alkylthio, alkylamino, dialkylamino, —NH(CH2)pNH2 wherein p is 1 to 4, —N(CH2CH2NH2)2, diazamino, amidino, guanidino, guanyl, semicarbazone, aryl, heterocycle and heteroaryl, any of which is optionally substituted with one or more of amino, halo, cyano, nitro, hydroxy, —NH(CH2)pNH2 wherein p is 1 to 4, —N(CH2CH2NH2)2, amidino, guanidino, guanyl, aminosulfonyl, aminoalkoxy, aminoalkylthio, lower acylamino, or benzyloxycarbonyl;\n
the —(CH2)pPL— alkylene chain is optionally substituted with one or more amino or hydroxy groups, or is unsaturated;\n
pPL is 0 to 8; and\n
q1PL and q2PL are independently 0, 1 or 2;\n
and a pharmaceutically acceptable carrier or diluent."],"number":1,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 1, wherein the facially amphiphilic oligomer is selected from the group consisting of:"],"number":2,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 1, wherein the microbial infection is a bacterial infection, a fungal infection, or a viral infection."],"number":3,"annotation":false,"title":false,"claim":true},{"lines":["A method of killing or inhibiting the growth of a microorganism, said method comprising contacting the microorganism with an effective amount of a facially amphiphilic oligomer of Formula IIa:\n
\n\nR1-x-A1-x-y-A2-y-x-A1-x-R2 (IIa)\n\nor an acceptable salt or solvate thereof,wherein:\n
x is NR8, O, S, or —N(R8)N(R8)—; and y is C═O, C═S, or O═S═O; wherein R8 is hydrogen;\n
A1 and A2 are independently arylene or heteroarylene, wherein A1 is substituted with one or more polar (PL) groups and is optionally substituted with one or more non-polar (NPL) groups and A2 is independently optionally substituted with one or more polar (PL) group(s), one or more non-polar (NPL) group(s), or a combination of one or more polar (PL) group(s) and one or more non-polar (NPL) group(s);\n
R1 is a polar group (PL) or a non-polar group (NPL); and R2 is R1;\n
NPL is a nonpolar group independently selected from the group consisting of —B(OR4)2 and —(NR3′)q1NPL—UNPL—(CH2)pNPL—(NR3″)q2NPL—R4′, wherein:\n
R3, R3′, and R3″ are independently selected from the group consisting of hydrogen, alkyl, and alkoxy;\n
R4 and R4′ are independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, and heteroaryl, any of which is optionally substituted with one or more alkyl or halo groups;\n
UNPL is absent or selected from the group consisting of O, S, S(═O), S(═O)2, NR3, —C(═O)—, —C(═O)—N═N—NR3—, —C(═O)—NR3—N═N—, —N═N—NR3—, —C(═N—N(R3)2)—, —C(═NR3)—, —C(═O)O—, —C(═O)S—, —C(═S)—, —O—P(═O)2O—, —R3O—, —R3S—, —S—C═N— and —C(═O)—NR3—O—, wherein groups with two chemically nonequivalent termini can adopt both possible orientations;\n
the —(CH2)pNPL— alkylene chain is optionally substituted with one or more amino or hydroxy groups, or is unsaturated;\n
pNPL is 0 to 8;\n
q1NPL and q2NPL are independently 0, 1 or 2;\n
PL is a polar group selected from the group consisting of halo, hydroxyethoxymethyl, methoxyethoxymethyl, polyoxyethylene, and —(NR5′)q1PL—UPL—(CH2)pPL—(NR5′)q2PL—V, wherein:\n
R5 and R5′ are independently selected from the group consisting of hydrogen, alkyl, and alkoxy;\n
UPL is absent or selected from the group consisting of O, S, S(═O), S(═O)2, NR5, —C(═O)—, —C(═O)—N═N—NR5—, —C(═O)—NR5—N═N—, —N═N—NR5—, —C(═N—N(R5)2)—, —C(═NR5)—, —C(═O)O—, —C(═O)S—, —C(═S)—, —O—P(═O)2O—, —R5O—, —R5S—, —S—C═N— and —C(═O)—NR5—O—, wherein groups with two chemically nonequivalent termini can adopt both possible orientations;\n
V is selected from the group consisting of nitro, cyano, amino, hydroxy, alkoxy, alkylthio, alkylamino, dialkylamino, —NH(CH2)pNH2 wherein p is 1 to 4, —N(CH2CH2NH2)2, diazamino, amidino, guanidino, guanyl, semicarbazone, aryl, heterocycle and heteroaryl, any of which is optionally substituted with one or more of amino, halo, cyano, nitro, hydroxy, —NH(CH2)pNH2 wherein p is 1 to 4, —N(CH2CH2NH2)2, amidino, guanidino, guanyl, aminosulfonyl, aminoalkoxy, aminoalkylthio, lower acylamino, or benzyloxycarbonyl;\n
the —(CH2)pPL— alkylene chain is optionally substituted with one or more amino or hydroxy groups, or is unsaturated;\n
pPL is 0 to 8; and\n
q1PL and q2PL are independently 0, 1 or 2;\n
and a pharmaceutically acceptable carrier or diluent."],"number":4,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 4, wherein the microorganism is a bacterial cell, a fungus, or a virus."],"number":5,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 1, said method comprising administering to the animal an effective amount of a pharmaceutical composition comprising a facially amphiphilic oligomer of Formula IIa, wherein x is NR8, y is C═O, and R8 is hydrogen."],"number":6,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 6, said method comprising administering to the animal an effective amount of a pharmaceutical composition comprising a facially amphiphilic oligomer of Formula IIa, wherein A1 is o-, m-, or p-phenylene and A2 is optionally substituted heteroarylene."],"number":7,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 7, said method comprising administering to the animal an effective amount of a pharmaceutical composition comprising a facially amphiphilic oligomer of Formula IIa, wherein A1 is m-phenylene and A2 is optionally substituted pyrimidinylene."],"number":8,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 8, said method comprising administering to the animal an effective amount of a pharmaceutical composition comprising a facially amphiphilic oligomer of Formula IIa, wherein A1 is substituted with one polar group (PL) and one nonpolar group (NPL)."],"number":9,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 8, said method comprising administering to the animal an effective amount of a pharmaceutical composition comprising a facially amphiphilic oligomer of Formula IIa, wherein A2 is unsubstituted."],"number":10,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 1, said method comprising administering to the animal an effective amount of a pharmaceutical composition comprising a facially amphiphilic oligomer of Formula IIa, wherein R1 is a polar (PL) group and R2 is R1."],"number":11,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 11, said method comprising administering to the animal an effective amount of a pharmaceutical composition comprising a facially amphiphilic oligomer of Formula IIa, wherein R1 is a polar (PL) group and R2 is R1, wherein:\n
PL is —(NR5′)q1pL—UPL—(CH2)pPL—(NR5′)q2PL—V; wherein\n\nq1PL is 0;\nUPL is —C(═O)—;\npPL is 2 to 4;\nq2PL is 0; and\nV is guanidino; and\n
R5′ is as defined in claim 1."],"number":12,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 1, said method comprising administering to the animal an effective amount of a pharmaceutical composition comprising a facially amphiphilic oligomer of Formula IIa, wherein:\n
NPL is —(NR3′)q1NPL—UNPL—(CH2)pNPL—(NR3″)q2NPL—R4′, wherein:\n"],"number":13,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 13, said method comprising administering to the animal an effective amount of a pharmaceutical composition comprising a facially amphiphilic oligomer of Formula IIa, wherein NPL is —(NR3′)q1NPL—UNPL—(CH2)pNPL—(NR3″)q2NPL—R4′, wherein:\nq1NPL is 0;\nUNPL is absent;\npNPL is 0, 1, or 2;\nq2NPL is 0; and\nR4′ is C1-C10 alkyl or C3-C18 branched alkyl, any of which are optionally substituted with one or more halo groups.\n
q1NPL is 0;\n
UNPL is absent;\n
pNPL is 0;\n
q2NPL is 0;\n
and R4′ is C1-C10 alkyl or C3-C18 branched alkyl, any of which are optionally substituted with one or more halo groups."],"number":14,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 14, said method comprising administering to the animal an effective amount of a pharmaceutical composition comprising a facially amphiphilic oligomer of Formula IIa, wherein NPL is tert-butyl."],"number":15,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 1, said method comprising administering to the animal an effective amount of a pharmaceutical composition comprising a facially amphiphilic oligomer of Formula IIa, wherein:\n
PL is —(NR5′)q1PL—UPL—(CH2)pPL—(NR5′)q2pL—V, wherein:\n"],"number":16,"annotation":false,"title":false,"claim":true},{"lines":["A method of treating a microbial infection in an animal in need thereof, said method comprising administering to the animal an effective amount of a pharmaceutical composition comprising a facially amphiphilic oligomer of Formula IIa:\nq1PL is 0;\nUPL is O or S;\npPL is 0 to 4;\nq2PL is 0; and\nV is amino, guanidino, or heterocycle.\n
\n\nR1-x-A1-x-y-A2-y-x-A1-x-R2 (IIa)\n\nor an acceptable salt or solvate thereof,wherein:\n
x is NR8; y is C═O; R8 is hydrogen;\n
A1 is m-phenylene and A2 is pyrimidinylene, wherein A1 is substituted with one polar (PL) group and one non-polar (NPL) group and A2 is unsubstituted; wherein\n"],"number":17,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 1, said method comprising administering to the animal an effective amount of a pharmaceutical composition comprising a facially amphiphilic oligomer of Formula IIa, wherein said pharmaceutical composition is administered by a route chosen from systemic, topical or oral."],"number":18,"annotation":false,"title":false,"claim":true},{"lines":["The method of claim 18, said method comprising administering to the animal an effective amount of a pharmaceutical composition comprising a facially amphiphilic oligomer of Formula IIa, wherein said pharmaceutical composition is administered by a route chosen from parenteral, subcutaneous, intravenous, intramuscular, intraperitoneal, transdermal, oral, buccal, ocular, intravaginally, inhalation, depot injection, and implant."],"number":19,"annotation":false,"title":false,"claim":true}]}},"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":[]}}PL is —(NR5′)q1pL—UPL—(CH2)pPL—(NR5′)q2PL—V, wherein:\n\nq1PL is 0;\nUPL is O or S;\npPL is 0 to 4;\nq2PL is 0; and\nV is amino, guanidino, or heterocycle;\nNPL is —(NR3′)q1PL—UNPL—(CH2)pNPL—(NR3″)q2NPL—R4′, wherein:\n\nq1NPL is 0;\nUNPL is absent;\npNPL is 0;\nq2NPL is 0; and\nR4′ is C1-C10 alkyl or C3-C18 branched alkyl, any of which are optionally substituted with one or more halo groups;\nR1 is —(NR5′)q1PL—UPL—(CH2)pPL—(NR5′)q2PL—V, wherein q1PL is 0; UPL is —C(═O)—; pPL is 2 to 4; q2PL is 0; and V is guanidino;\nand R2 is R1.\n