{"search_session":{},"preferences":{"l":"zh","queryLanguage":"zh"},"patentId":"EP_1949896_A2","frontPageModel":{"patentViewModel":{"ref":{"entityRefId":"077-571-828-114-757","entityRefType":"PATENT"},"entityMetadata":{"linkedIds":{"empty":true},"tags":[],"collections":[{"id":10731,"type":"PATENT","title":"The University of North Carolina at Chapel Hill - Patent Portfolio","description":"","access":"OPEN_ACCESS","displayAvatar":true,"attested":false,"itemCount":8887,"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":8232,"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 separately:\"uni* north caro*\". Select more for logical variants. Add to collection. Select all patents in the collection and expand by simple families. Add to collection. Total patents: 1000
Search Applicants and Owners separately:\"uni* north caro*\". Select more for logical variants. Add to collection. Select all patents in the collection and expand by simple families. Add to collection. Total patents: 1000
p and q are each independently an integer from 0 to 8;
Ar1 and Ar3 are independently selected from the group consisting of:wherein:
each A, D, E, G, Y, and Z is independently selected from the group consisting of N and CR4, wherein R4 is selected from the group consisting of H, hydroxyl, halo, nitro, alkyl, substituted alkyl, alkoxyl, aryl, substituted aryl, and aryloxyl;
X is selected from the group consisting of O, S, NH, and Se;
each m is independently an integer from 0 to 4;
each s is independently an integer from 0 to 2;
each R1, R2, R3, and R21 is independently selected from the group consisting of H, hydroxyl, halo, nitro, alkyl, substituted alkyl, alkoxyl, aryl, substituted aryl, and aryloxyl;Ar2 is selected from the group consisting of: and wherein:
A1, A2, A3, A4, A5, E1, E2, G1, G2, Y1, Y2, Y3, Y4, Y5, Z1, Z2, and Z3 are independently selected from the group consisting of N and CR7, wherein R7 is selected from the group consisting of H, hydroxyl, halo, nitro, alkyl, substituted alkyl, alkoxyl, aryl, substituted aryl, and aryloxyl;
n is an integer from 0 to 4;
t is an integer from 0 to 6;
each R5, R6, R8, R9, R10, R22, R23, R24, and R25 is independently selected from the group consisting of H, hydroxyl, halo, nitro, alkyl, substituted alkyl, alkoxyl, aryl, substituted aryl, aryloxyl; andL1 and L2 are independently selected from the group consisting of: wherein:
R11, R12, R13, R14, R15, and R20 are each independently selected from the group consisting of H, alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, aralkyl, hydroxyl, alkoxyl, hydroxyalkyl, hydroxycycloalkyl, alkoxycycloalkyl, aminoalkyl, acyloxyl, alkylaminoalkyl, and alkoxycarbonyl; or
R11 and R12 together represent a C2 to C10 alkyl, C2 to C10 hydroxyalkyl, or a C2 to C10 alkylene; or
R11 and R12 together are: wherein u is an integer from 1 to 4, and R16 is H or -CONHR17NR18R19 , wherein R17 is alkyl, and R18 and R19 are each independently selected from the group consisting of H and alkyl;or a pharmaceutically acceptable salt thereof."],"number":1,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 1, wherein at least one of Ar1 and Ar3 is at least one of A, D, E, G, Y, or Z is nitrogen; and at least one of L1 or L2 is ortho to the at least one nitrogen A, D, E, G, Y, or Z."],"number":2,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 2, wherein:
Ar1 and Ar3 are each:
Ar2 is: andthe compound of Formula (I) has a structure of Formula (IIe): optionally wherein the compound is selected from the group consisting of: and"],"number":3,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 2, wherein:
Ar1 is:
Ar2 is:
Ar3 is: andthe compound of Formula (I) has a structure of Formula (IIf): optionally wherein the compound is"],"number":4,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 2, wherein:
Ar1 is:
Ar2 is:
Ar3 is :and the compound of Formula (I) has a structure of Formula (IIg): optionally wherein the compound is"],"number":5,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 2, wherein:
Ar1 is:
Ar2 is:
Ar3 is:and the compound of Formula (I) has a structure of Formula (IIh): optionally wherein the compound is selected from the group consisting of: and"],"number":6,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 2, wherein:
Ar1 is:
Ar2 is:
Ar3 is: andthe compound of Formula (I) has a structure of Formula (IIIa-4): optionally wherein the compound is selected from the group consisting of: and"],"number":7,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 2, wherein:
Ar1 is:
Ar2 is
Ar3 is: andthe compound of Formula (I) has a structure of Formula (IIIa-5): optionally wherein the compound has the structure:"],"number":8,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 2, wherein:
Ar1 is:
Ar2 is:
Ar3 is: andthe compound of Formula (I) has a structure of Formula (IIIc-2): optionally wherein the compound has the structure:"],"number":9,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 1, wherein:
Ar1 is:
Ar2 is:
Ar3 is: andthe compound of Formula (I) has a structure of Formula (IIi): optionally wherein the compound of Formula (IIi) has the structure:"],"number":10,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 1, wherein:
Ar1 is:
Ar2 is:
Ar3 is: andthe compound of Formula (I) has a structure of Formula (IIIa-3): optionally wherein the compound of Formula (IIIa-3) has the structure:"],"number":11,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 1, wherein:
Ar1 and Ar3 are each:
Ar2 is: andthe compound of Formula (I) has a structure of Formula (IIIe): optionally wherein the compound of Formula (IIIe) has the structure:"],"number":12,"annotation":false,"claim":true,"title":false},{"lines":["A pharmaceutical formulation comprising:
(a) an aza teraryl compound of claim 1; and
(b) a pharmaceutically acceptable carrier."],"number":13,"annotation":false,"claim":true,"title":false},{"lines":["An effective amount of an aza teraryl compound of Formula (I): L1-Ar1-(CH2)p-Ar2-(CH2)q-Ar3-L2 (I) wherein:
p and q are each independently an integer from 0 to 8;
Ar1 and Ar3 are independently selected from the group consisting of:wherein:
each A, D, E, G, Y, and Z is independently selected from the group consisting of N and CR4, wherein R4 is selected from the group consisting of H, hydroxyl, halo, nitro, alkyl, substituted alkyl, alkoxyl, aryl, substituted aryl, and aryloxyl;
X is selected from the group consisting of O, S, NH, and Se;
each m is independently an integer from 0 to 4;
each s is independently an integer from 0 to 2;
each R1, R2, R3, and R21 is independently selected from the group consisting of H, hydroxyl, halo, nitro, alkyl, substituted alkyl, alkoxyl, aryl, substituted aryl, and aryloxyl;Ar2 is selected from the group consisting of: and wherein:
A1, A2, A3, A4, A5, E1, E2, G1, G2, Y1, Y2, Y3, Y4, Y5, Z1, Z2, and Z3 are independently selected from the group consisting of N and CR7, wherein R7 is selected from the group consisting of H, hydroxyl, halo, nitro, alkyl, substituted alkyl, alkoxyl, aryl, substituted aryl, and aryloxyl;
n is an integer from 0 to 4;
t is an integer from 0 to 6;
each R5, R6, R8, R9, R10, R22, R23, R24, and R25 is independently selected from the group consisting of H, hydroxyl, halo, nitro, alkyl, substituted alkyl, alkoxyl, aryl, substituted aryl, aryloxyl; andL1 and L2 are independently selected from the group consisting of: wherein:
R11, R12, R13, R14, R15, and R20 are each independently selected from the group consisting of H, alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, aralkyl, hydroxyl, alkoxyl, hydroxyalkyl, hydroxycycloalkyl, alkoxycycloalkyl, aminoalkyl, acyloxyl, alkylaminoalkyl, and alkoxycarbonyl; or
R11 and R12 together represent a C2 to C10 alkyl, C2 to C10 hydroxyalkyl, or a C2 to C10 alkylene; or
R11 and R12 together are: wherein u is an integer from 1 to 4, and R16 is H or -CONHR17NR18R19 , wherein R17 is alkyl, and R18 and R19 are each independently selected from the group consisting of H and alkyl;or a pharmaceutically acceptable salt thereof, for use in a method of treating a microbial infection in a subject in need of treatment thereof, by administering to the subject said effective amount of said compound."],"number":14,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 14, wherein the microbial infection is selected from the group consisting of a Trypanosoma brucei rhodesiense infection, a Plasmodium falciparum infection, and a Leishmania donovoni infection."],"number":15,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 14, wherein at least one of Ar1 and Ar3 is at least one of A, D, E, G, Y, or Z is nitrogen; and at least one of L1 or L2 is ortho to the at least one nitrogen A, D, E, G, Y, or Z."],"number":16,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 16, wherein:
Ar1 and Ar3 are each:
Ar2 is: andthe compound of Formula (I) has a structure of Formula (IIe): optionally wherein the compound is selected from the group consisting of: and"],"number":17,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 16, wherein:
Ar1 is:
Ar2 is:
Ar3 is: andthe compound of Formula (I) has a structure of Formula (IIf): optionally wherein the compound is"],"number":18,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 16, wherein:
Ar1 is:
Ar2 is:
Ar3 is: andthe compound of Formula (I) has a structure of Formula (IIg): optionally wherein the compound is"],"number":19,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 16, wherein:
Ar1 is:
Ar2 is:
Ar3 is: andthe compound of Formula (I) has a structure of Formula (IIh): optionally wherein the compound is selected from the group consisting of: and"],"number":20,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 16, wherein:
Ar1 is:
Ar2 is:
Ar3 is: andthe compound of Formula (I) has a structure of Formula (IIIa-4): optionally wherein the compound is selected from the group consisting of: and"],"number":21,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 16, wherein:
Ar1 is:
Ar2 is
Ar3 is: andthe compound of Formula (I) has a structure of Formula (IIIa-5): optionally wherein the compound has the structure:"],"number":22,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 16, wherein:
Ar1 is:
Ar2 is:
Ar3 is: andthe compound of Formula (I) has a structure of Formula (IIIc-2): optionally wherein the compound has the structure:"],"number":23,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 14, wherein:
Ar1 is:
Ar2 is:
Ar3 is: andthe compound of Formula (I) has a structure of Formula (IIi): optionally wherein the compound of Formula (IIi) has the structure:"],"number":24,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 14, wherein:
Ar1 is:
Ar2 is:
Ar3 is: andthe compound of Formula (I) has a structure of Formula (IIIa-3): optionally wherein the compound of Formula (IIIa-3) has the structure:"],"number":25,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 14, wherein:
Ar1 and Ar3 are each:
Ar2 is: andthe compound of Formula (I) has a structure of Formula (IIIe): optionally wherein the compound of Formula (IIIe) has the structure:"],"number":26,"annotation":false,"claim":true,"title":false},{"lines":["An effective amount of an aza teraryl compound, wherein the compound is has a structure selected from the group consisting of Formula (IIe) and Formula (IIh): and wherein:
p and q are each independently an integer from 0 to 8;
m is an integer from 0 to 4;
n is an integer from 0 to 4;
each Z, A, and Y is independently selected from the group consisting of N and CR4, wherein R4 is selected from the group consisting of H, hydroxyl, halo, nitro, alkyl, substituted alkyl, alkoxyl, aryl, substituted aryl, and aryloxyl;
each R1, R2 and R5 is independently selected from the group consisting of H, hydroxyl, halo, nitro, alkyl, substituted alkyl, alkoxyl, aryl, substituted aryl, and aryloxyl; and
L1 and L2 are independently selected from the group consisting of: wherein:for use in a method of treating an infection caused by a Leishmania species in a subject in need of treatment thereof by administering to the subject said effective amount of said compound."],"number":27,"annotation":false,"claim":true,"title":false},{"lines":["The compound of claim 27, wherein the compound is selected from the group consisting of: and or wherein the Leishmania species is Leishmania donovani, or wherein the Leishmania species is Leishmania mexicana amazonensis."],"number":28,"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":[]}}R11, R12, R13, R14, R15, and R20 are each independently selected from the group consisting of H, alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, aralkyl, hydroxyl, alkoxyl, hydroxyalkyl, hydroxycycloalkyl, alkoxycycloalkyl, aminoalkyl, acyloxyl, alkylaminoalkyl, and alkoxycarbonyl; orR11 and R12 together represent a C2 to C10 alkyl, C2 to C10 hydroxyalkyl, or a C2 to C10 alkylene; orR11 and R12 together are: wherein u is an integer from 1 to 4, and R16 is H or -CONHR17NR18R19 , wherein R17 is alkyl, and R18 and R19 are each independently selected from the group consisting of H and alkyl; ora pharmaceutically acceptable salt thereof,