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2H-1,2,3-Triazole derivatives as fibrosis inhibitors
专利权人:
The Scripps Research Institute
发明人:
LAIRSON, Luke,BOLLONG, Michael,SCHULTZ, Peter G.,CHATTERJEE, Arnab K.,YANG, Baiyuan,KUMAR, Puneet,URKALAN, Kaveri
申请号:
ES14807059
公开号:
ES2755125T3
申请日:
2014.06.05
申请国别(地区):
ES
年份:
2020
代理人:
摘要:
A compound of Formula (II), or a pharmaceutically acceptable salt, solvate, polymorph, N-oxide, or stereoisomer thereof: ** Formula ** wherein: A1 is ** Formula ** A2 is ** Formula ** pyridine , pyrazine, pyrimidine, pyridazine or triazine; ** Formula ** B is ** Formula ** C is ** Formula ** D is ** Formula ** E is aryl, heteroaryl, carbocyclyl, heterocyclyl or alkyl; each R1, R2, R3 and R4 is independently selected from H, alkyl, haloalkyl or alkoxy; R7 is alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, -alkylene (NR13R14), cycloalkyl, heterocyclyl, -alkylene (cycloalkyl), or -alkylene (heterocyclyl); each R8 is independently selected from alkyl, cycloalkyl, heterocyclyl, halo, hydroxy, nitrile, azido, nitro, alkoxy, haloalkoxy, haloalkyl, hydroxyalkyl, alkoxyalkyl, -alkylene (NR13R14), -alkylene (cycloalkyl), -alkylene (heterocyclyl), aryl, heteroaryl, -SR13, -SOR13, -SO2R13, -SO2NR13R14, -NR13R14, -NR13SO2R14, - NR13C (O) R14, -NR13C (O) OR14, -NR13C (O) NR13R14, -C (O) R14, -C (O) OR14 and -C (O) NR13R14; or two adjacent R8s form a heterocyclyl ring; each R13 and R14 is independently selected from H, alkyl, cycloalkyl, heterocyclylalkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, arylalkyl, heteroarylalkyl, aryl and heteroaryl; or R13 and R14 taken together form a heterocycle with the atoms to which they are attached; Y1 and Y2 are O; n is 1, 2 or 3; m is 1 or 2; p is 1, 2, 3 or 4; s is 0, 1, 2, 3 or 4; t is 0, 1, 2, 3 or 4; u is 0, 1, 2, 3, 4 or 5; and v is 0; where "alkyl" refers to a linear or branched hydrocarbon chain radical, having from one to thirty carbon atoms, and attached to the rest of the molecule by a single bond; "alkylene" refers to a straight or branched divalent hydrocarbon chain, as described for alkyl; "alkoxy" refers to a radical of the formula -ORa where Ra is an alkyl radical as defined above; "aryl" refers to a radical derived from a hydrocarbon ring system comprising hydrogen, from 6 to 30 carbon atoms and at least one aromatic ring; "cycloalky
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