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3-Oxo-2,3-dihydro-1H-indazol-4-carboxamide derivatives as PARP-1 inhibitors

机译:3-Oxo-2,3-dihydro-1H-吲唑-4-羧酰胺衍生物作为PARP-1抑制剂

摘要

A compound of formula (I): ** Formula ** wherein R1 is an optionally substituted group selected from C3-C7 cycloalkyl, heterocyclyl, aryl and heteroaryl; R2 is hydrogen, COR4 or an optionally substituted group selected from linear or branched C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, heterocyclyl, aryl and heteroaryl; R3 is hydrogen, halogen, cyano, nitro, NHCOR4, COR4, NR5R6, NR5COR4, OR7, SR7, SOR10, SO2R10, NHSOR10, NHSO2R10, or an optionally substituted group selected from linear or branched C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, heterocyclyl, aryl, heteroaryl, R8R9NC1-C6 alkyl and R8O-C1-C6 alkyl; R4 is hydrogen, NR5R7, OR7, SR7, or an optionally substituted group selected from linear or branched C1-C6 alkyl, C3-C7 cycloalkyl, heterocyclyl, aryl, heteroaryl, R8R9N-C1-C6 alkyl and R8O-C1-C6 alkyl; R5 and R6 are independently hydrogen, or an optionally substituted group selected from linear or branched C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, heterocyclyl, aryl, heteroaryl, R8R9N-C1-C6 alkyl and R8O-C1-C6 alkyl, or R5 and R6 taken together with the nitrogen to which they are attached, form an optionally substituted heterocyclyl group; R7 is hydrogen, COR5, SOR10, SO2R10 or an optionally substituted group selected from linear or branched C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, heterocyclyl, aryl, heteroaryl, R8R9N-C1-C6 alkyl , R8O-C1-C6 alkyl, heterocyclyl-C1-C6 alkyl, aryl-C1-C6 alkyl and heteroaryl-C1-C6 alkyl, where R5 is as defined above; R8 and R9 are independently hydrogen, COR4 or an optionally substituted group selected from linear or branched C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, heterocyclyl, aryl and heteroaryl, or R8 and R9, taken together with the nitrogen to which they are attached, they form an optionally substituted heterocyclyl group, where R 4 is as defined above; R10 is hydrogen, NR5R6, OR7 or an optionally substituted group selected from linear or branched C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, heterocyclyl, aryl, heteroaryl, R8R9NC1-C6 alkyl, R8O alkyl -C1-C6, where R5, R6, R7, R8 and R9 are as defined above; or a pharmaceutically acceptable salt thereof.
机译:式(I)化合物:**式**其中R 1为选自C 3 -C 7环烷基,杂环基,芳基和杂芳基的任选取代的基团; R2是氢,COR4或选自直链或支链C1-C6烷基,C2-C6烯基,C2-C6炔基,C3-C7环烷基,杂环基,芳基和杂芳基的任选取代的基团; R3是氢,卤素,氰基,硝基,NHCOR4,COR4,NR5R6,NR5COR4,OR7,SR7,SOR10,SO2R10,NHSOR10,NHSO2R10或选自直链或支链C1-C6烷基,C2-C6烯基的任选取代的基团, C2-C6炔基,C3-C7环烷基,杂环基,芳基,杂芳基,R8R9NC1-C6烷基和R8O-C1-C6烷基; R4是氢,NR5R7,OR7,SR7或选自直链或支链C1-C6烷基,C3-C7环烷基,杂环基,芳基,杂芳基,R8R9N-C1-C6烷基和R8O-C1-C6烷基的任选取代的基团; R 5和R 6独立地是氢,或选自直链或支链C 1 -C 6烷基,C 2 -C 6烯基,C 2 -C 6炔基,C 3 -C 7环烷基,杂环基,芳基,杂芳基,R 8 R 9 N-C 1 -C 6烷基和R 8 O-C 1 -C 6烷基,或R 5和R 6与它们所连接的氮一起形成任选取代的杂环基; R7是氢,COR5,SOR10,SO2R10或选自直链或支链C1-C6烷基,C2-C6烯基,C2-C6炔基,C3-C7环烷基,杂环基,芳基,杂芳基,R8R9N-C1-C6的任选取代的基团烷基,R 8 O-C 1 -C 6烷基,杂环基-C 1 -C 6烷基,芳基-C 1 -C 6烷基和杂芳基-C 1 -C 6烷基,其中R 5如上所定义; R 8和R 9独立地是氢,COR 4或选自直链或支链C 1 -C 6烷基,C 2 -C 6烯基,C 2 -C 6炔基,C 3 -C 7环烷基,杂环基,芳基和杂芳基的任选取代的基团,或R 8和R 9它们与它们所连接的氮一起形成任选取代的杂环基,其中R 4如上所定义; R 10是氢,NR 5 R 6,OR 7或选自直链或支链C 1 -C 6烷基,C 2 -C 6烯基,C 2 -C 6炔基,C 3 -C 7环烷基,杂环基,芳基,杂芳基,R 8 R 9NC 1 -C 6烷基,R 8 O烷基的任选取代的基团-C1-C6,其中R5,R6,R7,R8和R9如上所定义;或其药学上可接受的盐。

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