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1H-pyrrolo [2,3-b] pyridine derivatives and their use as kinase inhibitors
专利权人:
Vernalis (R&D) Limited
发明人:
STOKES, Stephen,GRAHAM, Christoper John,RAY, Stuart Christopher,STEFANIAK, Emma Jayne
申请号:
ES13703121
公开号:
ES2637340T3
申请日:
2013.01.30
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of formula I: ** Formula ** or a pharmaceutically acceptable salt thereof, wherein: each Z is independently (Alk) n-Rn- (Alk) nX, wherein each Alk is independently alkylene (C1 to C12) or alkenylene (C2 to C12), each of which may be optionally substituted; each n is independently 0 or 1; each R is independently optionally substituted arylene or heteroarylene, or optionally substituted cycloalkylene or heterocycle, -O-, -S-, - (C>; = O) -, - (C>; = S) -, -SO2-, -C ( >; = O) O-, -C (>; = O) NRA-, -C (>; = S) NRA-, -S02NRA-, -NRAC (>; = O) -, -NRASO2- or -NRA- where RA is hydrogen, C1-C6 alkyl, - (C1-C6 alkyl) - (cycloalkyl), (C1-C6 alkyl) - (C1-C6 alkoxy) or C1-C6 alkoxy; each X is independently halogen, -H, -ORA, NRARA, optionally substituted aryl or heteroaryl, or optionally substituted cycloalkyl or heterocycle, CN or C (halogen) aHb, where a is 1, 2 or 3, and b is (3-a ); Y is optionally substituted aryl or heteroaryl, or optionally substituted cycloalkyl or heterocycle; and R1 is H or C1-C6 alkyl, with the proviso that the compound is not N- (5-bromo-4-fluoro-1H-pyrrolo [2,3-b] pyridin-3-yl) -1- ( 4- methoxybenzyl) -1H-pyrazol-4-carboxamide or (R) -1- (5-bromo-3- (1- (4-methoxybenzyl) -1Hpirazol-4-carboxamido) -1H-pyrrolo [2,3- b] tert-butyl pyridin-4-yl) piperidin-3-ylcarbamate.Un compuesto de fórmula I: **Fórmula** o una de sus sales farmacéuticamente aceptables, en donde: cada Z es independientemente (Alk)n-Rn-(Alk)n-X, en donde cada Alk es independientemente alquileno (C1 a C12) o alquenileno (C2 a C12), cada uno de los cuales puede estar opcionalmente sustituido; cada n es independientemente 0 o 1; cada R es independientemente arileno o heteroarileno opcionalmente sustituido, o cicloalquileno o heterociclo opcionalmente sustituido, -O-, -S-, -(C>;=O)-, -(C>;=S)-, -SO2-, -C(>;=O)O-, -C(>;=O)NRA-, -C(>;=S)NRA-, -S02NRA-, -NRAC(>;=O)-, -NRASO2- o -NRA- en donde RA es hidrógeno, alquilo C1-C6 , -(alquil C1-C6)-(cicloalquil), (a
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