LELAIS, GERALD,EPPLE, ROBERT,MARSILJE III, THOMAS H.,MICHELLYS, PIERRE-YVES,MCNEILL, MATTHEW H.,LONG, YUN,LU, WENSHUO,CHEN, BEI,BURSULAYA, BADRY,JIANG, SONGCHUN
申请号:
PE0023772014
公开号:
PE07262015A1
申请日:
2013.06.05
申请国别(地区):
PE
年份:
2015
代理人:
摘要:
The Invention provides compounds of Formula 2, where the values of the sutituyentes are described in the statement of Claim) and Pharmaceutical compositions thereof, which are useful for modulating the activity of EGFR, as well as methods for using such compounds to treat, improve Or prevent a condition associated with abnormal activity or deregulated EGFR.Where The Compound selected among others: N - {7 - chlorine - 1 - [1 - [4 - (pyrrolidin-1-yl) but enoil] - 2 - Azepan - 3 - yl] - 1H - 1.3 - benzodiazol IL - 2 - 4 - carboxamide metilpiridin} - n {- 7 - chlorine - 1 - [(3R) - 1 - [4 - (3 - fluoroazetidin - il - 1 and - 2 - enoil Azepan] - 3 - yl] - 1H - 1.3 - benzodiazol - il - 2} - 2 - 4 - metilpiridin - carboxamide (R(e) - N - (7-chloro-1 - (1 - (4 - (dimethylamino) - 2 - Azepan but enoil) - 3 - yl) - 1H benzo [d] imidazole - 2 (IL - 2 - metilisonicotinamida), (R, e) - N - (7 - chlorine - 1 - (1 - (4 - (dimethylamino) - 2 - Azepan but enoil) - 3 - yl) - 1H benzo [d] imidazole - 2 - yl) - 2.6 - dimetilisonicotinamida (R, e) - N - (1 - (1 - (4 - (dimethylamino) - 2. - enoil) Azepan - 3 - il - 7 - methyl) - 1H - Ben Zo [d] imidazole - 2 - il) - 2 - (trifluoromethyl) isonicotinamide,(R) - N - (1 - (1 - acriloilazepan - 3 - 7 - chlorine - il) - 6 - (2 - (pyrrolidin-1-yl) ethoxy) - 1H benzo [d] imidazole - 2 - yl) - 2.6 - dimetilisonicotinamida, (R, e) - N - (7-chloro-1 - (1 - (4 - (methylamino) but Azepan - 2 - 3 - enoil) - yl) - 1H benzo [d] imidazole - 2 (IL - 2 metilisonicotinamida).La invencion proporciona compuestos (de formula 2, donde los valores de los sutituyentes estan descritos en el pliego de reivindicaciones) y composiciones farmaceuticas de los mismos, que son utiles para modular la actividad de EGFR, asi como metodos para usar tales compuestos para tratar, mejorar o prevenir una afeccion asociada con la actividad anormal o desregulada del EGFR. Donde dicho compuesto se selecciona entre otros de : N-{7-cloro-1-[1-[4-(pirrolidin-1-il)but-2-enoil]azepan-3