МЕРК ШАРП И ДОУМ КОРП. (US);ЛАЙСЕРА КОРПОРЕЙШН (US)
发明人:
АЙКЕР Томас (US),БАРР Кеннет (US),СИМОВ Владимир (US),ТОМАС Уилльям (US),ТУГУД Питер (US),ВАН ХЕЙС Чад (US)
申请号:
RU2014149149
公开号:
RU2014149149A
申请日:
2013.05.03
申请国别(地区):
RU
年份:
2016
代理人:
摘要:
1. The compound represented by formula I: or a pharmaceutically acceptable salt or solvate thereof; where: A represents aryl, aralkyl, heteroaryl, cycloalkyl or heterocycloalkyl; each of which is optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of halogen, hydroxyl, C1-6alkyl, haloalkyl, C-Chydroxyalkyl, Calkoxy, C haloalkoxy, -N (R) (R), -COR, -C (O ) R, -CN, -Calkylene-Calkoxy, -Calkylene-N (R) (R), -Calkylene-COR, -O-Calkylene-N (R) (R), -N (R) C (O) - Calkylene-N (R) (R), -S (O) Calkyl, -SON (R) (R), -N (R) SO (Calkyl), -C (O) N (R) (R) and - N (R) C (O) N (R) (R); X is —O— [C (R) (R)] - [C (R)] - Ψ, —OC (R) —C (R ) (R) -C (R) -Ψ, -OC (R) -C (R) (R) -Ψ, -C (R) - [C (R) (R)] - [C (R)] -Ψ, -C (O) - [C (R) (R)] - [C (R)] - Ψ or -C (R) -N (R) - [C (R) (R)] - [ C (R)] - Ψ; where Ψ represents a bond with a ring carbon atom containing sulfonyl in Formula I; Y and Y each independently represent C (R) or N; R represents, independently for each case, hydrogen or C1-6 alkyl; R represents-C (O ) -aryl, -C (O) -aralkyl, -C (O) - [C (R)] - cycloalkyl, -C (O) - [C (R)] - heterocyclyl, -C (O) -Calkyl, -C (O) -Calkylene-alkoxyl, -C (O) -Calkylene-cycloalkyl or C (O) -Calkylene-heterocycloalkyl; each of which is optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of halogen, hydroxyl, C 1 alkoxy, C 1 haloalkoxy, C 1-6 alkyl, C 1 haloalkyl, -N (R) (R), -CN, -CO-C 1-6 alkyl, -C ( O) -Calkyl, -C (O) N (R) (R), -S (O) C1-6alkyl, -SON (R) (R) and -N (R) SO (C1-6alkyl); R is independently for each hydrogen, halogen or C 1-6 alkyl; R and R 2 each represent, independently for each case, hydrogen or C 1-6 alkyl; or R and R, taken together with the nitrogen atom to which they are bonded, form a 3-7 membered heterocyclic ring; R represents, independently for each case, hydrogen or C 1-6 alkyl; R 1 represents hydrogen, hydroxyl, C hydroxyalkyl, C 1-6 alkyl, C 1 haloalkyl, -COR , Calkylene-COR,