МЕРК ШАРП И ДОУМ КОРП. (US);ЛАЙСЕРА КОРПОРЕЙШН (US)
发明人:
АЙКЕР Томас (US),БАРР Кеннет (US),ЛАПОЙНТ Блэйр (US),СИМОВ Владимир (US),СТЕЙН Карин (US),ТОМАС Уилльям (US),ТУГУД Питер (US),ВАН ХЕЙС Чад (US),УАЙТ Кэтрин (US)
申请号：
RU2014149136
公开号：
RU2014149136A
申请日:
2013.05.07
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； wherein A is 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, hydroxyalkyl, alkoxy, haloalkoxy, —N (R) (R), —COR, —C (O) R , -CN, -Calkylene-Salkoxy, -Calkylene-N (R) (R), -Calkylene-COR, -O-Calkylene-N (R) (R), -N (R) C (O) -Calkylene- N (R) (R), -S (O) C1-6alkyl, -SON (R) (R), -N (R) SO (C1-6alkyl), -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, -C (R) -N (R) - [C (R) (R)] - [C ( R)] - Ψ, -C (R) = N-Ψ, -C (R) C (R) = N-Ψ, -N = C (R) -Ψ or -N = C (R) C (R ) -Ψ, where Ψ represents a bond with the nitrogen atom of the sulfonamide ring and in formula I； Y and Y, each independently, are C (R) or N, provided that at least one of Y and Y is N； R is hydrogen or C 1-6 alkyl； R is hydrogen, -C (O) - aryl, —C (O) aralkyl, —C (O) - [C (R)] - cycloalkyl, —C (O) - [C (R)] - heterocyclyl, —C (O) —Calkyl, —C (O) -Calkylene-Salkoxyl, -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, alkoxy, haloalkoxy, C1-6alkyl, haloalkyl, —N (R) (R), —CN, —CO — C1-6alkyl, —C ( O) -Calkyl, -C (O) N (R) (R), -S (O) Calkyl, SON (R) (R) and -N (R) SO (Calkyl)； R is independently for each case , hydrogen, halogen or C 1-6 alkyl； R 1 and R 1 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 C1-6alkyl； R2 represents hydrogen, hydroxyl,
