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AZABENZENESIAZOLES, COMPOSITIONS AND METHODS OF APPLICATION
专利权人:
Ф. ХОФФМАНН-ЛЯ РОШ АГ (CH)
发明人:
БЛЕНЧ Тоби (GB),ЭЛЛВУД Чарльз (GB),ГУДАКР Саймон (GB),ЛАЙ Инцзе (US),ЛЯН Цзюнь (US),МАКЛЕОД Калум (GB),МАГНУСОН Стивен (US),ЦУИ Вики (US),УИЛЛЬЯМС Карен (GB),ЧЖАН Бижун (US)
申请号:
RU2013114352/04
公开号:
RU2013114352A
申请日:
2011.09.14
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
1. The compound of formula I: its stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts, where: A is CR or N; X is CR or N; R is independently hydrogen, halogen, C-C1-6 alkyl, C-C1-6 alkenyl, C- C1-6alkynyl, C1-6 cycloalkyl, -CF, -OR, -SR, -OCF, -CN, -NO, -C (O) R, -C (O) OR, -C (O) NRR, -S (O) R, -S (O) NRR, -NRS (O) R, -NRSONRR, -NRC (O) R, -NRC (O) OR, -NRC (O) NRR, -OC (O) NRR or -NRR, moreover both R cannot be hydrogen at the same time, and wherein said alkyl, alkenyl, alkynyl and cycloalkyl are optionally substituted with halogen, oxo, —CN, OR, —NRR, C-Cycloalkyl, 3-6 membered heterocyclyl or phenyl, and said cycloalkyl, heterocyclyl and phenyl are independently optionally substituted with R; R and R are each independently hydrogen, C-Calkyl, C-Calkenyl, C-Calkynyl, halogen, - (C-Calkylene) CN, - (C- Calkylene) OR, - (C-Calkylene) SR, - (C-Calkylene) NRR, - (C-Calkylene) CF, -O (C-Calkylene) CF, - (C-Calkylene) NO, - (C-Calkylene ) C (O) R, - (C-Calkylene) C (O) OR, - (C-Calkylene) C (O) NRR, - (C-Calkylene) NRC (O) R, - (C-Calkylene) S (O) R, - (C-Ci-alkylene) NRS (O) R, - (C-Ci-alkylene) S (O) NRR, - (C-Ci-alkylene) (C-Cycloalkyl), - (C-Ci-alkylene) (3- 10-membered heterocyclyl), - (C-C1-6 alkylene) (5-10-membered heteroaryl) or - (C-C1-6 alkylene) phenyl, wherein R and R are each independently optionally substituted with R; Rpred is hydrogen, -NR-, -NRR, -NRC (O) -, -NRC (O) O-, -NRC (O) NR-, -NRS (O) - or -NRS (O) NR-; R is absent or is hydrogen, C 1-6 alkyl, C 1-6 alkenyl, C 1-6 alkynyl, C 1-6 cycloalkyl, C 1-6 aryl, 3-10 membered heterocyclyl or 5-10 membered heteroaryl, wherein R is optionally substituted with R; R and R, each independently, are hydrogen, C 1-6 alkyl, C 1-6 alkenyl, C 1-6 alkynyl or C 1-6 cycloalkyl, wherein said alkyl, alkenyl, alkynyl and cycloalkyl are independently optionally substituted with halo, C 1-6 alkyl, oxo, —CN, —OR or —NRR; or R and R independently, together with the atom to which they are atta
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