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5-OXO-3-pyrrolidine-carboxamide derivatives as P2X7 modulators
专利权人:
ГЛЭКСО ГРУП ЛИМИТЕД (GB)
发明人:
СТИДМАН Джон Грэхэм Энтони (GB),УОЛТЕР Дэрил Саймон (GB)
申请号:
RU2010129929/04
公开号:
RU2010129929A
申请日:
2008.12.17
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
1. A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof:! ! where! R1 is C1-4 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C3-6 cycloalkylmethyl, phenyl-X or heteroaryl, any of which may optionally be substituted with C1-6 alkyl, CF3, - O-C1-6 alkyl, CN or 1, 2 or 3 halogen atoms; ! X represents - (CR12R13) n-; ! R12 and R13 are hydrogen or C1-6 alkyl; ! n represents an integer selected from 0-2; ! R2, R3, R4, R5 and R6 independently represent hydrogen, fluoro or methyl; and! R7, R8, R9, R10 and R11 independently represent hydrogen, halogen, cyano, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, where any of the above C1-6 alkyl, C2-6 alkenyl , C2-6 alkynyl or C3-6 cycloalkyl groups may optionally be substituted with 1, 2 or 3 halogen atoms,! so that at least two of R7, R8, R9, R10 and R11 represent a group other than hydrogen, and at least one of R7 and R11 represents a group other than hydrogen. ! 2. The composition according to claim 1, where! R1 is C1-4 alkyl or C3-5 cycloalkyl; ! each of R2, R3, R4, R5 and R6 represents hydrogen; ! R7 is hydrogen, fluoro, chloro, methyl or —CF3; ! R8 is hydrogen or —CF3; ! R9 represents hydrogen, fluorine or chlorine; ! R10 is hydrogen, fluoro, chloro or —CF3; and! R11 is hydrogen, fluoro, chloro, methyl or —CF3; ! so that at least two of R7, R8, R9, R10 and R11 represent a group other than hydrogen, and at least one of R7 and R11 represents a group other than hydrogen. ! 3. The composition according to claim 2, where! R1 is methyl, ethyl, isobutyl or cyclopropyl; ! R7 represents chlorine; ! R10 represents hydrogen; and! R11 represents hydrogen. ! 4. The compound of formula (IA) or its pharmaceutics1. Фармацевтическая композиция, содержащая соединение формулы (I) или его фармацевтически приемлемую соль: ! ! где ! R1 представляет C1-4 алкил, С2-6 алкенил, С2-6 алкинил, С3-6 циклоалкил, С3-6 циклоалкилметил-, фенил-Х- или гетероарил, любой из которых мо
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