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N-phenylmethyl-5-oxo-proline-2-substituted amides as P2X7 receptor antagonists and methods of use
专利权人:
GLAXO GROUP LIMITED
发明人:
CHAMBERS, LAURA J,GLEAVE, ROBERT,SENGER, STEFAN,WALTER, DARYL SIMON
申请号:
ES07787001
公开号:
ES2385505T3
申请日:
2007.07.03
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound of formula (I) or a pharmaceutically acceptable salt thereof: ** Formula ** wherein: R1 represents methyl or ethyl, or unsubstituted C3-5 cycloalkyl, pyridinylmethyl-, phenyl or benzyl; R 2 and R 3 independently represent hydrogen, halogen, C 1-6 alkyl, arylmethyl-, C 2-6 alkenyl, C 2-6 alkynyl or C 3-6 cycloalkylmethyl; and any of said C1-6 alkyl, arylmethyl-, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkylmethyl is optionally substituted with 1, 2 or 3 halogen atoms; R4, R5 and R6 independently represent hydrogen, fluorine 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 or phenyl, and any of said C1-6 alkyl, alkenyl C2-6, C2-6 alkynyl, C3-6 cycloalkyl or phenyl is optionally substituted with 1, 2 or 3 halogen atoms; or R10 and R11, together with the carbon atoms to which they are attached, form a benzene ring that is optionally substituted with 1, 2 or 3 halogen atoms; with the proviso that when R7 and R11 are both selected from hydrogen or fluorine, at least one of R8, R9 and R10 is a halogen atom, or R8, R9 and R10 are selected from the group consisting of hydrogen and CF3, and one, but not more than one, of R8, R9 and R10 is CF3.Un compuesto de fórmula (I) o una de sus sales farmacéuticamente aceptables: **Fórmula**donde: R1 representa metilo o etilo, o cicloalquilo C3-5 no sustituido, piridinilmetil-, fenilo o bencilo; R2 y R3 independientemente representan hidrógeno, halógeno, alquilo C1-6, arilmetil-, alquenilo C2-6, alquinilo C2-6 o cicloalquilmetil- C3-6; y cualquiera de dichos alquilo C1-6, arilmetil-, alquenilo C2-6, alquinilo C2-6 o cicloalquilmetil- C3-6 está opcionalmente sustituido con 1, 2 ó 3 átomos de halógeno; R4, R5 y R6 independientemente representan hidrógeno, flúor o metilo; y R7, R8, R9, R10 y R11 independientemente representan hidrógeno, halógeno, ciano, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6 o fenilo, y cualqui
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