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    • 1. 发明申请
    • 5-OXO-3-PYRROLIDINECARBOXAMIDE DERIVATIVES AS P2X7 MODULATORS
    • 作为P2X7调节剂的5-OXO-3-吡咯烷酰胺酰胺衍生物
    • WO2009077559A3
    • 2009-09-24
    • PCT/EP2008067733
    • 2008-12-17
    • GLAXO GROUP LTDSTEADMAN JON GRAHAM ANTHONYWALTER DARYL SIMON
    • STEADMAN JON GRAHAM ANTHONYWALTER DARYL SIMON
    • A61K31/4015A61P25/00A61P29/00
    • A61K31/4015
    • The present invention provides a compound of formula (IA) or a pharmaceutically acceptable salt thereof: wherein: R1 represents C1-4 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C3-6 cycloalkylmethyl-, phenyl-X- or heteroaryl, any of which may be optionally substituted; X represents -(CR12R13)n-; n represents 0 to 2; and R7, R8, R9, R10 and R11 independently represent H, halogen, or cyano; or optionally substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkyl; such that at least two of R7, R8, R9, R10 and R11 represent a group other than H and at least one of R7 and R11 represents a group other than H; and wherein the compound is other than N-[(2,4-dichlorophenyl)methyl]-5-oxo-1-(phenylmethyl)-3-pyrrolidinecarboxamide. The compounds and salts are thought to modulate P2X7 receptor function and be capable of antagonizing the effects of ATP at the P2X7 receptor.
    • 本发明提供式(IA)化合物或其药学上可接受的盐:其中:R 1表示C 1-4烷基,C 2-6烯基,C 2-6炔基,C 3-6环烷基,C 3-6环烷基甲基 - ,苯基 - X-或杂芳基,它们中的任何一个可被任选取代; X代表 - (CR 12 R 13)n - n表示0至2; 并且R 7,R 8,R 9,R 10和R 11独立地表示H,卤素或氰基; 或任选取代的C 1-6烷基,C 2-6烯基,C 2-6炔基或C 3-6环烷基; 使得R 7,R 8,R 9,R 10和R 11中的至少两个表示除H以外的基团并且R 7和R 11中的至少一个表示除H以外的基团; 并且其中所述化合物不是N - [(2,4-二氯苯基)甲基] -5-氧代-1-(苯基甲基)-3-吡咯烷甲酰胺。 认为化合物和盐调节P2X 7受体功能并能够拮抗ATP在P2X 7受体上的作用。
    • 7. 发明申请
    • 5-OXO-3-PYRROLIDINECARBOXAMIDE DERIVATIVES AS P2X7 MODULATORS
    • 作为P2X7调节剂的5-氧代-3-吡咯烷酮甲酰胺衍生物
    • WO2009077559A2
    • 2009-06-25
    • PCT/EP2008/067733
    • 2008-12-17
    • GLAXO GROUP LIMITEDSTEADMAN, Jon Graham AnthonyWALTER, Daryl Simon
    • STEADMAN, Jon Graham AnthonyWALTER, Daryl Simon
    • A61K31/4015A61P25/00A61P29/00
    • A61K31/4015
    • The present invention provides a compound of formula (IA) or a pharmaceutically acceptable salt thereof: wherein: R 1 represents C 1-4 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, C 3-6 cycloalkylmethyl-, phenyl-X- or heteroaryl, any of which may be optionally substituted; X represents -(CR 12 R 13 ) n -; n represents 0 to 2; and R 7 , R 8 , R 9 , R 10 and R 11 independently represent H, halogen, or cyano; or optionally substituted C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl or C 3-6 cycloalkyl; such that at least two of R 7 , R 8 , R 9 , R 10 and R 11 represent a group other than H and at least one of R 7 and R 11 represents a group other than H; and wherein the compound is other than N -[(2,4-dichlorophenyl)methyl]-5-oxo-1-(phenylmethyl)-3-pyrrolidinecarboxamide. The compounds and salts are thought to modulate P2X7 receptor function and be capable of antagonizing the effects of ATP at the P2X7 receptor.
    • 本发明提供式(IA)化合物或其药学上可接受的盐:其中:R 1表示C 1-4烷基,C 2-6烯基,C 2-6炔基,C 3-6环烷基,C 3-6环烷基甲基 - ,苯基 - X-或杂芳基,其中任何一个可以任选被取代; X表示 - (CR12R13)n-; n表示0〜2; 且R 7,R 8,R 9,R 10和R 11独立地表示H,卤素或氰基; 或任选取代的C 1-6烷基,C 2-6烯基,C 2-6炔基或C 3-6环烷基; 使得R 7,R 8,R 9,R 10和R 11中的至少两个表示除H以外的基团,并且R 7和R 11中的至少一个表示除H以外的基团; 并且其中所述化合物不是N - [(2,4-二氯苯基)甲基] -5-氧代-1-(苯甲基)-3-吡咯烷甲酰胺。 化合物和盐被认为调节P2X7受体功能,并能够拮抗ATP在P2X7受体上的作用。