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    • 3. 发明申请
    • SPIRO COMPOUNDS AS NPY Y5 RECEPTOR ANTAGONISTS
    • SPIRO化合物作为NPY Y5受体拮抗剂
    • WO2009095377A1
    • 2009-08-06
    • PCT/EP2009/050867
    • 2009-01-27
    • GLAXO GROUP LIMITEDBIAGETTI, MatteoCONTINI, Stefania AnneGENSKI, ThorstenGUERY, SebastienLESLIE, Colin PhilipMAZZALI, AngelicaPIZZI, Domenica AntoniaSABBATINI, Fabio MariaSERI, Catia
    • BIAGETTI, MatteoCONTINI, Stefania AnneGENSKI, ThorstenGUERY, SebastienLESLIE, Colin PhilipMAZZALI, AngelicaPIZZI, Domenica AntoniaSABBATINI, Fabio MariaSERI, Catia
    • C07D413/12C07D413/14C07D417/14A61K31/423A61P3/00
    • C07D413/12C07D413/14C07D417/14
    • The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt thereof, (I) wherein R is an aryl or heteroaryl, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano; Z 1 is H, C 1 -C 4 alkyl or F; Z is CH 2 , CH(C 1 -C 4 alkyl), C(C 1 -C 4 alkyl)2 or a bond; A is a 6-10 membered aryl or heteroaryl, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano; or -C(=O)-X; or O(CH 2 ) 0-1 R 1 ; B is hydrogen or is a 5-6 membered heteroaryl, or a 4-6 membered heterocycle, or phenyl, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, hydroxyl, cyano; A and B being linked via any atom; R 1 is -(C 1 -C 4 )alkyl(C 1 -C 4 )alkoxy; or C 3 -C 8 cycloalkyl; or R 1 is an aryl or heteroaryl, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano; or R 1 is a 4-6 membered heterocycle, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano; X is OR 2 or NR 3 R 4 ; R 2 is C 1 -C 4 alkyl; R 3 is hydrogen or together with R 4 and the nitrogen form a 5-6 saturated membered ring; R 4 is C 3 -C 8 cycloalkyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.
    • 本发明涉及新的式(I)化合物或其药学上可接受的盐,其中R是芳基或杂芳基,其可被一个或多个取代:卤素,C 1 -C 4烷基,C 1 -C 4 烷氧基,C 1 -C 4卤代烷基,C 1 -C 4卤代烷氧基,氰基; Z 1是H,C 1 -C 4烷基或F; Z是CH 2,CH(C 1 -C 4烷基),C(C 1 -C 4烷基)2或键; A是6-10元芳基或杂芳基,其可以被一个或多个取代:卤素,C 1 -C 4烷基,C 1 -C 4烷氧基,C 1 -C 4卤代烷基,C 1 -C 4卤代烷氧基,氰基; 或-C(= O)-X; 或O(CH 2)0-1R1; B是氢或是5-6元杂芳基或4-6元杂环,或苯基,其可被一个或多个取代:卤素,C 1 -C 4烷基,C 1 -C 4烷氧基,C 1 -C 4卤代烷基,C 1 -C4卤代烷氧基,羟基,氰基; A和B通过任何原子相连; R1是 - (C1-C4)烷基(C1-C4)烷氧基; 或C 3 -C 8环烷基; 或者R 1是可被一个或多个卤素取代的芳基或杂芳基:卤素,C 1 -C 4烷基,C 1 -C 4烷氧基,C 1 -C 4卤代烷基,C 1 -C 4卤代烷氧基,氰基; 或R 1是4-6元杂环,其可以被一个或多个取代:卤素,C 1 -C 4烷基,C 1 -C 4烷氧基,C 1 -C 4卤代烷基,C 1 -C 4卤代烷氧基,氰基; X为OR2或NR3R4; R2是C1-C4烷基; R3是氢或与R4一起形成5-6饱和的元环; R4是C3-C8环烷基; 它们的制备方法,这些方法中使用的中间体,含有它们的药物组合物及其在治疗中的用途,作为NPY Y5受体拮抗剂以及用于治疗和/或预防进食障碍如狂饮病症的药剂。