Spiro Compounds As NPY Y5 Receptor Antagonists
    4.
    发明申请
    Spiro Compounds As NPY Y5 Receptor Antagonists 审中-公开
    螺环化合物作为NPY Y5受体拮抗剂

    公开(公告)号:US20090203705A1

    公开(公告)日:2009-08-13

    申请号:US12360166

    申请日:2009-01-27

    摘要: The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R is an aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; Z1 is H, C1-C4 alkyl or F; Z is CH2, CH(C1-C4 alkyl), C(C1-C4 alkyl)2 or a bond; A is a 6-10 membered aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or —C(═O)—X; or —O(CH2)0-1R1; 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, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, hydroxyl, cyano; A and B being linked via any atom; R1 is —(C1-C4)alkyl(C1-C4)alkoxy; or C3-C8 cycloalkyl; or R1 is an aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or R1 is a 4-6 membered heterocycle, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; X is OR2 or NR3R4; R2 is C1-C4 alkyl; R3 is hydrogen or together with R4 and the nitrogen form a 5-6 saturated membered ring; R4 is C3-C8 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.

    摘要翻译: 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是可被一个或多个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 -C4卤代烷基,C1-C4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。