Amine-derivatives having NPY Y5 receptor antagonistic activity and the uses thereof
    5.
    发明授权
    Amine-derivatives having NPY Y5 receptor antagonistic activity and the uses thereof 失效
    具有NPY Y5受体拮抗活性的胺衍生物及其用途

    公开(公告)号:US08227618B2

    公开(公告)日:2012-07-24

    申请号:US12766458

    申请日:2010-04-23

    IPC分类号: C07D263/58 A61K31/423

    摘要: This invention provides an anorectic or anti-obesity composition comprising a compound of the formula (I): formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted lower alkyl, Y is —S(O)n- wherein n is 1 or 2, or —CO—, R2 is hydrogen or lower alkyl, R7 is hydrogen or lower alkyl, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, and Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like.

    摘要翻译: 本发明提供一种厌食或抗肥胖组合物,其包含式(I)化合物:式(I):其药学上可接受的盐或溶剂合物,其中R 1为任选取代的低级烷基,Y为-S(O) 其中n为1或2,或-CO-,R 2为氢或低级烷基,R 7为氢或低级烷基,X为低级亚烷基,低级亚烯基,亚芳基,亚环烷基等,Z为低级烷基,任选取代的碳环基 ,任选取代的杂环基等。

    Cyclohexane derivative having NPY Y5 receptor antagonism
    9.
    发明授权
    Cyclohexane derivative having NPY Y5 receptor antagonism 失效
    具有NPY Y5受体拮抗作用的环己烷衍生物

    公开(公告)号:US08653125B2

    公开(公告)日:2014-02-18

    申请号:US13254702

    申请日:2010-03-05

    摘要: The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted aryl or heterocyclyl; a combination of X and Y is a combination selected from (X, Y)═(C(═O)N(R1), C(═O)N(R2)), (C(═O)N(R1), imidazole-1,3-diyl), (N(R1), C(═O)N(R2)), (O, C(═O)N(R2)), (C(R3)(R4), N(R2)) or (a single bond, C(═O)N(R2)); R1, R2 and R3 are independently hydrogen or substituted or unsubstituted alkyl; R5 is substituted or unsubstituted aryl or heterocyclyl; R6 is halogen, oxo, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy; m is 0 or 1; and n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or fused bicyclic heterocycle.

    摘要翻译: 本发明公开了具有NPY Y5受体拮抗活性的新型环己烷衍生物。 具体而言,本发明公开了式(I)表示的化合物或其药学上可接受的盐或溶剂化物:其中A为取代或未取代的芳基或杂环基; X和Y的组合是选自(X,Y)=(C(= O)N(R1),C(= O)N(R2)),(C(= O)N(R1) 咪唑-1,3-二基),(N(R1),C(= O)N(R2)),(O,C(= O)N(R2)),(C(R3) (R2))或(单键,C(= O)N(R2)); R1,R2和R3独立地是氢或取代或未取代的烷基; R5是取代或未取代的芳基或杂环基; R 6是卤素,氧代,取代或未取代的烷基,取代或未取代的烷氧基,取代或未取代的芳氧基; m为0或1; n为0〜5的整数。 和B是芳族碳环,单环杂环或稠合双环杂环。