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    Piperidine derivatives and their use as antagonists of tachykinins
    15.
    发明授权
    Piperidine derivatives and their use as antagonists of tachykinins 失效
    哌啶衍生物及其作为速激肽拮抗剂的用途

    公开(公告)号：US07276509B2

    公开(公告)日：2007-10-02

    申请号：US10502261

    申请日：2003-02-05

    申请人： Giuseppe Alvaro ,  Romano Di Fabio

    发明人： Giuseppe Alvaro ,  Romano Di Fabio

    IPC分类号： A61K31/496 ,  C07D401/04 ,  C07D211/58

    CPC分类号： C07D401/04

    摘要： The present invention relates to piperidine derivatives of formula (I): wherein R represents halogen or C1-4 alkyl; R1 represents hydrogen or C1-4 alkyl; R2 represents hydrogen, C1-4 alkyl; R3 represents hydrogen, C1-4 alkyl; R4 represents trifluoromethyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy or halogen; R5 represents hydrogen, C1-4 alkyl, C3-7 cycloalkyl, C(O)R6 or S(O)2R6; R6 represents C1-4 alkyl or C3-7 cycloalkyl; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; p is an integer from 1 to 2; X and Y are independently C(O) or CH2; provided that i) X and Y are not both C(O) and ii) when X and Y are both CH2 and p is 1, R5 is not hydrogen, C1-4 alkyl or C(O)R6; and pharmaceutically acceptable salts and solvates thereof, the process for their preparation and their use in the treatment of conditions mediated by tachykinins.

    摘要翻译： 本发明涉及式（I）的哌啶衍生物：其中R表示卤素或C 1-4烷基; R 1表示氢或C 1-4烷基; R 2表示氢，C 1-4烷基; R 3表示氢，C 1-4烷基; R 4表示三氟甲基，C 1-4烷基，C 1-4烷氧基，三氟甲氧基或卤素; R 5表示氢，C 1-4烷基，C 3-7环烷基，C（O）R 6 >或S（O）2 R 6 R 6; R 6表示C 1-4烷基或C 3-7环烷基; m为0或1〜3的整数; n为1〜3的整数， p是从1到2的整数; X和Y独立地为C（O）或CH 2 O 2; 条件是i）X和Y不同时为C（O），ii）当X和Y均为CH 2且p为1时，R 5不为氢， C 1-4烷基或C（O）R 6; 及其药学上可接受的盐和溶剂合物，其制备方法及其用于治疗由速激肽介导的病症。