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13 条记录 (耗时 0.012 秒)

    8-substituted-1,3,8-triazaspiro[4.5]decan-4-on derivatives
    13.
    发明公开
    8-substituted-1,3,8-triazaspiro[4.5]decan-4-on derivatives 失效
    8 substituierte -1,3,8-三氮杂螺[4,5]癸烷-4- onderivate

    公开(公告)号：EP0856514A1

    公开(公告)日：1998-08-05

    申请号：EP98100970.7

    申请日：1998-01-21

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： Adam, Geo ,  Cesura, Andrea ,  Galley, Guido ,  Jenck, François ,  Monsma, Frederick ,  Röver, Stephan ,  Wichmann, Jürgen

    IPC分类号： C07D471/10 ,  A61K31/44

    CPC分类号： C07D471/10

    摘要： The present invention relates to compounds of the formula
    wherein

    R 1 and R 2 are, independently from each other, hydrogen, lower alkyl, lower alkoxy or halogen;
    R 3 is phenyl, optionally substituted by lower alkyl,CF 3 , lower alkoxy or halogen; and
    R 4 is hydrogen, lower alkyl, lower alkenyl, -C(O)-lower alkyl, -C(O)-phenyl, lower alkyl-C(O)-phenyl, lower alkylen-C(O)O-lower alkyl, lower alkantriyl-di-C(O)O-lower alkyl, hydroxy-lower alkyl, lower alkyl-O-lower alkyl, lower alkyl-CH(OH)CF 3 , phenyl or benzyl,
    R 5 and R 6 are, independently from each other, hydrogen, phenyl, lower alkyl or di-lower alkyl or may form together a phenyl ring, and
    R 5 and one of R 1 or R 2 may form together a saturated or unsaturated 6 membered ring,
    A is a 4 - 7 membered saturated ring which may contain a heteroatom such as O or S,
    and to pharmaceutically acceptable acid addition salts thereof which are agonists and/or antagonists of the OFQ receptor.

    摘要翻译： 本发明涉及式CHEM的化合物，其中R 1和R 2彼此独立地为氢，低级烷基，低级烷氧基或卤素; R 3是任选被低级烷基，CF 3，低级烷氧基或卤素取代的苯基; （O） - 低级烷基，-C（O） - 苯基，低级烷基-C（O） - 苯基，低级亚烷基-C（O）O- 低级烷基，低级三烷基 - 二-C（O）O-低级烷基，羟基 - 低级烷基，低级烷基-O-低级烷基，低级烷基-CH（OH）CF 3，苯基或苄基，R 5和R' 6>彼此独立地为氢，苯基，低级烷基或二 - 低级烷基，或者可以一起形成苯环，R 5和R 1或R 2中的一个可以一起形成饱和的 或不饱和6元环，A为可含有杂原子如O或S的4-7元饱和环，以及作为OFQ受体的激动剂和/或拮抗剂的药学上可接受的酸加成盐。