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    Heterocyclic compounds as bradykinin antagonists
    1.
    发明公开
    Heterocyclic compounds as bradykinin antagonists 失效
    Heterocyclische Verbindungen als缓激肽拮抗剂。

    公开(公告)号：EP0622361A1

    公开(公告)日：1994-11-02

    申请号：EP94106486.7

    申请日：1994-04-26

    申请人： FUJISAWA PHARMACEUTICAL CO., LTD.

    发明人： Oku, Teruo ,  Kayakiri, Hiroshi ,  Satoh, Shigeki ,  Abe, Yoshito ,  Sawada, Yuki ,  Inoue, Takayuki ,  Tanaka,Hirokazu

    IPC分类号： C07D257/00 ,  C07D215/26 ,  A61K31/395 ,  C07D401/12 ,  C07D409/12 ,  C07D403/12 ,  C07D241/42 ,  C07D237/28 ,  C07F7/18 ,  C07K5/06 ,  C07D239/86 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14

    CPC分类号： C07D401/12 ,  C07D215/26 ,  C07D237/28 ,  C07D239/74 ,  C07D241/42 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07F7/1856

    摘要： A compound of the formula :

    wherein

    X¹ is N or C-R⁶,
    X² is N or C-R⁷,
    X³ is N or C-R⁸,
    R¹ is hydrogen or halogen,
    R² is halogen,
    R³ is hydrogen, nitro, amino optionally having suitable substituent(s) or a heterocyclic group optionally having suitable substituent(s),
    R⁴ and R⁵ are each hydrogen or halogen,
    R⁶ and R⁸ are each hydrogen, halogen, lower alkyl, hydroxy, lower alkylthio, amino optionally substituted with lower alkyl, or lower alkoxy optionally substituted with a substituent selected from the group consisting of hydroxy, lower alkoxy, amino, lower alkylamino and aryl optionally substituted with lower alkoxy,
    R⁷ is hydrogen or lower alkyl,
    A is lower alkylene, and
    Q is O or N-R⁹, in which R⁹ is hydrogen or
    acyl, provided that R³ is not hydrogen when X¹ is C-R⁶, in which R⁶ is hydrogen,
    and pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising them.

    摘要翻译： 下式的化合物：其中X 1为N或CR 6，X 2为N或CR 7，X 3为N或CR 8，R 1为下式的化合物：其中X 1为N或CR 6， R 4是氢或卤素，R 2是卤素，R 3是氢，硝基，任选地具有合适的取代基的氨基或任选具有适当取代基的杂环基，R 4和R 5， 各自为氢或卤素，R 6和R 8各自为氢，卤素，低级烷基，羟基，低级烷硫基，任选被低级烷基取代的氨基或任选被选自以下的取代基取代的低级烷氧基： 羟基，低级烷氧基，氨基，低级烷基氨基和任选被低级烷氧基取代的芳基，R 7是氢或低级烷基，A是低级亚烷基，Q是O或NR 9，其中R 9是氢 或酰基，条件是当X 1为CR 6时R 3不为氢，其中R 6为氢，及其药学上可接受的盐，其制备方法和包含它们的药物组合物。