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    Benzothiophene compounds as antithrombotic agents and intermediates
    8.
    发明公开
    Benzothiophene compounds as antithrombotic agents and intermediates 有权
    Benzothiophenderivate als ANTITROMBOTISCHE MITTELN und zwischenprodukte

    公开(公告)号：EP0997460A1

    公开(公告)日：2000-05-03

    申请号：EP99308495.3

    申请日：1999-10-27

    申请人： ELI LILLY AND COMPANY

    发明人： McCowan, Jefferson Ray ,  Sall, Daniel Jon ,  Toth, John Eldon

    IPC分类号： C07D333/66 ,  A61K31/381 ,  A61P7/02

    CPC分类号： C07D409/12 ,  C07D333/66

    摘要： This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.
    wherein

    E is CR e or N in which R e is hydrogen, methyl, methoxy or halo;
    R 1 is hydrogen or methyl;
    R 2 is R 2a or R 2b in which
    R 2a is -X 2 -(CH 2 ) n -R f in which X 2 is a direct bond, methylene or O; n is 1, 2 or 3; and R f is 5-tetrazolyl, carboxy, [(1-4C)alkoxy]carbonyl or hydroxymethyl;
    R 2b is -X 2 -(CH 2 ) m -NR a R b in which X 2 is a direct bond, methylene or O; m is 1, 2 or 3; provided that when m is 1, then X 2 is a direct bond; and R a and R b are independently hydrogen or (1-3C)alkyl or the group NR a R b is pyrrolidino, piperidino or morpholino;
    R 3 is -X 3 -(CH 2 ) s -NR s R t in which X 3 is a direct bond, methylene or O; s is 1 or 2; provided that when s is 1, then X 3 is a direct bond; and R s and R t are independently hydrogen or (1-3C)alkyl or the group NR s R t is pyrrolidino, piperidino or morpholino; and
    R 6 is hydrogen, hydroxy or methoxy.

    摘要翻译： 本申请涉及本文所定义的式I（及其药学上可接受的盐）的新化合物，其制备方法和中间体，包含式I的新型化合物的药物制剂，以及式I化合物作为凝血酶抑制剂的用途 。 其中E是CR e或N，其中R e是氢，甲基，甲氧基或卤素; R 1是氢或甲基; R 2是R 2a或R 2b，其中R 2a是-X 2 - （CH 2）n -R 5，其中X 2是直接键，亚甲基或O; n为1,2或3; 并且R f是5-四唑基，羧基，Ä（1-4C）烷氧基羰基或羟甲基; R 2b是-X 2 - （CH 2）m -NR a R b，其中X 2是直接键，亚甲基或O; m为1,2或3; 条件是当m为1时，X 2为直接键; R a和R b独立地是氢或（1-3C）烷基，或者NR a R b是吡咯烷子基，哌啶子基或吗啉代; R 3是-X 3 - （CH 2）s -NR s R t，其中X 3是直接键，亚甲基或O; s是1或2; 条件是当s为1时，X 3为直接键; 且R和R独立地为氢或（1-3C）烷基或基团NR≡为吡咯烷子基，哌啶子基或吗啉代; 和R 6是氢，羟基或甲氧基