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    Pyridinoylpiperidines As 5-HT1F Agonists
    3.
    发明申请
    Pyridinoylpiperidines As 5-HT1F Agonists 有权
    吡啶基哌啶作为5-HT1F激动剂

    公开(公告)号：US20120329820A1

    公开(公告)日：2012-12-27

    申请号：US13363895

    申请日：2012-02-01

    申请人： Michael P. Cohen ,  Daniel T. Kohlman ,  Sidney X. Liang ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  Deanna P. Zacherl ,  Deyi Zhang

    发明人： Michael P. Cohen ,  Daniel T. Kohlman ,  Sidney X. Liang ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  Deanna P. Zacherl ,  Deyi Zhang

    IPC分类号： A61K31/4545 ,  C07D409/14 ,  A61K31/506 ,  C07D405/14 ,  C07D417/14 ,  A61P25/06 ,  C07D401/06 ,  C07D401/14

    CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

    摘要： The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II R3 is hydrogen or C1-C3 alkyl; R4 is hydrogen, halo, or C1-C3 alkyl; R5 is hydrogen or C1-C3 alkyl; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.

    摘要翻译： 本发明涉及式I化合物或其药学上可接受的酸加成盐，其中： R 1是C 1 -C 6烷基，取代的C 1 -C 6烷基，C 3 -C 7环烷基，取代的C 3 -C 7环烷基，C 3 -C 7环烷基-C 1 -C 3烷基，取代的C 3 -C 7环烷基-C 1 -C 3烷基，苯基，取代的苯基， 杂环或取代的杂环; R 2是氢，C 1 -C 3烷基，C 3 -C 6环烷基-C 1 -C 3烷基或式II的基团R 3是氢或C 1 -C 3烷基; R4是氢，卤素或C1-C3烷基; R5是氢或C1-C3烷基; R6是氢或C1-C6烷基; n为1〜6的整数。 本发明的化合物可用于激活5-HT1F受体，抑制神经元蛋白质外渗，以及治疗或预防哺乳动物偏头痛。 本发明还涉及合成式I化合物中的中间体的方法。