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    Pyridinoylpiperidines as 5-HT1F agonists
    1.
    发明授权
    Pyridinoylpiperidines as 5-HT1F agonists 有权
    吡啶基哌啶作为5-HT1F激动剂

    公开(公告)号：US07423050B2

    公开(公告)日：2008-09-09

    申请号：US10509770

    申请日：2003-03-27

    申请人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Vincent Mancuso ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Piatt Zacherl ,  Deyi Zhang ,  Frantz Victor

    发明人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Vincent Mancuso ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Piatt Zacherl ,  Deyi Zhang ,  Frantz Victor

    IPC分类号： A61K31/445 ,  C07D401/06

    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; andn 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亚烷基 烷基，C 3 -C 7环烷基，取代的C 3 -C 7环烷基，C 1 -C 3烷基， 取代的C 3 -C 3烷基，取代的C 3 -C 3烷基，C 1 -C 3烷基，C 3 -C 3 - 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烷基，C 3 -C 3烷基，C 3 -C 3烷基， 或者式II的基团R 3是氢或C 1 -C 6烷基， C 1 -C 3烷基; R 4是氢，卤素或C 1 -C 3烷基; R 5是氢或C 1 -C 3烷基; R 5是氢或C 1 -C 3烷基; R 6是氢或C 1 -C 6烷基; n为1〜6的整数。 本发明的化合物可用于激活5-HT 1F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。

    Pyridinoylpiperidines as 5-HT1F agonists
    2.
    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：US20080300407A1

    公开(公告)日：2008-12-04

    申请号：US12220225

    申请日：2008-07-22

    申请人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Vincent Mancuso ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Piatt Zacherl ,  Deyi Zhang

    发明人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Vincent Mancuso ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Piatt Zacherl ,  Deyi Zhang

    IPC分类号： C07D401/14 ,  C07D401/06

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

    摘要： The 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基团; R3是氢或C1-C3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。

    Pyridinoylpiperidines as 5-HT1F agonists
    3.
    发明授权
    Pyridinoylpiperidines as 5-HT1F agonists 有权
    吡啶基哌啶作为5-HT1F激动剂

    公开(公告)号：US08748459B2

    公开(公告)日：2014-06-10

    申请号：US13363895

    申请日：2012-02-01

    申请人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Piatt Zacherl ,  Deyi Zhang

    发明人： Michael Philip Cohen ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  DeAnna Piatt Zacherl ,  Deyi Zhang

    IPC分类号： A61K31/445 ,  C07D401/06

    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-HTlF 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，以及用于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。

    Substituted (4-aminocyclohexen-1-yl)phenyl and (4-aminocyclohexen-1-yl)pyridinyl compounds as 5-ht1f agonists
    10.
    发明申请
    Substituted (4-aminocyclohexen-1-yl)phenyl and (4-aminocyclohexen-1-yl)pyridinyl compounds as 5-ht1f agonists 失效
    取代的（4-氨基环己烯-1-基）苯基和（4-氨基环己烯-1-基）吡啶基化合物作为5-ht1f激动剂

    公开(公告)号：US20070078169A1

    公开(公告)日：2007-04-05

    申请号：US10576762

    申请日：2004-12-06

    申请人： Daniel Kohlman ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  Deyi Zhang

    发明人： Daniel Kohlman ,  Frantz Victor ,  Yao-Chang Xu ,  Bai-Ping Ying ,  Deyi Zhang

    IPC分类号： A61K31/4439 ,  A61K31/44 ,  A61K31/277 ,  A61K31/165

    CPC分类号： C07D213/73 ,  C07C233/80 ,  C07C2601/16 ,  C07C2601/18 ,  C07D213/61 ,  C07D213/75

    摘要： The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, where; X is —C(R4)═ or —N═; Ar is phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R1 and R2 are independently hydrogen or C1-C3 alkyl; R3 is hydrogen, fluoro, or methyl; when X is —C(R4)═, R4 is hydrogen, fluoro, or methyl, provided that no more than one of R3 and R4 may be other than hydrogen; and R5 is hydrogen, methyl, or ethyl. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting dural protein extravasation, and for the treatment or prevention of migraine in a mammal.

    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： X是-C（R 4） - 或-N-; Ar是苯基，取代的苯基，杂环或取代的杂环; R 1和R 2独立地是氢或C 1 -C 3烷基; R 3是氢，氟或甲基; 当X是-C（R 4） - ）时，R 4是氢，氟或甲基，条件是R 3不超过一个 >和R 4可以不同于氢; R 5是氢，甲基或乙基。 本发明的化合物可用于活化5-HT 1F受体，抑制硬脑膜蛋白质外渗，以及治疗或预防哺乳动物偏头痛。