Substituted (4-aminocyclohexen-1-yl)phenyl and (4-aminocyclohexen-1-yl)pyridinyl compounds as 5-ht1f agonists
    8.
    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

    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。

    Pyridinoylpiperidines as 5-HT1F agonists
    9.
    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

    IPC分类号: A61K31/445 C07D401/06

    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。

    Substituted (4-aminocyclohexen-1-yl)phenyl and (4-aminocyclohexen-1-yl)pyridinyl compounds as 5-HT1F agonists
    10.
    发明授权
    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:US07312236B2

    公开(公告)日:2007-12-25

    申请号:US10576762

    申请日:2004-12-06

    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 R3and 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。