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13 条记录 (耗时 0.011 秒)

    Polyamines useful as antagonists of excitatory amino acid neurotransmitters and/or as blockers of calcium channels
    5.
    发明公开
    Polyamines useful as antagonists of excitatory amino acid neurotransmitters and/or as blockers of calcium channels 失效
    多胺和由氨基酸和/或钙通道的阻断剂激发神经递质的拮抗剂的多肽。

    公开(公告)号：EP0395357A2

    公开(公告)日：1990-10-31

    申请号：EP90304397.4

    申请日：1990-04-24

    申请人： PFIZER INC. ,  NPS PHARMACEUTICALS, INC.

    发明人： Saccomano, Nicholas Alex ,  Volkmann, Robert Alfred

    IPC分类号： C07D209/18 ,  C07C235/50 ,  C07C235/60 ,  C07K14/235 ,  A61K31/165 ,  A61K31/405 ,  A61K38/16

    CPC分类号： C07D209/18 ,  A61K38/00 ,  C07C239/16 ,  C07K14/43518

    摘要： This invention relates to certain polyamines and polypeptides found to be present in the venom of the Agelenopsis aperta spider. The polyamines of this invention and the salts thereof antagonize excitatory amino acid neurotransmitters, which neurotransmitters affect cells of various organisms and are useful in antagonizing said neurotransmitters, per se, in the treatment of excitatory amino acid neurotransmitter mediated diseases and conditions and in the control of invertebrate pests. The polypeptides of this invention and one of said polyamines and the salts thereof block calcium channels in cells of various organisms and are useful in blocking said calcium channels in cells, per se, in the treatment of calcium channel mediated diseases and conditions and in the control of invertebrate pests. This invention also relates to compositions comprising said polyamines, polypeptides and salts thereof.

    摘要翻译： 本发明涉及某些聚胺和多肽被发现存在于棚蛛属aperta蜘蛛毒液中。 本发明的和多胺及其盐拮抗兴奋性氨基酸神经递质，其中神经递质影响各种细胞生物的细胞，并且可用于拮抗所述神经递质，本身，在兴奋性氨基酸神经递质介导的疾病和病症的治疗和控制 无脊椎动物害虫。 本发明的多肽和所述多胺之一，在各种生物体的细胞或其块钙通道的盐，并且在阻断细胞本身所述钙通道是有用的，在有钙通道介导的疾病和病症的治疗，并在控制 无脊椎动物害虫。 本发明因此涉及的组合物包括所述聚胺，多肽和它们的盐。

    Antidepressant N-substituted nicotinamide compounds
    6.
    发明公开
    Antidepressant N-substituted nicotinamide compounds 失效
    抗抑郁药N-取代基烟酰胺 - 维生素

    公开(公告)号：EP0357316A1

    公开(公告)日：1990-03-07

    申请号：EP89308481.4

    申请日：1989-08-22

    申请人： PFIZER INC.

    发明人： Saccomano, Nicholas Alex ,  Vinick, Fredric James

    IPC分类号： C07D213/82 ,  C07D401/12 ,  A61K31/455 ,  A61K31/475

    CPC分类号： C07D213/82 ,  C07D401/12

    摘要： Certain N-substituted nicotinamide compounds having formula (I) below
    and pharmaceutically acceptable acid addition salts thereof wherein R¹ is 1-piperidyl, 1-(3-indolyl)ethyl, C₁₋₄ alkyl, phenyl, 1-(1-phenylethyl), benzyl or mono-substituted benzyl wherein the substituent is methyl, methoxy, chloro or fluoro; and R² is bicyclo[2.2.1]hept-2-yl or
    wherein Y is hydrogen, fluoro or chloro; and
    X is hydrogen, fluoro, chloro, methoxy, trifluoromethyl, cyano, carboxy, carbo(C₁₋₄ alkoxy), methylcarbamoyl or dimethylcarbamoyl function as selective inhibitors of calcium-independent phosphodiesterase and are useful as antidepressants.

    摘要翻译： 具有下式（I）的某些N-取代烟酰胺化合物及其药学上可接受的酸加成盐，其中R 1是1-哌啶基，1-（3-吲哚基）乙基，C 1-4烷基，苯基， （1-苯基乙基），苄基或单取代的苄基，其中取代基是甲基，甲氧基，氯或氟; 和R 2是双环[2.2.1]庚-2-基或CHEM，其中Y是氢，氟或氯; 并且X是氢，氟，氯，甲氧基，三氟甲基，氰基，羧基，碳（C 1-4烷氧基），甲基氨基甲酰基或二甲基氨基甲酰基作为钙非依赖性磷酸二酯酶的选择性抑制剂，可用作抗抑郁剂。