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    Pyrido-pyridazine derivatives as ligands for GABA receptors
    4.
    发明授权
    Pyrido-pyridazine derivatives as ligands for GABA receptors 失效
    吡啶并哒嗪衍生物作为GABA受体的配体

    公开(公告)号：US06593325B1

    公开(公告)日：2003-07-15

    申请号：US10069379

    申请日：2002-02-20

    申请人： William Robert Carling ,  Jose Luis Castro Pineiro ,  Andrew Mitchinson ,  Leslie Joseph Street

    发明人： William Robert Carling ,  Jose Luis Castro Pineiro ,  Andrew Mitchinson ,  Leslie Joseph Street

    IPC分类号： A61K315025

    CPC分类号： C07D471/04

    摘要： A class of pyrido[2,3-d]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 8-position, a substituted alkoxy moiety at the 2-position, and a range of substituents at the 3-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 and/or &agr;5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

    摘要翻译： 一类吡啶并[2,3-d]哒嗪衍生物，其在8-位上具有任选取代的环烷基，苯基或杂芳基取代基，2-位上的取代烷氧基部分和3-位上的取代基范围 是用于GABA A受体的选择性配体，特别是对α2和/或α3和/或α5亚基具有高亲和力，因此有益于治疗和/或预防中枢神经系统的不良状况，包括焦虑 抽搐和认知障碍。

    Triazolo-pyridazine derivatives as ligands for GABA receptors
    5.
    发明授权
    Triazolo-pyridazine derivatives as ligands for GABA receptors 失效
    三唑并哒嗪衍生物作为GABA受体的配体

    公开(公告)号：US06699859B1

    公开(公告)日：2004-03-02

    申请号：US09582445

    申请日：2000-06-26

    申请人： William Robert Carling ,  Andrew Mitchinson ,  Leslie Joseph Street

    发明人： William Robert Carling ,  Andrew Mitchinson ,  Leslie Joseph Street

    IPC分类号： A61P2508

    CPC分类号： C07D487/04

    摘要： 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, an optionally substituted N-linked nitrogen-containing aliphatic ring at the 7-position, and a chloro at the 8-position are selective ligands for GABAZA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, are useful in the treatment of anxiety and convulsions.

    摘要翻译： 具有任选取代的环烷基，3-位上的苯基或杂芳基取代基，6-位取代的烷氧基部分，任选取代的N-连接的氮原子的1,2,4-三唑并[4,3-b]哒嗪衍生物 含有7位的脂肪环，8位上的氯是GABAZA受体的选择性配体，特别是对其α2和/或α3亚基具有高亲和力，可用于治疗焦虑和抽搐。