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    Pyrido-pyridazine derivatives as ligands for GABA receptors
    1.
    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。

    Imidazopyrazinones as GABA-A receptor anxiolytics
    6.
    发明授权
    Imidazopyrazinones as GABA-A receptor anxiolytics 失效
    咪唑并吡嗪酮作为GABA-A受体抗焦虑药

    公开(公告)号：US07485640B2

    公开(公告)日：2009-02-03

    申请号：US10533152

    申请日：2003-10-29

    申请人： William Robert Carling ,  Jose Luis Castro Pineiro ,  Simon Charles Goodacre ,  David James Hallett ,  Leslie Joseph Street

    发明人： William Robert Carling ,  Jose Luis Castro Pineiro ,  Simon Charles Goodacre ,  David James Hallett ,  Leslie Joseph Street

    IPC分类号： A01N43/64 ,  A01N43/90 ,  A61K31/53 ,  A61K31/519 ,  C07D253/08 ,  C07D487/00

    CPC分类号： C07D487/04

    摘要： The present invention discloses a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein —U—V— represents —CH═CH—, or —CH2—CH2—, —N═CH— or —CH═N—; X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— or —OCH2— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrocarbon, a heterocyclic group, trifluoromethyl, —SO2Ra, —SO2NRaRb, —CORa, —CO2Ra or —CONRaRb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; pharmaceutical compositions comprising it; its use in methods of treatment; use of it in the manufacture of a medicament for treating and/or preventing anxiety; convulsions or a cognitive disorder; and methods of treatment using it.

    摘要翻译： 本发明公开了式I化合物或其药学上可接受的盐：（I）其中-U-V-表示-CH-CH-或-CH 2 -CH 2 - ， - N-CH-或-CH-N-; X 1表示氢，卤素，C 1-6烷基，三氟甲基或C 1-6烷氧基; X2表示氢或卤素; Y代表化学键，氧原子或-NH-或-OCH2-键; Z表示任选取代的芳基或杂芳基; R1表示烃，杂环基，三氟甲基，-SO2Ra，-SO2NRaRb，-CORa，-CO2Ra或-CONRaRb; 并且R a和R b独立地表示氢，烃或杂环基; 包含它的药物组合物; 其用于治疗方法; 在制备用于治疗和/或预防焦虑的药物中的用途; 惊厥或认知障碍; 和使用它的治疗方法。