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20 条记录 (耗时 0.034 秒)

    Imidazopyrazinones as GABA-A receptor anxiolytics
    7.
    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。

    Substituted pyrido-pyridazine derivatives which enhance cognition via the GABA-A receptors
    9.
    发明授权
    Substituted pyrido-pyridazine derivatives which enhance cognition via the GABA-A receptors 失效
    取代的吡啶并哒嗪衍生物，其通过GABA-A受体增强认知

    公开(公告)号：US07148222B2

    公开(公告)日：2006-12-12

    申请号：US10531517

    申请日：2003-10-29

    申请人： Simon Charles Goodacre ,  David James Hallett

    发明人： Simon Charles Goodacre ,  David James Hallett

    IPC分类号： C07D471/04 ,  A61K31/5025

    CPC分类号： C07D471/04

    摘要： The present invention discloses a compound of formula 1, or a pharmaceutically acceptable salt thereof: wherein 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— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, NRaRb, —NRaCORb, —NRaCO2Rb, —CORa, —CO2Ra, —CONRaRb or —CRa&═NORb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; a pharmaceutical composition comprising it; its use in a method of treatment; use of it to manufacture a medicament; and a method of using it to prevent or treat anxiety, convulsions or cognitive disorders.

    摘要翻译： 本发明公开了式1化合物或其药学上可接受的盐：其中X 1表示氢，卤素，C 1-6烷基，三氟甲基或C 1-6烷氧基; X 2表示氢或卤素; Y表示化学键，氧原子或-NH-键; Z表示任选取代的芳基或杂芳基; R 1表示氢，烃，杂环基，卤素，氰基，三氟甲基，硝基，-OR a，-SR a，-SOR 一个或两个以上的一个或多个，其中，R 1，R 2，R 2， 其中，R a，R b，R b，R b，R b， CO 2，CO 2 CO 2 SO 2，-SO 2 R 2， 或者 ， 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; 使用它制造药物; 以及使用它来预防或治疗焦虑，抽搐或认知障碍的方法。

    5-phenyl[1,2,4]triazines as ligands for GABA-A α2/α3 receptors for treating anxiety or depression
    10.
    发明授权
    5-phenyl[1,2,4]triazines as ligands for GABA-A α2/α3 receptors for treating anxiety or depression 失效
    5-苯基[1,2,4]三嗪作为用于治疗焦虑或抑郁症的GABA-Aα2/α3受体的配体

    公开(公告)号：US06969716B2

    公开(公告)日：2005-11-29

    申请号：US10769070

    申请日：2004-01-30

    申请人： Wesley Peter Blackaby ,  Simon Charles Goodacre ,  David James Hallett ,  Andrew Jennings ,  Richard Thomas Lewis ,  Leslie Joseph Street ,  Kevin Wilson

    发明人： Wesley Peter Blackaby ,  Simon Charles Goodacre ,  David James Hallett ,  Andrew Jennings ,  Richard Thomas Lewis ,  Leslie Joseph Street ,  Kevin Wilson

    IPC分类号： A61K31/53 ,  C07D253/065 ,  A61P25/22

    CPC分类号： A61K31/53

    摘要： The present invention provides a compound of formula I, or an N-oxide thereof or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy;X2 represents hydrogen or halogen;Z represents hydrogen, halogen, cyano, cyanomethyl, trifluoromethyl, nitro, hydroxy, hydroxy(C1-6)alkyl, C1-6 alkoxy, C1-6 alkoxy(C1-6)alkyl, trifluoromethoxy, trifluoromethylthio, trifluoromethanesulfinyl, formyl, C2-6 alkoxycarbonyl, oxopyrrolidinyl, or an optionally substituted aryl, heteroaryl or heteroaryl(C1-6)alkoxy group; andR1 represents aryl or heteroaryl, either of which groups may be optionally substituted;pharmaceutical compositions comprising it, its use in therapy and methods of treatment of anxiety and/or depression using it.

    摘要翻译： 本发明提供式I化合物或其N-氧化物或其药学上可接受的盐：其中X 1表示氢，卤素，C 1-6烷基 ，三氟甲基或C 1-6烷氧基; X 2表示氢或卤素; Z表示氢，卤素，氰基，氰基甲基，三氟甲基，硝基，羟基，羟基（C 1-6 - ）烷基，C 1-6烷氧基，C 1 C 1-6烷氧基（C 1-6）烷基，三氟甲氧基，三氟甲硫基，三氟甲磺酰基，甲酰基，C 2-6烷氧基羰基，氧代吡咯烷基或任选取代的芳基 ，杂芳基或杂芳基（C 1-6 - ）烷氧基; 且R 1表示芳基或杂芳基，其中任一个可以任选被取代; 包含它的药物组合物，其在治疗中的用途以及使用其治疗焦虑和/或抑郁症的方法。