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    SUSTITUTED IMIDAZOLOPYRAZINE AND TRIAZOLOPYRAZINE DERIVATIVES: GABAA RECEPTOR LIGANDS
    2.
    发明公开
    SUSTITUTED IMIDAZOLOPYRAZINE AND TRIAZOLOPYRAZINE DERIVATIVES: GABAA RECEPTOR LIGANDS 审中-公开
    悬浮咪唑并吡嗪和三唑并吡嗪衍生物：GABAA受体配体

    公开(公告)号：EP1619948A1

    公开(公告)日：2006-02-01

    申请号：EP04751255.3

    申请日：2004-05-03

    申请人： NEUROGEN CORPORATION ,  Xu, Yuelian ,  Han, Bingsong ,  Xie, Linghong

    发明人： XU, Yuelian ,  HAN, Bingsong ,  XIE, Linghong

    IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/495 ,  A61K31/50 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00 ,  C07D495/00 ,  C07D497/00

    CPC分类号： C07D487/04 ,  G01N33/566

    摘要： Compounds of Formula (I) are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8, and Ar in the above Formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).

    摘要翻译： 提供式（I）化合物，以及它们的制备方法。 上式中的变量Z1，Z2，Z3，R4，R5，R6，R7，R8和Ar在本文中定义。 此类化合物可用于在体内或体外调节配体与GABAA受体的结合，并且特别可用于治疗人，家养伴侣动物和家畜中的各种中枢神经系统（CNS）疾病。 本文提供的化合物可以单独施用或与一种或多种其他CNS试剂组合施用以增强其他CNS试剂的作用。 提供了用于治疗此类病症的药物组合物和方法，以及使用这些配体用于检测GABAA受体（例如受体定位研究）的方法。

    TETRAHYDROPYRIDO[3,4-D]PYRIMIDINES AND RELATED ANALOGUES
    5.
    发明公开
    TETRAHYDROPYRIDO[3,4-D]PYRIMIDINES AND RELATED ANALOGUES 审中-公开
    四氢吡啶[3,4-D]嘧啶及其类似物

    公开(公告)号：EP2029588A2

    公开(公告)日：2009-03-04

    申请号：EP07795899.9

    申请日：2007-06-08

    申请人： NEUROGEN CORPORATION

    发明人： XU, Yuelian ,  GAO, Yang ,  XIE, Linghong

    IPC分类号： C07D471/02 ,  C07D417/14 ,  C07D265/30 ,  A61K31/54

    CPC分类号： A61K31/496 ,  A61K31/55 ,  C07D471/04 ,  C07D487/04

    摘要： Tetrahydropyrido[3,4-d]pyrimidines and related analogues are provided, of the formula (I) in which variables are as described herein, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).

    摘要翻译： 提供了式（I）的四氢吡啶并[3,4-d]嘧啶及相关类似物，其中变量如本文所述，以及它们的制备和使用方法。 这些化合物通常可以用于在体内或体外调节配体与组胺H3受体的结合，并且特别可用于治疗人，家养伴侣动物和家畜动物中的各种病症。 提供了药物组合物和治疗方法，以及使用这些配体检测组胺H3受体的方法（例如受体定位研究）。

    THIAZOLE AMIDES, IMIDAZOLE AMIDES AND RELATED ANALOGUES
    7.
    发明公开
    THIAZOLE AMIDES, IMIDAZOLE AMIDES AND RELATED ANALOGUES 审中-公开
    噻唑酰胺，咪唑酰胺和相关类似物

    公开(公告)号：EP1848428A2

    公开(公告)日：2007-10-31

    申请号：EP06735288.0

    申请日：2006-02-16

    申请人： NEUROGEN CORPORATION

    发明人： PRINGLE, Wallace C. ,  PETERSON, John M. ,  XIE, Linghong ,  GE, Ping ,  GAO, Yang ,  OCHTERSKI, Joseph W. ,  LAN, Jiong

    IPC分类号： A61K31/426 ,  C07D277/24 ,  C07D277/28

    CPC分类号： C07D231/14 ,  C07D233/64 ,  C07D233/90 ,  C07D277/28 ,  C07D277/30 ,  C07D401/06 ,  C07D403/06 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04

    摘要： Thiazole amides, imidazole amides and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).

    摘要翻译： 提供噻唑酰胺，咪唑酰胺和式的相关类似物，其中变量如本文所述。 此类化合物可用于在体内或体外调节配体与组胺H3受体的结合，并且特别用于治疗人类，家养伴侣动物和家畜动物中的各种中枢神经系统（CNS）和其他病症。 本文提供的化合物可以单独施用或与一种或多种其他CNS试剂组合施用以增强其他CNS试剂的作用。 提供了用于治疗此类病症的药物组合物和方法，以及使用这些配体检测组胺H3受体的方法（例如受体定位研究）。

    PYRAZOLYLMETHYL HETEROARYL DERIVATIVES
    9.
    发明公开
    PYRAZOLYLMETHYL HETEROARYL DERIVATIVES 审中-公开
    吡唑基，HETEROARYLDERIVATE

    公开(公告)号：EP1807417A2

    公开(公告)日：2007-07-18

    申请号：EP05825135.6

    申请日：2005-11-01

    申请人： NEUROGEN CORPORATION

    发明人： XU, Yuelian ,  XIE, Linghong ,  GAO, Yang ,  HAN, Bingsong ,  MAYNARD, George, D. ,  CHENARD, Bertrand, L. ,  LAN, Jiong

    IPC分类号： C07D401/14 ,  C07D403/14 ,  C07D231/28

    CPC分类号： G01N33/9426 ,  C07D401/14 ,  C07D417/14 ,  C07D487/04

    摘要： Compounds of Formula (I) are provided, as are methods for their preparation. The variables W, X, Y, Z, R5, R8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).

    IMIDAZOL-1-YLMETHYL PYRIDAZINE DERIVATIVES
    10.
    发明公开
    IMIDAZOL-1-YLMETHYL PYRIDAZINE DERIVATIVES 审中-公开
    咪唑烷-1-基甲基吡啶衍生物

    公开(公告)号：EP1549636A1

    公开(公告)日：2005-07-06

    申请号：EP03748416.9

    申请日：2003-10-06

    申请人： Neurogen Corporation

    发明人： XIE, Linghong ,  HAN, Bingson ,  XU, Yuelian ,  MAYNARD, George

    IPC分类号： C07D401/14 ,  C07D403/06 ,  C07D409/14 ,  A61K31/501 ,  A61P25/00

    CPC分类号： C07D409/14 ,  C07D401/14 ,  C07D403/06 ,  C07D417/14

    摘要： The invention provides imidazol-l-ylmethyl pyridazine derivatives of the Formula (I), that bind to GABAA receptors. In the above formula, R1, R2 R3, R4, R5, R6 and Ar are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).