IMIDAZO-PYRIMIDINES AND TRIAZOLO-PYRIMIDINES: BENZODIAZEPINE RECEPTOR LIGANDS
    3.
    发明申请
    IMIDAZO-PYRIMIDINES AND TRIAZOLO-PYRIMIDINES: BENZODIAZEPINE RECEPTOR LIGANDS 审中-公开
    咪唑并吡啶和三唑并嘧啶:苯并咪唑受体配体

    公开(公告)号:US20080139580A1

    公开(公告)日:2008-06-12

    申请号:US11855386

    申请日:2007-09-14

    CPC分类号: C07D487/04

    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: 提供了式I化合物,以及其制备方法。 变量Z 1,Z 2,Z 3,R 4,R 5,/或 >,R 6,R 7,R 8和Ar如上所定义。 这样的化合物可用于在体内或体外调节配体与GABA A A受体的结合,并且特别可用于治疗人类中的各种中枢神经系统(CNS)紊乱,驯养伴侣动物 和牲畜。 本文提供的化合物可以单独施用或与一种或多种其它CNS剂组合施用,以增强其它CNS剂的作用。 还提供了用于治疗这种病症的药物组合物和方法,以及使用这种配体检测GABA A受体的方法(例如,受体定位研究)。

    Pyrazolylmethy Heteroaryl Derivatives
    4.
    发明申请
    Pyrazolylmethy Heteroaryl Derivatives 审中-公开
    吡唑基甲基杂芳基衍生物

    公开(公告)号:US20080004269A1

    公开(公告)日:2008-01-03

    申请号:US11718528

    申请日:2005-11-01

    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 receptorsin 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)的化合物,以及它们的制备方法。 上式定义了上式中的变量W,X,Y,Z,R 5,R 8和Ar。 这样的化合物可用于在体内或体外调节配体与GABA A A受体的结合,并且特别可用于治疗人类中的各种中枢神经系统(CNS)障碍,驯养的伴侣动物和 牲畜。 本文提供的化合物可以单独施用或与一种或多种其它CNS剂组合施用,以增强其它CNS剂的作用。 还提供了用于治疗这种病症的药物组合物和方法,以及使用这种配体检测GABA A受体的方法(例如,受体定位研究)。

    Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands
    6.
    发明申请
    Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands 有权
    咪唑并 - 嘧啶和三唑并嘧啶:苯并二氮杂受体配体

    公开(公告)号:US20050038043A1

    公开(公告)日:2005-02-17

    申请号:US10898690

    申请日:2004-07-23

    IPC分类号: C07D487/04 A61K31/519

    CPC分类号: C07D487/04

    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: 提供了式I化合物,以及其制备方法。 上述式中的变量Z1,Z2,Z3,R4,R5,R6,R7,R8和Ar定义如下。 这样的化合物可用于在体内或体外调节配体与GABA A受体的结合,并且特别可用于治疗人,驯养的伴侣动物和家畜中的各种中枢神经系统(CNS)障碍。 本文提供的化合物可以单独施用或与一种或多种其它CNS剂组合施用,以增强其它CNS剂的作用。 还提供了用于治疗这种病症的药物组合物和方法,以及使用这种配体检测GABA A受体的方法(例如受体定位研究)。

    TETRAHYDROPYRIDO[3,4-D]PYRIMIDINES AND RELATED ANALOGUES
    8.
    发明申请
    TETRAHYDROPYRIDO[3,4-D]PYRIMIDINES AND RELATED ANALOGUES 审中-公开
    四氢吡咯并[3,4-D]吡嗪和相关的类似物

    公开(公告)号:US20080051387A1

    公开(公告)日:2008-02-28

    申请号:US11759929

    申请日:2007-06-07

    摘要: Tetrahydropyrido[3,4-d]pyrimidines and related analogues are provided, of the formula: 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 partially 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: 四氢吡啶并[3,4-d]嘧啶和相关的类似物具有下式:其中变量如本文所述,以及其制备和使用方法。 这样的化合物通常可用于在体内或体外调节配体与组胺H3受体的结合,并且部分可用于治疗人类,驯养的伴侣动物和家畜中的各种疾病。 提供药物组合物和治疗方法,以及使用这种配体检测组胺H3受体的方法(例如,受体定位研究)。

    Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands
    9.
    发明授权
    Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands 有权
    咪唑并 - 嘧啶和三唑并嘧啶:苯并二氮杂受体配体

    公开(公告)号:US07271170B2

    公开(公告)日:2007-09-18

    申请号:US10898690

    申请日:2004-07-23

    CPC分类号: C07D487/04

    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: 提供了式I化合物,以及其制备方法。 变量Z 1,Z 2,Z 3,R 4,R 5,/或 >,R 6,R 7,R 8和Ar如上所定义。 这样的化合物可用于在体内或体外调节配体与GABA A A受体的结合,并且特别可用于治疗人类中的各种中枢神经系统(CNS)紊乱,驯养伴侣动物 和牲畜。 本文提供的化合物可以单独施用或与一种或多种其它CNS剂组合施用,以增强其它CNS剂的作用。 还提供了用于治疗这种病症的药物组合物和方法,以及使用这种配体检测GABA A受体的方法(例如,受体定位研究)。