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    • 4. 发明申请
    • THIAZOLYLMETHYL AND OXAZOLYLMETHYL HETEROARYL DERIVATIVES
    • 三唑基甲基和氧代甲基苯乙烯衍生物
    • WO2006093911A2
    • 2006-09-08
    • PCT/US2006006937
    • 2006-02-28
    • NEUROGEN CORPXU YUELIANXIE LINGHONG
    • XU YUELIANXIE LINGHONG
    • C07D487/04C07D413/14C07D417/14
    • Compounds of Formula: (I) are provided, as are methods for their preparation. The variables in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABA A 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 GABA A receptors (e.g., receptor localization studies).
    • 提供式(I)的化合物,以及它们的制备方法。 上述公式中的变量在此定义。 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)障碍,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。 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(例如受体定位研究)的方法。
    • 8. 发明申请
    • SUSTITUTED IMIDAZOLOPYRAZINE AND TRIAZOLOPYRAZINE DERIVATIVES: GABAA RECEPTOR LIGANDS
    • 不溶性咪唑并吡嗪和三唑并吡啶衍生物:GABAA受体配体
    • WO2004107863A1
    • 2004-12-16
    • PCT/US2004/013778
    • 2004-05-03
    • NEUROGEN CORPORATIONXU, YuelianHAN, BingsongXIE, Linghong
    • XU, YuelianHAN, BingsongXIE, Linghong
    • A01N43/58
    • C07D487/04G01N33/566
    • Compounds of Formula (I) are provided, as are methods for their preparation. The variables Z 1 , Z 2 , Z 3 , R 4 , R 5 , R 6 , R 7 , R 8 , and Ar in the above Formula are defined herein. Such compounds may be used to modulate ligand binding to GABA A 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 GABA A receptors ( e.g ., receptor localization studies).
    • 提供式(I)的化合物,以及它们的制备方法。 上述式中的变量Z1,Z2,Z3,R4,R5,R6,R7,R8和Ar如本文所定义。 此类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,家养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)。