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281 条记录 (耗时 0.038 秒)

    Bicyclic and tricyclic heteroaromatic compounds
    12.
    发明申请
    Bicyclic and tricyclic heteroaromatic compounds 失效
    双环和三环杂芳族化合物

    公开(公告)号：US20060217384A1

    公开(公告)日：2006-09-28

    申请号：US11442812

    申请日：2006-05-30

    申请人： Jun Yuan ,  Pamela Albaugh ,  Kenneth Shaw ,  Alan Hutchison

    发明人： Jun Yuan ,  Pamela Albaugh ,  Kenneth Shaw ,  Alan Hutchison

    IPC分类号： C07D487/04 ,  A61K31/503 ,  A61K31/4745

    CPC分类号： C07D217/26 ,  C07D237/30 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  G01N2333/70571

    摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.

    摘要翻译： 公开了下式的化合物及其药学上可接受的盐，其中W，Q，X，X 1，Y和Z如本文所定义。 这些化合物以高选择性和/或高亲和力结合GABA A A受体的苯并二氮杂位点，因此可用于治疗中枢神经系统（CNS）疾病和用作GABA < 组织样品中的受体。 还公开了可用于制备这些化合物的中间体。

    Bicyclic and tricyclic hetroaromatic compounds
    13.
    发明授权
    Bicyclic and tricyclic hetroaromatic compounds 失效
    双环和三环杂芳族化合物

    公开(公告)号：US07053093B2

    公开(公告)日：2006-05-30

    申请号：US10352519

    申请日：2003-01-28

    申请人： Jun Yuan ,  Pamela Albaugh ,  Kenneth Shaw ,  Alan Hutchison

    发明人： Jun Yuan ,  Pamela Albaugh ,  Kenneth Shaw ,  Alan Hutchison

    IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K25/24 ,  A61P25/22

    CPC分类号： C07D217/26 ,  C07D237/30 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  G01N2333/70571

    摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.

    摘要翻译： 公开了下式的化合物及其药学上可接受的盐，其中W，Q，X，X 1，Y和Z如本文所定义。 这些化合物以高选择性和/或高亲和力结合GABA A A受体的苯并二氮杂位点，因此可用于治疗中枢神经系统（CNS）疾病和用作GABA < 组织样品中的受体。 还公开了可用于制备这些化合物的中间体。

    Heteroaryl substituted fused bicyclic heteroaryl compounds as GABAA receptor ligands
    14.
    发明申请
    Heteroaryl substituted fused bicyclic heteroaryl compounds as GABAA receptor ligands 审中-公开
    杂芳基取代的稠合双环杂芳基化合物作为GABA A受体配体

    公开(公告)号：US20060014746A1

    公开(公告)日：2006-01-19

    申请号：US11214345

    申请日：2005-08-29

    申请人： Alan Hutchison ,  George Maynard ,  Pamela Albaugh ,  Linghong Xie ,  Jun Yuan ,  Scott Mitchell ,  Vinod Singh ,  Manuka Ghosh ,  Guiying Li ,  Nian Liu

    发明人： Alan Hutchison ,  George Maynard ,  Pamela Albaugh ,  Linghong Xie ,  Jun Yuan ,  Scott Mitchell ,  Vinod Singh ,  Manuka Ghosh ,  Guiying Li ,  Nian Liu

    IPC分类号： C07D487/04 ,  C07D471/02 ,  A61K31/519 ,  A61K31/503 ,  A61K31/4745

    CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D513/04

    摘要： This invention relates to heteroaryl substituted fused bicyclic heteroaryl compounds, such as heteroaryl substituted imidazopyridines, imidazopyrazines, imidazopyridizines, imidazopyrimidines, and imidazothiazoles, which may be described by Formula I or Formula II: The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Processes for preparing compounds of Formula I and Formula II are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I or Formula II in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.

    摘要翻译： 本发明涉及可以由式I或式II描述的杂芳基取代的稠合双环杂芳基化合物，例如杂芳基取代的咪唑并吡啶，咪唑并吡嗪，咪唑并吡啶，咪唑并嘧啶和咪唑并噻唑。本发明特别涉及以高选择性结合的这些化合物 并且对GABA A A受体的苯并二氮杂位点具有高亲和力。 本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗某些中枢神经系统（CNS）疾病中的用途。 公开了制备式I和式II化合物的方法。 本发明还涉及式I或式II的苯并咪唑，吡啶基咪唑和相关双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。 此外，本发明涉及使用这些化合物作为组织切片中GABA A A受体定位的探针。

    Bicyclic and tricyclic heteroaromatic compounds
    16.
    发明授权
    Bicyclic and tricyclic heteroaromatic compounds 失效
    双环和三环杂芳族化合物

    公开(公告)号：US06511987B1

    公开(公告)日：2003-01-28

    申请号：US09709887

    申请日：2000-11-10

    申请人： Jun Yuan ,  Pamela Albaugh ,  Kenneth Shaw ,  Alan Hutchinson

    发明人： Jun Yuan ,  Pamela Albaugh ,  Kenneth Shaw ,  Alan Hutchinson

    IPC分类号： C07D47104

    CPC分类号： C07D217/26 ,  C07D237/30 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  G01N2333/70571

    摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.

    摘要翻译： 公开了下式的化合物及其药学上可接受的盐，其中W，Q，X，X 1，Y和Z如本文所定义。 这些化合物以高选择性和/或高亲和力结合GABA A受体的苯并二氮杂位点，因此可用于治疗中枢神经系统（CNS）疾病和作为组织样品中GABA A受体定位的探针。 还公开了可用于制备这些化合物的中间体。

    Substituted ring-fused imidazole derivative: GABAA receptors ligands
    19.
    发明授权
    Substituted ring-fused imidazole derivative: GABAA receptors ligands 失效
    取代的环稠合咪唑衍生物：GABA A受体配体

    公开(公告)号：US06916827B2

    公开(公告)日：2005-07-12

    申请号：US10438496

    申请日：2003-05-15

    申请人： George D. Maynard ,  Jun Yuan ,  George P. Luke ,  Kevin Currie

    发明人： George D. Maynard ,  Jun Yuan ,  George P. Luke ,  Kevin Currie

    IPC分类号： A61P25/00 ,  C07D471/04 ,  A61K31/437 ,  A61K31/4184 ,  A61K31/506 ,  C07D403/06

    CPC分类号： C07D471/04

    摘要： Substituted ring-fused imidazole derivatives that bind to GABAA receptors are provided. 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： 提供了与GABA A A受体结合的取代的环稠合咪唑衍生物。 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）。

    Aryl fused 2,4-disubstituted pyridines: NK3 receptor ligands
    20.
    发明申请
    Aryl fused 2,4-disubstituted pyridines: NK3 receptor ligands 审中-公开

    公开(公告)号：US20060142324A1

    公开(公告)日：2006-06-29

    申请号：US11355439

    申请日：2006-02-15

    申请人： Jun Yuan ,  George Maynard ,  Alan Hutchison

    发明人： Jun Yuan ,  George Maynard ,  Alan Hutchison

    IPC分类号： A61K31/4745 ,  C07D471/02

    CPC分类号： C07D471/04 ,  C07D495/04

    摘要： Disclosed are compounds of formula (I) or pharmaceutically acceptable non-toxic salts or pharmaceutically acceptable solvates thereof wherein: (II) represents (a), (b), (c) or (d) and W, X, Y, A, B, C, D, E are variables as described herein. These compounds are highly selective agonists or antagonists at NK3 receptors or prodrugs thereof. The novel tachykinin NK-3 receptor antagonists contained in this invention have potential utility in the treatment of a broad array of disorders and diseases of the central nervous system (CNS) and periphery in mammals in which activation of NK-3 receptors is of importance.