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    PYRROLO-PYRIDINE, PYRROLO-PYRIMIDINE AND RELATED HETEROCYCLIC COMPOUNDS
    11.
    发明申请
    PYRROLO-PYRIDINE, PYRROLO-PYRIMIDINE AND RELATED HETEROCYCLIC COMPOUNDS 失效
    吡咯并吡啶，吡咯并吡啶和相关的杂环化合物

    公开(公告)号：US20110118273A1

    公开(公告)日：2011-05-19

    申请号：US13014066

    申请日：2011-01-26

    Applicant: Jun Yuan ,  Peter Hrnciar ,  Qin Guo ,  George D. Maynard

    Inventor： Jun Yuan ,  Peter Hrnciar ,  Qin Guo ,  George D. Maynard

    IPC: A61K31/519 ,  C07D487/04 ,  A61P29/00 ,  A61P37/00 ,  A61P37/06 ,  A61P11/06 ,  A61P17/06 ,  A61P25/28 ,  A61P25/00 ,  A61P11/00 ,  A61P9/10 ,  A61P13/12 ,  A61P27/02 ,  A61P31/18

    CPC classification number: C07D471/04

    Abstract: Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.

    Abstract translation: 吡咯并 - 吡啶，吡咯并 - 嘧啶和相关的杂环化合物，其分子式如下：其中R，R 2，R 5，E，Z 1，Z 3，Z 4和Ar如本文所定义。 这些化合物是C5a受体的配体。 本发明优选的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物以高亲和力结合C5a受体，并在C5a受体上表现出中性拮抗剂或反向激动剂活性。 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各种炎性，心血管和免疫系统疾病中的用途。 此外，本发明提供了标记的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物，其可用作C5a受体定位的探针。

    Imidazo-Pyridazines, Triazolo-Pyridazines and Related Benzodiazepine Receptor Ligands
    14.
    发明申请
    Imidazo-Pyridazines, Triazolo-Pyridazines and Related Benzodiazepine Receptor Ligands 审中-公开
    咪唑 - 哒嗪，三唑并哒嗪和相关苯并二氮杂受体配体

    公开(公告)号：US20090023737A1

    公开(公告)日：2009-01-22

    申请号：US10589095

    申请日：2005-02-09

    Applicant: Yuelian Xu ,  Bingsong Han ,  Linghong Xie ,  George D. Maynard

    Inventor： Yuelian Xu ,  Bingsong Han ,  Linghong Xie ,  George D. Maynard

    IPC: A61K31/5025 ,  C07D487/04 ,  A61P25/24 ,  A61P25/22

    CPC classification number: C07D487/04 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/53

    Abstract: Compounds of the Formula: are provided, as are methods for their preparation. The variables Z1, Z2, R3, Z4, 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).

    Abstract translation: 提供式的化合物：其制备方法。 上述式中的变量Z1，Z2，R3，Z4，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）。

    4-imidazol-1-ylmethyl-pyrimidine derivatives
    17.
    发明授权
    4-imidazol-1-ylmethyl-pyrimidine derivatives 失效
    4-咪唑-1-基甲基 - 嘧啶衍生物

    公开(公告)号：US06951864B2

    公开(公告)日：2005-10-04

    申请号：US10702629

    申请日：2003-11-06

    Applicant: Linghong Xie ,  Bingsong Han ,  Yuelian Xu ,  George D. Maynard

    Inventor： Linghong Xie ,  Bingsong Han ,  Yuelian Xu ,  George D. Maynard

    IPC: A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  C07D401/14 ,  C07D403/06 ,  C07D417/14 ,  A61K31/4178

    CPC classification number: C07D401/14 ,  C07D403/06 ,  C07D417/14

    Abstract: The invention provides 4-imidazol-1-ylmethyl pyrimidine of the formula 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).

    Abstract translation: 本发明提供了结合GABA A A受体的下式的4-咪唑-1-基甲基嘧啶。 在上式中，R 1，R 2，R 3，R 4，R 5， / SUB，R 6和Ar如本文所定义。 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）。

    Substituted ring-fused imidazole derivative: GABAA receptors ligands
    18.
    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

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

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

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

    CPC classification number: C07D471/04

    Abstract: 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).

    Abstract translation: 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）。

    1H-pyrrolo [3,2-b] pyridine-3-carboxylic acid amines as GABAA receptor ligands
    20.
    发明授权
    1H-pyrrolo [3,2-b] pyridine-3-carboxylic acid amines as GABAA receptor ligands 失效
    1H-吡咯并[3,2-b]吡啶-3-甲酸胺作为GABA A受体配体

    公开(公告)号：US06673811B1

    公开(公告)日：2004-01-06

    申请号：US10299199

    申请日：2002-11-19

    Applicant: George D. Maynard ,  Manuka Ghosh ,  Christopher J. O'Donnell

    Inventor： George D. Maynard ,  Manuka Ghosh ,  Christopher J. O'Donnell

    IPC: A61K314965

    CPC classification number: C07D471/04

    Abstract: Disclosed are 1H-Pyrrolo[3,2-b]pyridine-3-carboxylic acid amides that bind to the benzodiazepine site of GABAA receptors. Such compounds can be used to modulate ligand binding to GABAA receptors in vivo and 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.

    Abstract translation: 公开了结合GABA A受体的苯并二氮杂位点的1H-吡咯并[3,2-b]吡啶-3-羧酸酰胺。 这些化合物可用于体内和体外调节配体与GABA A受体的结合，并且特别可用于治疗人类，驯养的伴侣动物和家畜中的各种中枢神经系统（CNS）紊乱。

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