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    1-aryl-4-substituted isoquinolines
    1.
    发明授权
    1-aryl-4-substituted isoquinolines 失效
    1-芳基-4-取代的异喹啉

    公开(公告)号：US07915288B2

    公开(公告)日：2011-03-29

    申请号：US11587906

    申请日：2005-05-06

    申请人： Kyungae Lee ,  Jun Yuan ,  George D. Maynard ,  Alan Hutchison ,  Scott Mitchell

    发明人： Kyungae Lee ,  Jun Yuan ,  George D. Maynard ,  Alan Hutchison ,  Scott Mitchell

    IPC分类号： C07D217/02 ,  A61K31/47

    CPC分类号： C07D405/12 ,  A61K31/47 ,  C07D217/14 ,  C07D217/16 ,  C07D217/22 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D413/14

    摘要： 1-aryl-4-substituted isoquinoline or 1-aryl-3,4-disubstituted isoquinoline analogues of Formula I and Formula II, as follows: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II 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 1-aryl-4-substituted isoquinolines or 1-aryl-3,4-disubstituted isoquinolines, which are useful as probes for the localization of C5a receptors.

    摘要翻译： 式I和式II的1-芳基-4-取代的异喹啉或1-芳基-3,4-二取代的异喹啉类似物如下：其中R1，R2，R3，R8，R9，A和Ar如本文所定义。 这些化合物是C5a受体的配体。 优选的式I和II化合物以高亲和力结合C5a受体，并在C5a受体上呈现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，本发明提供标记的1-芳基-4-取代的异喹啉或1-芳基-3,4-二取代的异喹啉，其可用作C5a受体定位的探针。

    Heteroaryl substituted fused bicyclic heteroaryl compounds as GABAA receptor ligands
    9.
    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。