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    • 10. 发明授权
    • Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds
    • 吡咯并吡啶,吡咯并嘧啶和相关的杂环化合物
    • US08633193B2
    • 2014-01-21
    • US13014066
    • 2011-01-26
    • Jun YuanPeter HrnciarQin GuoGeorge D. Maynard
    • Jun YuanPeter HrnciarQin GuoGeorge D. Maynard
    • A61K31/519C07D487/04A61P37/00A61P37/06A61P11/06A61P17/06
    • C07D471/04
    • 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.
    • 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。