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    • 2. 发明授权
    • 3,5 phenyl-substituted beta amino acid derivatives as integrin antagonists
    • 3,5-苯基取代的β氨基酸衍生物作为整联蛋白拮抗剂
    • US08716226B2
    • 2014-05-06
    • US13944319
    • 2013-07-17
    • Saint Louis University
    • Peter RuminskiDavid Griggs
    • A61K38/36
    • C07D239/14
    • Disclosed herein are novel pharmaceutical agents which are useful as integrin receptor antagonists that mediate the pathologic processes of angiogenesis and fibrosis and as such are useful in pharmaceutical compositions and in methods for treating conditions mediated by these integrins by inhibiting or antagonizing these integrins. The novel pharmaceutical agents include those of the formula: wherein X is bromo or iodo, or pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods and intermediates useful for making the pharmaceutical agents and methods of using the pharmaceutical agents are also provided.
    • 本文公开了可用作介导血管生成和纤维化的病理过程的整联蛋白受体拮抗剂的新型药剂,因此可用于药物组合物和通过抑制或拮抗这些整联蛋白来治疗由这些整联蛋白介导的病症的方法。 新型药剂包括下式的那些:其中X是溴或碘,或其药学上可接受的盐。 还提供了包含这种药剂的药物组合物,试剂盒和制品。 还提供了可用于制备药剂的方法和中间体以及使用药剂的方法。