INHIBITORS OF BRUTON'S TYROSINE KINASE
    9.
    发明公开
    INHIBITORS OF BRUTON'S TYROSINE KINASE 审中-公开
    HEMMER DER BRUTON-TYROSINKINASE

    公开(公告)号:EP2925740A4

    公开(公告)日:2016-06-08

    申请号:EP13858966

    申请日:2013-11-29

    摘要: The invention provides novel poly-substituted 5-membered heterocyclic compounds represented by Formula (IV), or a pharmaceutically acceptable salt, solvate, metabolites, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as selective irreversible bruton's tyrosine kinase (Btk) inhibitors and is further useful to treat inflammatory, auto immune diseases associated with aberrant B-cell proliferation such as RA (rheumatoid arthritis) and cancers. This invention also provided the preparation of a medicament using of Formula (IV), and methods of preventing or treating diseases associated with excessive Btk activity in mammals, especially humans. Formula (IV)

    摘要翻译: 本发明提供由式(IV)表示的新型多取代五元杂环化合物或其药学上可接受的盐,溶剂合物,代谢物,多晶型物,酯,互变异构体或前药,以及包含这些化合物的组合物。 所提供的化合物可用作选择性不可逆的布鲁特酪氨酸激酶(Btk)抑制剂,并且还可用于治疗与异常B细胞增殖(例如RA(类风湿性关节炎)和癌症)相关的炎性,自身免疫疾病。 本发明还提供了使用式(IV)的药物的制备,以及用于预防或治疗与哺乳动物尤其是人类中过量Btk活性相关的疾病的方法。 式(IV)