Inhibitors of Bruton's tyrosine kinase
    8.
    发明授权
    Inhibitors of Bruton's tyrosine kinase 有权
    Bruton酪氨酸激酶抑制剂

    公开(公告)号:US08318719B2

    公开(公告)日:2012-11-27

    申请号:US12765904

    申请日:2010-04-23

    CPC分类号: C07D413/14 C07D403/14

    摘要: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-II: wherein, variables Q1, Q2, R, X, Y1, Y2, Y2′, Y3, Y4, Y5, m, and p are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-II and at least one carrier, diluent or excipient.

    摘要翻译: 本申请公开了根据通式I-II的5-苯基-1H-吡啶-2-酮,6-苯基-2H-哒嗪-3-酮和5-苯基-1H-吡嗪-2-酮衍生物:其中, 变量Q1,Q2,R,X,Y1,Y2,Y2',Y3,Y4,Y5,m和p如本文所述限定Btk。 本文公开的化合物可用于调节Btk的活性并治疗与过量Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病,例如类风湿性关节炎。 还公开了含有式I-II化合物和至少一种载体,稀释剂或赋形剂的组合物。