Inhibitors of bruton's tyrosine kinase
    3.
    发明授权
    Inhibitors of bruton's tyrosine kinase 有权
    布鲁特酪氨酸激酶抑制剂

    公开(公告)号:US08124604B2

    公开(公告)日:2012-02-28

    申请号:US12987187

    申请日:2011-01-10

    摘要: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y1, Y2, Y2′, Y3, Y4, n and m 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 comprising compounds of Formulae I-IV and at least one carrier, diluent or excipient.

    摘要翻译: 本申请公开了根据通式I-IV的5-苯基-1H-吡啶-2-酮和6-苯基-2H-哒嗪-3-酮衍生物:其中,变量R,X,Y 1,Y 2,Y 2',Y 3 ,Y4,n和m定义如本文所述,其抑制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。 还公开了包含式I-IV化合物和至少一种载体,稀释剂或赋形剂的组合物。

    Inhibitors of bruton's tyrosine kinase
    5.
    发明授权
    Inhibitors of bruton's tyrosine kinase 有权
    布鲁特酪氨酸激酶抑制剂

    公开(公告)号:US08618098B2

    公开(公告)日:2013-12-31

    申请号:US13358557

    申请日:2012-01-26

    IPC分类号: A61K31/5377 A61K31/517

    摘要: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y1, Y2, Y2′, Y3, Y4, n and m 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 comprising compounds of Formulae I-IV and at least one carrier, diluent or excipient.

    摘要翻译: 本申请公开了根据通式I-IV的5-苯基-1H-吡啶-2-酮和6-苯基-2H-哒嗪-3-酮衍生物:其中,变量R,X,Y 1,Y 2,Y 2',Y 3 ,Y4,n和m定义如本文所述,其抑制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。 还公开了包含式I-IV化合物和至少一种载体,稀释剂或赋形剂的组合物。

    Inhibitors of bruton's tyrosine kinase
    8.
    发明授权
    Inhibitors of bruton's tyrosine kinase 有权
    布鲁特酪氨酸激酶抑制剂

    公开(公告)号:US07902194B2

    公开(公告)日:2011-03-08

    申请号:US12456911

    申请日:2009-06-24

    IPC分类号: A61K31/502 C07D237/32

    摘要: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y1, Y2, Y2, Y3, Y4, n and m 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 comprising compounds of Formulae I-IV and at least one carrier, diluent or excipient.

    摘要翻译: 本申请公开了根据通式I-IV的5-苯基-1H-吡啶-2-酮和6-苯基-2H-哒嗪-3-酮衍生物:其中,变量R,X,Y 1,Y 2,Y 2,Y 3, Y4,n和m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。 还公开了包含式I-IV化合物和至少一种载体,稀释剂或赋形剂的组合物。

    Btk protein kinase inhibitors
    9.
    发明授权
    Btk protein kinase inhibitors 有权
    Btk蛋白激酶抑制剂

    公开(公告)号:US07943618B2

    公开(公告)日:2011-05-17

    申请号:US12288730

    申请日:2008-10-23

    IPC分类号: A61K31/50

    摘要: This application discloses pyridine and pyrimidine compounds according to formula I wherein R1, R2, R3, R4, R5, X1 and A are 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 formula I and at least one carrier, diluent or excipient.

    摘要翻译: 本申请公开了根据式I的吡啶和嘧啶化合物,其中R 1,R 2,R 3,R 4,R 5,X 1和A如本文所述抑制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化合物和至少一种载体,稀释剂或赋形剂的组合物。

    BTK protein kinase inhibitors
    10.
    发明申请
    BTK protein kinase inhibitors 有权
    BTK蛋白激酶抑制剂

    公开(公告)号:US20090105209A1

    公开(公告)日:2009-04-23

    申请号:US12288730

    申请日:2008-10-23

    摘要: This application discloses pyridine and pyrimidine compounds according to formula I wherein R1, R2, R3, R4, R5, X1 and A are 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 formula I and at least one carrier, diluent or excipient.

    摘要翻译: 本申请公开了根据式I的吡啶和嘧啶化合物,其中R 1,R 2,R 3,R 4,R 5,X 1和A如本文所述抑制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化合物和至少一种载体,稀释剂或赋形剂的组合物。