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    INHIBITORS OF BRUTON'S TYROSINE KINASE
    1.
    发明公开
    INHIBITORS OF BRUTON'S TYROSINE KINASE 有权
    酪氨酸激酶抑制剂

    公开(公告)号：EP2964627A1

    公开(公告)日：2016-01-13

    申请号：EP14707399.3

    申请日：2014-03-03

    申请人： F.Hoffmann-La Roche AG

    发明人： BROTHERTON-PLEISS, Christine E. ,  KONDRU, Rama K. ,  LOPEZ-TAPIA, Francisco Javier ,  LOU, Yan

    IPC分类号： C07D401/14

    CPC分类号： C07D401/14 ,  A61K31/502 ,  C07D237/32

    摘要： This application discloses compounds according to generic Formula I: (I) wherein all variables 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 Formula I and at least one carrier, diluent or excipient.

    摘要翻译： 该申请公开了根据通式I的化合物：（I）其中所有变量如本文所述定义，其抑制BTK。 本文公开的化合物可用于调节BTK的活性并治疗与过度BTK活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎性和自身免疫疾病，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。

    NOVEL PHENYLIMIDAZOPYRAZINES
    2.
    发明公开
    NOVEL PHENYLIMIDAZOPYRAZINES 有权
    新的苯基咪唑并吡嗪类

    公开(公告)号：EP2307418A1

    公开(公告)日：2011-04-13

    申请号：EP09780304.3

    申请日：2009-07-08

    申请人： F.Hoffmann-La Roche AG

    发明人： KONDRU, Rama K. ,  LOU, Yan ,  SJOGREN, Eric Brian ,  SOTH, Michael

    IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K31/517 ,  A61P37/00 ,  A61P29/00

    CPC分类号： C07D487/04

    摘要： 6-Phenyl-imidazo[l,2-a]pyrazine derivatives according to generic Formulae I-V: wherein variables Q, R, Y
    1 , Y
    2 , Y
    3 , Y
    4 , 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-V and at least one carrier, diluent or excipient.

    摘要翻译： 根据通式IV的6-苯基 - 咪唑并[1,2-a]吡嗪衍生物：其中变量Q，R，Y 1，Y 2，Y 3，Y 4，n和m如本文所述定义， BTK。 本文公开的化合物可用于调节Btk的活性并治疗与过度Btk活性相关的疾病。 该化合物还可用于治疗与异常B细胞增殖相关的炎性和自身免疫疾病，如类风湿性关节炎。 还公开了包含式I-V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
    7.
    发明公开
    INHIBITORS OF BRUTON'S TYROSINE KINASE 有权
    布鲁顿酪氨酸激酶抑制剂

    公开(公告)号：EP2421854A1

    公开(公告)日：2012-02-29

    申请号：EP10714295.2

    申请日：2010-04-21

    申请人： F.Hoffmann-La Roche AG

    发明人： DEWDNEY, Nolan James ,  HAWLEY, Ronald Charles ,  KONDRU, Rama K. ,  LAI, Yingjie ,  LOU, Yan

    IPC分类号： C07D403/14 ,  C07D413/14 ,  A61K31/5513 ,  A61K31/553 ,  A61P29/00

    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 Formula A wherein, variables Z* or Q
    1 , Q
    2 , Y
    3 , Y
    4 , Y
    5 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 containing compounds of Formula A and at least one carrier, diluent or excipient.