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    4-aryl-2-anilino-pyrimidines
    1.
    发明授权
    4-aryl-2-anilino-pyrimidines 有权
    4-芳基-2-苯胺基 - 嘧啶

    公开(公告)号：US08318929B2

    公开(公告)日：2012-11-27

    申请号：US12921499

    申请日：2009-03-09

    申请人： Peter Jacobus Johannes Antonius Buijnsters ,  Marc Gustaaf Celine Verdonck ,  Kristof Van Emelen ,  Pascal Ghislain André Bonnet

    发明人： Peter Jacobus Johannes Antonius Buijnsters ,  Marc Gustaaf Celine Verdonck ,  Kristof Van Emelen ,  Pascal Ghislain André Bonnet

    IPC分类号： C07D345/00

    CPC分类号： C07D471/08 ,  C07D471/18 ,  C07D471/22 ,  C07D498/08 ,  C07D498/18

    摘要： The present invention relates to compounds of Formula (Ia) or (Ib), the N-oxide forms, pharmaceutically acceptable addition salts, quaternary amines, stereoisomers, tautomers, racemics, metabolites, prodrugs, hydrates, or solvates thereof, wherein Y1, m, n, R1; X1; X2; R2; X3; X4; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are kinase inhibitors useful for the treatment of disease states mediated by kinase, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.

    摘要翻译： 本发明涉及式（Ia）或（Ib）的化合物，N-氧化物形式，药学上可接受的加成盐，季胺，立体异构体，互变异构体，外消旋学，代谢物，前药，水合物或溶剂化物，其中Y1， ，n，R1; X1; X2; R2; X3; X4; R3; 和R4具有权利要求中限定的含义。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在治疗中的用途。 本发明特别涉及可用于治疗由激酶，特别是PLK4介导的疾病状态的激酶抑制剂的化合物，特别是可用于治疗涉及异常细胞增殖的病理过程的化合物，例如肿瘤生长，类风湿 关节炎，再狭窄和动脉粥样硬化。

    4-ARYL-2-ANILINO-PYRIMIDINES
    2.
    发明申请
    4-ARYL-2-ANILINO-PYRIMIDINES 有权

    公开(公告)号：US20110009404A1

    公开(公告)日：2011-01-13

    申请号：US12921499

    申请日：2009-03-09

    申请人： Peter Jacobus Johannes Buijnsters ,  Marc Gustaaf Celine Verdonck ,  Kristof Van Emelen ,  Pascal Ghislain André Bonnet

    发明人： Peter Jacobus Johannes Buijnsters ,  Marc Gustaaf Celine Verdonck ,  Kristof Van Emelen ,  Pascal Ghislain André Bonnet

    IPC分类号： A61K31/5377 ,  C07D487/14 ,  C07D487/04 ,  A61K31/519 ,  A61K31/496 ,  A61P35/00

    CPC分类号： C07D471/08 ,  C07D471/18 ,  C07D471/22 ,  C07D498/08 ,  C07D498/18

    摘要： The present invention relates to compounds of Formula (Ia) or (Ib), the N-oxide forms, pharmaceutically acceptable addition salts, quaternary amines, stereoisomers, tautomers, racemics, metabolites, prodrugs, hydrates, or solvates thereof, wherein Y1, m, n, R1; X1; X2; R2; X3; X4; R3; and R4 have the meaning defined in the claims.The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are kinase inhibitors useful for the treatment of disease states mediated by kinase, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.

    摘要翻译： 本发明涉及式（Ia）或（Ib）的化合物，N-氧化物形式，药学上可接受的加成盐，季胺，立体异构体，互变异构体，外消旋学，代谢物，前药，水合物或溶剂化物，其中Y1， ，n，R1; X1; X2; R2; X3; X4; R3; 和R4具有权利要求中限定的含义。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在治疗中的用途。 本发明特别涉及可用于治疗由激酶，特别是PLK4介导的疾病状态的激酶抑制剂的化合物，特别是可用于治疗涉及异常细胞增殖的病理过程的化合物，例如肿瘤生长，类风湿 关节炎，再狭窄和动脉粥样硬化。