Pyrimidine derivatives and compositions as C-kit and PDGFR kinase inhibitors
    61.
    发明授权
    Pyrimidine derivatives and compositions as C-kit and PDGFR kinase inhibitors 失效
    嘧啶衍生物和组合物作为C-kit和PDGFR激酶抑制剂

    公开(公告)号:US08268850B2

    公开(公告)日:2012-09-18

    申请号:US12598919

    申请日:2008-05-01

    IPC分类号: C07D401/14 A61K31/444

    CPC分类号: C07D401/14 C07D405/14

    摘要: The invention provides a novel class of pyrimidine derivatives, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases.

    摘要翻译: 本发明提供了一类新颖的嘧啶衍生物,包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法,特别是涉及c-kit,PDGFRα异常活化的疾病或病症 和PDGFR&bgr; 激酶。

    Compositions and methods for modulating c-kit and PDGFR receptors
    62.
    发明授权
    Compositions and methods for modulating c-kit and PDGFR receptors 失效
    用于调节c-kit和PDGFR受体的组合物和方法

    公开(公告)号:US08106068B2

    公开(公告)日:2012-01-31

    申请号:US12629665

    申请日:2009-12-02

    CPC分类号: C07D471/04

    摘要: The invention provides compounds of Formula (2), and pharmaceutical compositions thereof, wherein R1, R2, R3, R4 and L are as described herein; as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFRα, PDGFRβ, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGFβ, SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2β, BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.

    摘要翻译: 本发明提供式(2)的化合物及其药物组合物,其中R1,R2,R3,R4和L如本文所述; 以及使用这些化合物治疗,改善或预防与异常或失调的激酶活性相关的病症的方法。 在一些实施方案中,本发明提供了使用这些化合物治疗,改善或预防涉及c-kit,PDGFRα,PDGFR和bgr,CSF1R,Abl,BCR-Abl,CSK,JNK1,JNK2,p38异常活化的疾病或病症的方法 ,p70S6K,TGF-bgr,SRC,EGFR,trkB,FGFR3,FLT3,Fes,Lck,Syk,RAF,MKK4,MKK6,SAPK2&bgr,BRK,KDR,c-raf或b-raf激酶或其突变形式。