PTERIDINONES AS KINASE INHIBITORS
    1.
    发明申请
    PTERIDINONES AS KINASE INHIBITORS 审中-公开
    西替尼嗪作为激酶抑制剂

    公开(公告)号:US20070049600A1

    公开(公告)日:2007-03-01

    申请号:US11553935

    申请日:2006-10-27

    IPC分类号: C07D475/02 A61K31/525

    CPC分类号: C07D475/00

    摘要: Disclosed are compounds of the formula wherein: W is NH, S, SO, or SO2; R2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle; Q is hydrogen or lower alkyl; R4 and R6 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl; and R8 is hydrogen, lower alkyl or an (un)substituted carbocyclic group containing from 3-7 members, up to two of which members are optionally hetero atoms selected from oxygen and nitrogen; or R8 is (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl. These compounds are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The present invention also provides a method of treating cell proliferative disorders. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula I.

    摘要翻译: 公开了下式的化合物其中:W是NH,S,SO或SO 2; R 2是(未)取代的芳基,(未)取代的杂芳基或(取代的)取代的碳环或杂环; Q是氢或低级烷基; R 4和R 6相同或不同,表示氢,卤素,低级烷基,低级烷氧基,(未)取代的芳基,(未)取代的杂芳基,(un )取代的芳基烷基或(未)取代的杂芳基烷基; 和R 8是氢,低级烷基或含有3-7个成员的(未)取代的碳环,其中至多两个成员任选是选自氧和氮的杂原子; 或(R 8)是(un)取代的芳基,(未)取代的杂芳基,(未)取代的芳基烷基或(未)取代的杂芳基烷基。 这些化合物可用于治疗细胞增殖性疾病,如癌症和再狭窄。 这些化合物是细胞周期蛋白依赖性激酶(cdks)和生长因子介导的激酶的有效抑制剂。 本发明还提供了治疗细胞增殖性疾病的方法。 本发明还提供了含有式I化合物的药学上可接受的组合物。

    Pteridinones as kinase inhibitors
    2.
    发明授权
    Pteridinones as kinase inhibitors 失效
    蝶啶酮作为激酶抑制剂

    公开(公告)号:US07169778B2

    公开(公告)日:2007-01-30

    申请号:US10070530

    申请日:2000-06-21

    IPC分类号: A61K31/535 C07D475/00

    CPC分类号: C07D475/00

    摘要: Disclosed are compounds of Formulae (Ia), (Ib), (Ic), (Id) wherein: W is NH, S, SO, or SO2; R2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle; Q is hydrogen or lower alkyl; R4 and R6 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl; and R8 is hydrogen, lower alkyl or an (un)substituted carbocyclic group containing from 3–7 members, up to two of which members are optionally hetero atoms selected from oxygen and nitrogen; or R8 is (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl. These compounds are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The present invention also provides a method of treating cell proliferative disorders. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula (I).

    摘要翻译: 公开了式(Ia),(Ib),(Ic),(Id)的化合物,其中:W是NH,S,SO或SO 2; R 2是(未)取代的芳基,(未)取代的杂芳基或(取代的)取代的碳环或杂环; Q是氢或低级烷基; R 4和R 6相同或不同,表示氢,卤素,低级烷基,低级烷氧基,(未)取代的芳基,(未)取代的杂芳基,(un )取代的芳基烷基或(未)取代的杂芳基烷基; 和R 8是氢,低级烷基或含有3-7个成员的(未)取代的碳环,其中至多两个成员任选是选自氧和氮的杂原子; 或(R 8)是(un)取代的芳基,(未)取代的杂芳基,(未)取代的芳基烷基或(未)取代的杂芳基烷基。 这些化合物可用于治疗细胞增殖性疾病,如癌症和再狭窄。 这些化合物是细胞周期蛋白依赖性激酶(cdks)和生长因子介导的激酶的有效抑制剂。 本发明还提供了治疗细胞增殖性疾病的方法。 本发明还提供含有式(I)化合物的药学上可接受的组合物。