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    Purine inhibitors of cyclin dependent kinase 2 and IκB-α
    52.
    发明授权
    Purine inhibitors of cyclin dependent kinase 2 and IκB-α 失效
    细胞周期蛋白依赖性激酶2和IkappaB-α的嘌呤抑制剂

    公开(公告)号：US07109330B2

    公开(公告)日：2006-09-19

    申请号：US10794828

    申请日：2004-03-03

    申请人： Robert Lum ,  Cheri Lynn Blum ,  Richard Mackman ,  Michael Wick ,  Steven Schow ,  Jeff Zablocki ,  Prabha Ibrahim

    发明人： Robert Lum ,  Cheri Lynn Blum ,  Richard Mackman ,  Michael Wick ,  Steven Schow ,  Jeff Zablocki ,  Prabha Ibrahim

    IPC分类号： C07D473/16 ,  C07D473/40 ,  A61K31/53 ,  A61P35/00 ,  A61P3/10

    CPC分类号： B60R1/00 ,  C07D473/16 ,  C07D473/40 ,  G08G1/163

    摘要： Compounds of the following formula are provided: In the Formula (I), R1 is —X—R1′; in which R1′ is optionally substituted lower alkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocyclyl, and X is —NH—. R2 is lower alkyl optionally substituted with one, two or three groups chosen from hydroxy, lower alkoxy, and halogen. And R3 is —NR4R5; in which R4 is hydrogen and R5 is lower alkyl substituted with amino; or (ii) R4 and R5 are both lower alkyl optionally substituted with one, two or three groups chosen from hydroxy and amino. It is to be understood that R1′ is not cyclohexylmethyl, phenyl, substituted phenyl, benzyl, phenylethyl, or m-hydroxybenzyl. The compounds inhibit CDK-2 activity and are useful for treating disorders characterized by undesirable cell proliferation.

    摘要翻译： 提供下式的化合物：在式（I）中，R 1是-X-R 1'; 其中R 1'是任选取代的低级烷基，任选取代的芳基，任选取代的杂芳基或任选取代的杂环基，X是-NH-。 R 2是任选被一个，两个或三个选自羟基，低级烷氧基和卤素的基团取代的低级烷基。 并且R 3是-NR 4 R 5; 其中R 4是氢，R 5是被氨基取代的低级烷基; 或（ii）R 4和R 5均为任选被一个，两个或三个选自羟基和氨基的基团取代的低级烷基。 应当理解，R 1不是环己基甲基，苯基，取代的苯基，苄基，苯乙基或间羟基苄基。 该化合物抑制CDK-2活性，并且可用于治疗以不期望的细胞增殖为特征的疾病。