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    Purine inhibitors of cyclin dependent kinase 2 and IκB-α
    1.
    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。

    Purine inhibitors of cyclin dependent kinase 2 and IkappaB-alpha
    2.
    发明申请
    Purine inhibitors of cyclin dependent kinase 2 and IkappaB-alpha 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：US20050080261A1

    公开(公告)日：2005-04-14

    申请号：US10794828

    申请日：2004-03-03

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

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

    IPC分类号： B60R1/00 ,  C07D473/16 ,  C07D473/40 ,  G08G1/16 ,  C07D473/10 ,  C07D473/14

    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：式（I）中，R 1为-X-R 1'; 其中R 1'为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为-NH-。 R2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R4是氢，R5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，R1'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。

    Sensitization to another anticancer therapy and/or amelioration of a side effect of another anitcancer therapy by treatment with a GST-activated anticancer compound
    5.
    发明申请
    Sensitization to another anticancer therapy and/or amelioration of a side effect of another anitcancer therapy by treatment with a GST-activated anticancer compound 审中-公开
    通过用GST活化的抗癌化合物治疗对另一种抗癌疗法的敏化和/或改善另一种癌症治疗的副作用

    公开(公告)号：US20050261202A1

    公开(公告)日：2005-11-24

    申请号：US11133833

    申请日：2005-05-19

    申请人： Gail Brown ,  James Keck ,  Michael Wick

    发明人： Gail Brown ,  James Keck ,  Michael Wick

    IPC分类号： A61K38/04 ,  A61K38/05 ,  A61K38/06 ,  A61K45/06

    CPC分类号： A61K38/06 ,  A61K38/05 ,  A61K45/06 ,  A61K2300/00

    摘要： A method of sensitizing a mammal, especially a human, to another anticancer therapy by administering a sensitizing effective amount of a GST-activated anticancer compound. A method of ameliorating a side effect of another anticancer therapy in a mammal, especially a human, by administering an ameliorating effective amount of a GST-activated anticancer compound. Pharmaceutical compositions for the methods. The GST-activated anticancer compound is preferably a compound of U.S. Pat. No. 5,556,942, and more preferably canfosfamide, especially as the hydrochloride salt.

    摘要翻译： 通过施用敏化有效量的GST活化的抗癌化合物，使哺乳动物，特别是人对另一种抗癌疗法敏感的方法。 通过施用改善有效量的GST活化的抗癌化合物，改善哺乳动物，特别是人中另一种抗癌疗法的副作用的方法。 方法的药物组合物。 GST活化的抗癌化合物优选为美国专利No. 更优选地是卡夫酰胺，尤其是盐酸盐。