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8 条记录 (耗时 0.018 秒)

    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
    7.
    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。

    Tripeptide and tetrapeptide sulfones
    8.
    发明申请
    Tripeptide and tetrapeptide sulfones 失效
    三肽和四肽砜

    公开(公告)号：US20060148719A1

    公开(公告)日：2006-07-06

    申请号：US11326975

    申请日：2006-01-05

    申请人： Steven Schow

    发明人： Steven Schow

    IPC分类号： A61K38/05 ,  A61K38/04

    CPC分类号： C07K5/0215 ,  A61K38/00

    摘要： Tripeptide and tetrapeptide sulfones, pharmaceutical compositions containing them, their pharmaceutical use, and their preparation. The compounds are useful in potentiating the cytotoxic effects of chemotherapeutic agents in tumor cells, selectively exerting toxicity in tumor cells, elevating the production of GM progenitors in bone marrow cells, stimulating the differentiation of bone marrow, mitigating the myelosuppressive effects of chemotherapeutic agents, and modulating hematopoiesis in bone marrow.

    摘要翻译： 三肽和四肽砜，含有它们的药物组合物，其药物用途及其制备。 这些化合物可用于增强化疗药物在肿瘤细胞中的细胞毒性作用，选择性地在肿瘤细胞中发挥毒性，提高骨髓细胞中转基因祖细胞的产生，刺激骨髓分化，减轻化疗药物的骨髓抑制作用，以及 调节骨髓造血功能。