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15 条记录 (耗时 0.045 秒)

    HMG-CoA reductase inhibitors
    2.
    发明申请
    HMG-CoA reductase inhibitors 有权
    HMG-CoA还原酶抑制剂

    公开(公告)号：US20070249583A1

    公开(公告)日：2007-10-25

    申请号：US11789335

    申请日：2007-04-24

    申请人： Philip D. Stein ,  Steven P. Seitz ,  David J. Carini ,  Yan Shi ,  Jeffrey A. Robl ,  Jay A. Markwalder ,  Chunhong He

    发明人： Philip D. Stein ,  Steven P. Seitz ,  David J. Carini ,  Yan Shi ,  Jeffrey A. Robl ,  Jay A. Markwalder ,  Chunhong He

    IPC分类号： A61K31/553 ,  A61K31/55 ,  A61K31/473

    CPC分类号： C07D221/16 ,  C07D471/04

    摘要： Compounds are provided of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia and dyslipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis wherein A is chosen from B is chosen from wherein the variables R1 to R7, m, n, are as defined herein.A method for treating the above diseases employing the above compounds is also provided.

    摘要翻译： 提供以下结构的化合物是HMG CoA还原酶抑制剂，因此有效抑制胆固醇生物合成，调节血清脂质，例如降低LDL胆固醇和/或增加HDL胆固醇，以及治疗高脂血症和血脂异常，高胆固醇血症，高甘油三酯血症和动脉粥样硬化 其中A选自B，其中变量R 1至R 7，m，n，如本文所定义。 还提供了使用上述化合物治疗上述疾病的方法。

    6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
    4.
    发明授权
    6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as cyclin dependent kinase inhibitors 有权
    6-取代的吡唑并[3,4-d]嘧啶-4-酮可用作细胞周期蛋白依赖性激酶抑制剂

    公开(公告)号：US06559152B2

    公开(公告)日：2003-05-06

    申请号：US09794825

    申请日：2001-02-27

    申请人： Jay A. Markwalder ,  Steven P. Seitz ,  Susan R. Sherk

    发明人： Jay A. Markwalder ,  Steven P. Seitz ,  Susan R. Sherk

    IPC分类号： A61K31519

    CPC分类号： C07D487/04 ,  C07D471/04

    摘要： The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

    摘要翻译： 本发明涉及新型的式（I）吡唑并[3,4-d]嘧啶-4-酮的合成，或者由互变异构体（II）表示：已知的酶类的有效抑制剂 作为细胞周期蛋白依赖性激酶，其涉及催化亚单位细胞周期蛋白依赖性激酶1-8及其调节亚基，其被称为细胞周期蛋白AH，K，N和T.本发明还提供了一种通过施用治疗癌症或其它增殖性疾病的新方法 治疗有效量的这些化合物之一或其药学上可接受的盐形式。 或者，可以通过施用本发明的一种化合物和一种或多种其它已知的抗癌或抗增殖剂的治疗有效组合来治疗癌症或其它增殖性疾病。

    6-substituted pyrazolo [3,4-d] pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
    5.
    发明授权
    6-substituted pyrazolo [3,4-d] pyrimidin-4-ones useful as cyclin dependent kinase inhibitors 有权
    6-取代的吡唑并[3,4-d]嘧啶-4-酮可用作细胞周期蛋白依赖性激酶抑制剂

    公开(公告)号：US06531477B1

    公开(公告)日：2003-03-11

    申请号：US09416584

    申请日：1999-10-12

    申请人： Jay A. Markwalder ,  Steven P. Seitz ,  Susan R. Sherk

    发明人： Jay A. Markwalder ,  Steven P. Seitz ,  Susan R. Sherk

    IPC分类号： A61K31519

    CPC分类号： C07D471/04

    摘要： The present invention relates to the synthesis of a novel class of pyrazolo[3,4-d]pyrimidin-4-ones of formula (I), alternatively represented by the tautomer (II): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cyclin dependent kinase 1-8 and their regulatory subunits know as cyclins A-H, K, N, and T. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

    摘要翻译： 本发明涉及新型的式（I）吡唑并[3,4-d]嘧啶-4-酮的合成，或者由互变异构体（II）表示：已知的酶类的有效抑制剂 作为细胞周期蛋白依赖性激酶，其涉及催化亚单位细胞周期蛋白依赖性激酶1-8及其调节亚基，其被称为细胞周期蛋白AH，K，N和T.本发明还提供了一种通过施用治疗癌症或其它增殖性疾病的新方法 治疗有效量的这些化合物之一或其药学上可接受的盐形式。 或者，可以通过施用本发明的一种化合物和一种或多种其它已知的抗癌或抗增殖剂的治疗有效组合来治疗癌症或其它增殖性疾病。

    Unsymmetrical bis-imides as anticancer agents
    7.
    发明授权
    Unsymmetrical bis-imides as anticancer agents 失效
    不对称双酰亚胺作为抗癌剂

    公开(公告)号：US5359070A

    公开(公告)日：1994-10-25

    申请号：US16555

    申请日：1993-02-11

    申请人： Robert J. Cherney ,  Steven P. Seitz

    发明人： Robert J. Cherney ,  Steven P. Seitz

    IPC分类号： C07D221/14 ,  A61K31/435 ,  A61P35/00 ,  C07D221/18

    CPC分类号： C07D221/18

    摘要： This invention relates to unsymmetrical bis-imide compounds, and pharmaceutically acceptable salts thereof, of the formula (i): ##STR1## including (R,R)-1-[2-(acenaphthene-5,6-dicarboximido) propylamino]-2-[2-(3-nitronaphthalene-1,8-dicarboximido) propylamino]ethane, processes for the preparation of such compounds, pharmaceutical compositions containing such compounds, and methods of using such compounds to treat cancer, particularly solid tumor carcinomas, in mammals.

    摘要翻译： 本发明涉及式（i）的不对称双酰亚胺化合物及其药学上可接受的盐：（i）包括（R，R）-1- [2-（苊-5-甲酰脒基） 丙基氨基] -2- [2-（3-硝基萘-1,8-二羧酰亚氨基）丙基氨基]乙烷，制备这些化合物的方法，含有这些化合物的药物组合物，以及使用这些化合物治疗癌症，特别是实体瘤的方法 癌，哺乳动物。