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    NOVEL MODULATORS OF CELL CYCLE CHECKPOINTS AND THEIR USE IN COMBINATION WITH CHECKPOINT KINASE INHIBITORS
    32.
    发明申请
    NOVEL MODULATORS OF CELL CYCLE CHECKPOINTS AND THEIR USE IN COMBINATION WITH CHECKPOINT KINASE INHIBITORS 有权
    细胞周期调节因子的新型调节因子及其与检查点激酶抑制剂的组合使用

    公开(公告)号：US20110183933A1

    公开(公告)日：2011-07-28

    申请号：US12744021

    申请日：2008-11-05

    申请人： Timothy J. Guzi ,  David A. Parry ,  Marc A. Labroli ,  Michael P. Dwyer ,  Kamil Paruch

    发明人： Timothy J. Guzi ,  David A. Parry ,  Marc A. Labroli ,  Michael P. Dwyer ,  Kamil Paruch

    IPC分类号： A61K31/7072 ,  C07H19/06 ,  A61K31/7068 ,  A61P35/00 ,  A61P35/02

    CPC分类号： C07H19/067 ,  C07H19/073

    摘要： In its many embodiments, the present invention provides a novel class of pyrimidine analogs of formula (V) as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the activator as well as the combination and pharmaceutical kits.

    摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的式（V）嘧啶类似物作为细胞周期检查点的靶向基于机制的调节剂。 可以通过施用本发明的细胞周期检查点调节剂来治疗癌症和/或恶性肿瘤。 还讨论了细胞周期检查点调节剂与检查点激酶抑制剂的合适组合，以在癌细胞中产生协同凋亡。 本发明包括通过施用细胞周期检查点调节剂和检查点激酶抑制剂的组合，包含活化剂的药物组合物以及组合药物试剂盒来治疗癌症的方法。

    Pyrazolopyrimidines as protein kinase inhibitors
    34.
    发明授权
    Pyrazolopyrimidines as protein kinase inhibitors 有权
    吡唑并嘧啶作为蛋白激酶抑制剂

    公开(公告)号：US07449488B2

    公开(公告)日：2008-11-11

    申请号：US11244628

    申请日：2005-10-06

    申请人： Kamil Paruch ,  Timothy J. Guzi ,  Michael P. Dwyer ,  Gerald W. Shipps, Jr.

    发明人： Kamil Paruch ,  Timothy J. Guzi ,  Michael P. Dwyer ,  Gerald W. Shipps, Jr.

    IPC分类号： C07D231/00 ,  C07D231/54 ,  A61K31/415 ,  A01N43/56

    CPC分类号： C07D487/04

    摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions. The invention also relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.

    摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的吡唑并[1,5-a]嘧啶化合物作为蛋白质和/或检查点激酶的抑制剂，制备此类化合物的方法，包含一种或多种这类化合物的药物组合物， 制备包括一种或多种这样的化合物的药物制剂，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与蛋白质或检查点激酶相关的一种或多种疾病的方法。 本发明还涉及丙型肝炎病毒（HCV）复制的抑制。 特别地，本发明的实施方案提供了用于抑制HCV RNA依赖性RNA聚合酶酶活性的化合物和方法。 本发明还提供了预防和治疗HCV感染的组合物和方法。

    Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
    37.
    发明授权
    Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors 失效
    取代的吡唑并[1,5-a]嘧啶作为蛋白激酶抑制剂

    公开(公告)号：US07642266B2

    公开(公告)日：2010-01-05

    申请号：US11542852

    申请日：2006-10-04

    申请人： Timothy J. Guzi ,  Kamil Paruch ,  Michael P. Dwyer

    发明人： Timothy J. Guzi ,  Kamil Paruch ,  Michael P. Dwyer

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/04

    CPC分类号： C07D487/04

    摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a] pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions. An illustrative compound is shown below:

    摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的吡唑并[1,5-a]嘧啶化合物作为蛋白质和/或检查点激酶的抑制剂，制备此类化合物的方法，包含一种或多种这类化合物的药物组合物， 制备包括一种或多种这样的化合物的药物制剂，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与蛋白质或检查点激酶相关的一种或多种疾病的方法。 示例性化合物如下所示：

    Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
    38.
    发明授权
    Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors 有权
    取代的吡唑并[1,5-a]嘧啶作为蛋白激酶抑制剂

    公开(公告)号：US07601724B2

    公开(公告)日：2009-10-13

    申请号：US11542833

    申请日：2006-10-04

    申请人： Timothy J. Guzi ,  Kamil Paruch ,  Michael P. Dwyer

    发明人： Timothy J. Guzi ,  Kamil Paruch ,  Michael P. Dwyer

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/04

    CPC分类号： C07D487/04

    摘要： In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions. An illustrative compound of the invention is shown below:

    摘要翻译： 在其许多实施方案中，本发明提供了一类作为细胞周期蛋白依赖性激酶（CDK）抑制剂的吡唑并[1,5-a]嘧啶化合物，制备这些化合物的方法，含有一种或多种这类化合物的药物组合物，制备方法 包含一种或多种这样的化合物的药物制剂，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与CDK相关的一种或多种疾病的方法。 本发明的说明性化合物如下所示：