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    PHOSPHOROUS PROTECTING GROUPS AND METHODS OF PREPARATION AND USE THEREOF
    5.
    发明申请
    PHOSPHOROUS PROTECTING GROUPS AND METHODS OF PREPARATION AND USE THEREOF 审中-公开
    磷保护基团及其制备方法和用途

    公开(公告)号：WO2015168461A2

    公开(公告)日：2015-11-05

    申请号：PCT/US2015/028624

    申请日：2015-04-30

    Applicant: AGILENT TECHNOLOGIES, INC.

    Inventor： DELLINGER, Douglas J. ,  MONFREGOLA, Luca ,  CARUTHERS, Marvin ,  ROY, Mithum

    IPC: C07H19/10 ,  C07H21/04

    CPC classification number: C07H21/04 ,  C07H19/073 ,  C07H19/10 ,  C07H19/173 ,  C07H19/23 ,  Y02P20/55

    Abstract: Aspects of the present disclosure include compositions that make use of phosphorus and/or nucleobase protecting groups which find use in the synthesis of long polynucleotides. Phosphorus protecting groups are provided that help increase the stepwise coupling yield and/or phosphorous protecting groups that can be removed during the oxidation step. Amidine nucleobase protecting groups are provided that find use in the subject compositions and methods which provides for e.g., increased resistance to depurination during polynucleotide synthesis. In some instances, the methods and compositions disclosed herein utilize a combination of the phosphorus and amidine nucleobase protecting groups in the synthesis of polynucleotides having a sequence of 200 or more monomeric units in length. Also provided are methods for synthesizing a polynucleotide (e.g., a DNA) using one or more compounds disclosed herein.

    Abstract translation: 本公开的方面包括利用在长多核苷酸的合成中使用的磷和/或核碱基保护基团的组合物。 提供了有助于增加在氧化步骤中可以除去的逐步偶联产率和/或磷保护基团的磷保护基团。 提供了脒核碱基保护基，其可用于本发明组合物和方法中，所述组合物和方法在多核苷酸合成期间提供例如增加的去嘌呤抗性。 在一些情况下，本文公开的方法和组合物在合成具有200个或更多个单体单元长度的序列的多核苷酸中利用磷和脒核碱基保护基的组合。 还提供了使用本文公开的一种或多种化合物合成多核苷酸（例如DNA）的方法。

    MODULATORS OF CELL CYCLE CHECKPOINTS AND THEIR USE IN COMBINATION WITH CHECKPOINT KINASE INHIBITORS
    8.
    发明申请
    MODULATORS OF CELL CYCLE CHECKPOINTS AND THEIR USE IN COMBINATION WITH CHECKPOINT KINASE INHIBITORS 审中-公开
    细胞周期调节因子的调节因子及其与检测点激酶抑制剂的组合使用

    公开(公告)号：WO2011028638A1

    公开(公告)日：2011-03-10

    申请号：PCT/US2010/046936

    申请日：2010-08-27

    Applicant: SCHERING CORPORATION ,  POPOVICI-MULLER, Janeta ,  ROSNER, Kristin, E. ,  GUZI, Timothy, J.

    Inventor： POPOVICI-MULLER, Janeta ,  ROSNER, Kristin, E. ,  GUZI, Timothy, J.

    IPC: A01N43/04 ,  A61K31/70

    CPC classification number: A61K31/70 ,  C07D405/04 ,  C07D405/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07H19/06 ,  C07H19/23

    Abstract: In its many embodiments, the present invention provides a novel class of pyrimidine analogs 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 also includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the cell cycle checkpoint modulator as well as combinations and pharmaceutical kits. An example cell cycle checkpoint modulator is shown below: formula (I).

    Abstract translation: 在其许多实施方案中，本发明提供了一类新颖的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。 本发明还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来治疗癌症的方法，包含细胞周期检查点调节剂的药物组合物以及组合和药物试剂盒。 示例细胞周期检查点调制器如下所示：公式（I）。

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