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    METHOD FOR INVERTING THE C2’ HYDROXYL GROUP OF TAXANE ESTERS
    1.
    发明申请
    METHOD FOR INVERTING THE C2’ HYDROXYL GROUP OF TAXANE ESTERS 审中-公开
    用于反应C2'羟基的羟基的方法

    公开(公告)号：WO2005037840A1

    公开(公告)日：2005-04-28

    申请号：PCT/US2004/033858

    申请日：2004-10-14

    Applicant: MAYNE PHARMA (USA), INC. ,  MCCHESNEY, James, D. ,  CHANDER, Madhavi, C. ,  HENRI, John, T. ,  FERRARA, James, V. ,  BRINKMAN, Herbert, R.

    Inventor： MCCHESNEY, James, D. ,  CHANDER, Madhavi, C. ,  HENRI, John, T. ,  FERRARA, James, V. ,  BRINKMAN, Herbert, R.

    IPC: C07D493/00

    CPC classification number: C07D307/93 ,  Y02P20/55

    Abstract: The present invention provides a method for inverting the 2’-hydroxy position of selected taxanes. The method includes protecting the 2’ hydroxyl group of a first selected taxane with a hydroxyl protecting group, such as a tosyl group, a mesyl group or a nosyl group. The protected taxane compound is then converted to an oxazole compound having an oxazole ring. The oxaxole ring is then opened by an appropriate process, such as by hydrolyzing the oxaxole compound thereby to form an intermediate compound, which is then converted to a second taxane. The intermediate compound may be an anime salt that is treated with a base to form the second taxane. The method contemplated by be used to convert 2’epi paclitaxel into paclitaxel. Alternatively, the method may be used to convert paclitaxel into 2’epi paclitaxel. The present invention also relates to novel compounds and intermediates formed by the process.

    Abstract translation: 本发明提供了使所选择的紫杉烷类的2'-羟基位置反转的方法。 该方法包括使用羟基保护基（例如甲苯磺酰基，甲磺酰基或诺基）保护第一选择的紫杉烷的2'羟基。 然后将受保护的紫杉烷化合物转化为具有恶唑环的恶唑化合物。 然后通过适当的方法打开恶唑环，例如通过水解oxaxole化合物从而形成中间体化合物，然后将其转化为第二紫杉烷。 中间体化合物可以是用碱处理以形成第二紫杉烷的动物盐。 用于将2'epi紫杉醇转化成紫杉醇的方法。 或者，该方法可用于将紫杉醇转化成2'epi紫杉醇。 本发明还涉及通过该方法形成的新型化合物和中间体。

    TAXANE ANALOGUES, THEIR USE, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND PROCESSES FOR THEIR PREPARATION
    7.
    发明申请
    TAXANE ANALOGUES, THEIR USE, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND PROCESSES FOR THEIR PREPARATION 审中-公开
    TAXANE类似物，其使用，含有它们的药物组合物及其制备方法

    公开(公告)号：WO2011028571A1

    公开(公告)日：2011-03-10

    申请号：PCT/US2010/046627

    申请日：2010-08-25

    Applicant: TAPESTRY PHARMACEUTICALS, INC. ,  MCCHESNEY, James, D. ,  VENKATARAMAN, Sylesh ,  HENRI, John, T.

    Inventor： MCCHESNEY, James, D. ,  VENKATARAMAN, Sylesh ,  HENRI, John, T.

    IPC: A01N43/02

    CPC classification number: C07D493/06

    Abstract: The present invention relates to novel taxane analogues, processes of making the novel taxane analogues, compositions containing the novel taxane analogues, and their use in treating cancer and neurodegenerative disorders. In some embodiments, the taxane analogues are represented by the generic structure of formula (I) : wherein R 1 , R 2 ,R 3 and A are defined herein; and esters especially pro-drugs thereof wherein one or more of the hydroxy! groups is esterified to form an in-vivo hydrolysable ester group; or pharmaceutically acceptable salts thereof.

    Abstract translation: 本发明涉及新型紫杉烷类似物，制备新型紫杉烷类似物的方法，含有新型紫杉烷类似物的组合物及其在治疗癌症和神经变性疾病中的用途。 在一些实施方案中，紫杉烷类似物由式（I）的通式结构表示：其中R1，R2，R3和A在本文中定义; 和酯，特别是其前体药物，其中一个或多个羟基 酯基酯化以形成体内可水解的酯基团; 或其药学上可接受的盐。

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