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    Discodermolide analogues and methods of their use
    3.
    发明授权
    Discodermolide analogues and methods of their use 有权
    木霉烯类似物及其使用方法

    公开(公告)号：US08193241B2

    公开(公告)日：2012-06-05

    申请号：US12946280

    申请日：2010-11-15

    申请人： Amos B. Smith, III ,  Simon J. Shaw ,  David C. Myles

    发明人： Amos B. Smith, III ,  Simon J. Shaw ,  David C. Myles

    IPC分类号： C07D215/227 ,  C07D265/36 ,  C07D311/22 ,  A61K31/538 ,  A61K31/353 ,  A61K31/4704

    CPC分类号： C07D311/16 ,  C07D215/227 ,  C07D265/36

    摘要： 6- and 7-substituted coumarin and related 6- and 7-substituted 1H-quinolin-2-one compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the 7-substituted coumarin and related 7-substituted 1H-quinolin-2-one compounds mimic or exceed the high level of pharmacological activity of discodermolide. In other embodiments, their preparation involves more readily available materials, higher yield processes and/or simpler synthetic sequences. In yet other embodiments, the compounds of the invention represent structurally simpler, therapeutically active analogues of discodermolide than heretofore known and may be useful as microtubule stabilizers and, inter alia, for treating and/or preventing cancer and other diseases, disorders, and/or conditions mediated by the stabilization of microtubules.

    摘要翻译： 6-和7-取代的香豆素及相关的6-和7-取代的1H-喹啉-2-酮化合物，含有这些化合物的药物组合物及其药物用途的方法。 在某些实施方案中，7-取代的香豆素和相关的7-取代的1H-喹啉-2-酮化合物模仿或超过氯仿的高水平的药理活性。 在其他实施方案中，它们的制备涉及更容易获得的材料，更高的产率过程和/或更简单的合成序列。 在其它实施方案中，本发明的化合物表示比迄今已知的结构上更简单的治疗活性的discodermolide类似物，并且可用作微管稳定剂，尤其用于治疗和/或预防癌症和其它疾病，障碍和/或 由微管稳定介导的病症。

    DISCODERMOLIDE ANALOGUES AND METHODS OF THEIR USE
    4.
    发明申请
    DISCODERMOLIDE ANALOGUES AND METHODS OF THEIR USE 有权
    异恶草酮类似物及其使用方法

    公开(公告)号：US20110172220A1

    公开(公告)日：2011-07-14

    申请号：US12946280

    申请日：2010-11-15

    申请人： Amos B. Smith, III ,  Simon J. Shaw ,  David C. Myles

    发明人： Amos B. Smith, III ,  Simon J. Shaw ,  David C. Myles

    IPC分类号： A61K31/538 ,  C07D265/36 ,  C07D311/22 ,  A61K31/353 ,  C07D215/227 ,  A61K31/4704 ,  A61P35/00

    CPC分类号： C07D311/16 ,  C07D215/227 ,  C07D265/36

    摘要： 6- and 7-substituted coumarin and related 6- and 7-substituted 1H-quinolin-2-one compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the 7-substituted coumarin and related 7-substituted 1H-quinolin-2-one compounds mimic or exceed the high level of pharmacological activity of discodermolide. In other embodiments, their preparation involves more readily available materials, higher yield processes and/or simpler synthetic sequences. In yet other embodiments, the compounds of the invention represent structurally simpler, therapeutically active analogues of discodermolide than heretofore known and may be useful as microtubule stabilizers and, inter alia, for treating and/or preventing cancer and other diseases, disorders, and/or conditions mediated by the stabilization of microtubules.

    摘要翻译： 6-和7-取代的香豆素及相关的6-和7-取代的1H-喹啉-2-酮化合物，含有这些化合物的药物组合物及其药物用途的方法。 在某些实施方案中，7-取代的香豆素和相关的7-取代的1H-喹啉-2-酮化合物模仿或超过氯仿的高水平的药理活性。 在其他实施方案中，它们的制备涉及更容易获得的材料，更高的产率过程和/或更简单的合成序列。 在其它实施方案中，本发明的化合物表示比迄今已知的结构上更简单的治疗活性的discodermolide类似物，并且可用作微管稳定剂，尤其用于治疗和/或预防癌症和其它疾病，障碍和/或 由微管稳定介导的病症。