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    MICROTUBULE STABILIZING COMPOUNDS AND METHODS OF THEIR USE
    2.
    发明申请
    MICROTUBULE STABILIZING COMPOUNDS AND METHODS OF THEIR USE 审中-公开
    MICROTUBULE STABIL化合物及其使用方法

    公开(公告)号：WO2006091728A3

    公开(公告)日：2007-04-05

    申请号：PCT/US2006006401

    申请日：2006-02-24

    申请人： UNIV PENNSYLVANIA ,  TROJANOWSKI JOHN Q ,  SMITH AMOS B III ,  LEE VIRGINIA M Y

    发明人： TROJANOWSKI JOHN Q ,  SMITH AMOS B III ,  LEE VIRGINIA M Y

    IPC分类号： A61K39/00 ,  A01N37/18 ,  A01N61/00 ,  A61K31/00 ,  A61K38/00 ,  A61K39/38

    CPC分类号： A61K31/337 ,  A61K45/06 ,  A61K2300/00

    摘要： Methods for the stabilization of microtubules involved in axonal transport are disclosed. The methods employing compounds which functionally substitute for microtubule binding protein tau are useful, inter alia, in the treatment of neurodegenerative diseases or tauopathies. Microtubule stabilizing compounds are useful for the treatment of neurodegenerative diseases, as well as schizophrenia and other mental disorders that are characterized by disruption of maintain neuronal intracellular transport, neurite architecture, or neuronal migration.

    摘要翻译： 公开了稳定涉及轴突运输的微管的方法。 使用功能性取代微管结合蛋白tau的化合物的方法尤其可用于治疗神经变性疾病或tau蛋白病。 微管稳定化合物可用于治疗神经变性疾病以及精神分裂症和其他精神障碍，其特征在于维持神经元细胞内运输，神经突构造或神经元迁移的破坏。

    DISCODERMOLIDE ANALOGUES AND METHODS OF THEIR USE
    8.
    发明申请
    DISCODERMOLIDE ANALOGUES AND METHODS OF THEIR USE 审中-公开
    异恶草酮类似物及其使用方法

    公开(公告)号：WO2009006184A1

    公开(公告)日：2009-01-08

    申请号：PCT/US2008/068288

    申请日：2008-06-26

    申请人： THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA ,  KOSAN BIOSCIENCES, INC. ,  SMITH, Amos, B. ,  SHAW, Simon, J. ,  MYLES, David, C.

    发明人： SMITH, Amos, B. ,  SHAW, Simon, J. ,  MYLES, David, C.

    IPC分类号： A01N43/42 ,  A61K31/47

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

    摘要： 6- and 7-substituted coumarin and related 6- and 7-substituted l H -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 l H -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-酮化合物模拟或超过discodermolide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。