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6 条记录 (耗时 0.015 秒)

    Cationic ceramides, and analogs thereof, and their use for preventing or treating cancer
    2.
    发明授权
    Cationic ceramides, and analogs thereof, and their use for preventing or treating cancer 有权
    阳离子神经酰胺及其类似物及其用于预防或治疗癌症的用途

    公开(公告)号：US08093393B2

    公开(公告)日：2012-01-10

    申请号：US11666518

    申请日：2005-10-31

    申请人： Alicja Bielawska ,  Zdzislaw M. Szulc ,  Yusuf A. Hannun ,  Lina M. Obeid ,  Besim Ogretmen

    发明人： Alicja Bielawska ,  Zdzislaw M. Szulc ,  Yusuf A. Hannun ,  Lina M. Obeid ,  Besim Ogretmen

    IPC分类号： C07D211/00 ,  C07D211/92

    CPC分类号： C07D213/56

    摘要： The present invention relates to cationic ceramides, their dihydro-analogs and aromatic analogs and their derivatives, comprising a pyridinium group. Also provided are methods for making cationic ceramides comprising a pyridinium group, and their use for treating or preventing diseases associated with cell overproliferation and sphingolipid signal transduction, such as cancer, inflammation, and stenosis. The compounds are also useful as mitochondritropic agents that are localized to mitochondria carrying with them chemical cargoes, such as drugs, or signaling molecules, such as fluorophores for probing organelle structure and functions.

    摘要翻译： 本发明涉及阳离子神经酰胺，其二氢类似物和芳族类似物及其衍生物，其包含吡啶鎓基团。 还提供了制备包含吡啶鎓基团的阳离子神经酰胺的方法及其用于治疗或预防与细胞过度增殖和鞘脂信号转导相关的疾病如癌症，炎症和狭窄的用途。 该化合物也可用作线粒体药物，其被定位于与其携带化学货物的线粒体，例如药物或信号分子，例如用于探测细胞器结构和功能的荧光团。

    Lysosomotropic inhibitors of acid ceramidase
    3.
    发明授权
    Lysosomotropic inhibitors of acid ceramidase 有权
    酸性神经酰胺酶的溶酶体抑制剂

    公开(公告)号：US08697379B2

    公开(公告)日：2014-04-15

    申请号：US13127888

    申请日：2009-11-06

    申请人： Alicja Bielawska ,  Aiping Bai ,  Zdzislaw M. Szulc ,  Yusuf A. Hannun ,  James S. Norris ,  Liu Xiang

    发明人： Alicja Bielawska ,  Aiping Bai ,  Zdzislaw M. Szulc ,  Yusuf A. Hannun ,  James S. Norris ,  Liu Xiang

    IPC分类号： A61K31/41 ,  A61K31/44 ,  C07C229/00 ,  C07D211/78

    CPC分类号： A61K31/16 ,  C07C233/18

    摘要： The presently disclosed subject matter provides compounds of the formula, formula (Ia): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, and n are as defined herein. Also disclosed are methods for making the compounds of the formula as set forth hereinabove, their use in inhibiting acid ceramidase and ceramidase-related activity, and their use as drugs and prodrugs in the treatment and/or prevention of diseases associated with undesirable ceramidase or sphingosine kinase activity, including, but not limited to, cancer, cancer metastasis, atherosclerosis, stenosis, inflammation, asthma, and atopic dermatitis.

    摘要翻译： 目前公开的主题提供式（Ia）化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5，X，Y和n如本文所定义。 还公开了制备如上所述的式的化合物，其用于抑制酸性神经酰胺酶和神经酰胺酶相关活性的方法，以及它们作为药物和前药用于治疗和/或预防与不期望的神经酰胺酶或鞘氨醇相关的疾病的用途的方法 激酶活性，包括但不限于癌症，癌症转移，动脉粥样硬化，狭窄，炎症，哮喘和特应性皮炎。