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12 条记录 (耗时 0.052 秒)

    Cytoskeletal active compounds, composition and use
    6.
    发明授权
    Cytoskeletal active compounds, composition and use 失效
    细胞骨架活性化合物，组成和用途

    公开(公告)号：US08039465B2

    公开(公告)日：2011-10-18

    申请号：US12695348

    申请日：2010-01-28

    申请人： John W. Lampe ,  Robert Plourde, Jr. ,  Jin She ,  Jason L. Vittitow ,  Paul S. Watson ,  Michael T. Crimmins ,  David J. Slade

    发明人： John W. Lampe ,  Robert Plourde, Jr. ,  Jin She ,  Jason L. Vittitow ,  Paul S. Watson ,  Michael T. Crimmins ,  David J. Slade

    IPC分类号： A61K31/54

    CPC分类号： C07D491/08 ,  C07D277/06 ,  C07D277/14 ,  C07D277/16 ,  C07D277/34 ,  C07D277/56 ,  C07D417/04 ,  C07D493/08 ,  C07D497/18

    摘要： The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.

    摘要翻译： 本发明涉及与天然的秋水仙素A或梭菌素B相关的合成细胞骨架活性化合物。本发明还涉及包含这些化合物和药学上可接受的载体的药物组合物。 本发明另外涉及预防或治疗与肌动蛋白聚合相关的疾病或病症的方法。 在本发明的一个实施方案中，该方法治疗增加的眼内压，例如原发性开角型青光眼。 该方法包括向受试者施用治疗有效量的式I或II的细胞骨架活性化合物，其中所述量有效影响细胞骨架，例如通过抑制肌动蛋白聚合。

    Method for reducing intraocular pressure using indole derivatives
    9.
    发明授权
    Method for reducing intraocular pressure using indole derivatives 失效
    使用吲哚衍生物降低眼内压的方法

    公开(公告)号：US06730707B2

    公开(公告)日：2004-05-04

    申请号：US09915486

    申请日：2001-07-25

    申请人： Jesus J. Pintor ,  Maria A. Peral ,  Ward M. Peterson ,  Robert Plourde, Jr. ,  Edward G. Brown ,  Benjamin R. Yerxa

    发明人： Jesus J. Pintor ,  Maria A. Peral ,  Ward M. Peterson ,  Robert Plourde, Jr. ,  Edward G. Brown ,  Benjamin R. Yerxa

    IPC分类号： A61K4732

    CPC分类号： A61K31/404 ,  A61K31/4045 ,  A61K31/55 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention provides a method of reducing intraocular pressure by administering pharmaceutical compositions comprising indole derivatives. The pharmaceutical compositions useful in this invention comprise indole derivatives and melatonin analogs of Formulae I-IV. A preferred embodiment is a method of lowering intraocular pressure using 5-(methoxycarbonylamino)-N-acetyltryptamine (5-MCA-NAT), also known as GR 135531, which has a prolonged duration of action and greater efficacy in lowering intraocular pressure compared to melatonin. The present invention further provides a method of treating disorders associated with ocular hypertension, and a method of treating various forms of glaucoma; the method comprises administering an effective dose of a pharmacuetical composition comprising an indole derivative with or without agents commonly used to treat such disorders.

    摘要翻译： 本发明提供通过给药包含吲哚衍生物的药物组合物降低眼内压的方法。 用于本发明的药物组合物包含式I-IV的吲哚衍生物和褪黑素类似物。 优选的实施方案是使用5-（甲氧基羰基氨基）-N-乙酰基色胺（5-MCA-NAT）（也称为GR135531）降低眼内压的方法，其具有延长的作用时间和降低眼内压的更高功效， 褪黑激素 本发明还提供了治疗与高眼压相关的疾病的方法和治疗各种形式的青光眼的方法; 该方法包括施用有效剂量的药物组合物，所述药物组合物包含吲哚衍生物，所述药物组合物含或不含通常用于治疗所述疾病的试剂。