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    Process for the preparation of Rho-kinase inhibitor compounds
    1.
    发明授权
    Process for the preparation of Rho-kinase inhibitor compounds 失效
    制备Rho激酶抑制剂化合物的方法

    公开(公告)号：US08158796B2

    公开(公告)日：2012-04-17

    申请号：US12470377

    申请日：2009-05-21

    申请人： Jin She ,  Jonathan Bryan deCamp ,  Paul S. Watson ,  David J. Slade

    发明人： Jin She ,  Jonathan Bryan deCamp ,  Paul S. Watson ,  David J. Slade

    IPC分类号： C07D217/22

    CPC分类号： C07D401/12 ,  C07C67/08 ,  C07C69/78

    摘要： The present invention is directed to practical high-yielding synthetic processes to prepare compounds of general Formula III, IV, V, VII, VIII, IX, X, XII, XIV, and XV. Such compounds are useful as final products or can be used as intermediates and be further modified to prepare other desired products such as rho-kinase inhibitors. The present invention is also directed to certain novel compounds and/or novel solid forms of certain compounds.

    摘要翻译： 本发明涉及制备通式III，IV，V，VII，VIII，IX，X，XII，XIV和XV的化合物的实际高产合成方法。 这些化合物可用作最终产物，或可用作中间体，并进一步修饰以制备其它所需产物如rho激酶抑制剂。 本发明还涉及某些新化合物和/或某些化合物的新型固体形式。

    PROCESS FOR THE PREPARATION OF RHO-KINASE INHIBITOR COMPOUNDS
    2.
    发明申请
    PROCESS FOR THE PREPARATION OF RHO-KINASE INHIBITOR COMPOUNDS 失效
    制备RHO-激酶抑制剂化合物的方法

    公开(公告)号：US20100022775A1

    公开(公告)日：2010-01-28

    申请号：US12470377

    申请日：2009-05-21

    申请人： Jin She ,  Jonathan Bryan deCamp ,  Paul S. Watson ,  David J. Slade

    发明人： Jin She ,  Jonathan Bryan deCamp ,  Paul S. Watson ,  David J. Slade

    IPC分类号： C07D217/22 ,  C07C65/30

    CPC分类号： C07D401/12 ,  C07C67/08 ,  C07C69/78

    摘要： The present invention is directed to practical high-yielding synthetic processes to prepare compounds of general Formula III, IV, V, VII, VIII, IX, X, XII, XIV, and XV. Such compounds are useful as final products or can be used as intermediates and be further modified to prepare other desired products such as rho-kinase inhibitors. The present invention is also directed to certain novel compounds and/or novel solid forms of certain compounds.

    摘要翻译： 本发明涉及制备通式III，IV，V，VII，VIII，IX，X，XII，XIV和XV的化合物的实际高产合成方法。 这些化合物可用作最终产物，或可用作中间体，并进一步修饰以制备其它所需产物如rho激酶抑制剂。 本发明还涉及某些新化合物和/或某些化合物的新型固体形式。

    Cytoskeletal active compounds, composition and use
    9.
    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。