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30 条记录 (耗时 0.064 秒)

    Bridged bicyclic RHO kinase inhibitor compounds, compositions and use
    12.
    发明授权
    Bridged bicyclic RHO kinase inhibitor compounds, compositions and use 有权
    桥联的双环RHO激酶抑制剂化合物，组合物和用途

    公开(公告)号：US08835457B2

    公开(公告)日：2014-09-16

    申请号：US13918020

    申请日：2013-06-14

    申请人： John W. Lampe ,  Paul S. Watson ,  David J. Slade

    发明人： John W. Lampe ,  Paul S. Watson ,  David J. Slade

    IPC分类号： C07D451/04 ,  C07D401/12

    CPC分类号： C07D451/04 ,  A61K31/46 ,  A61K31/4725 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D453/06 ,  C07D471/08 ,  C07D487/08

    摘要： The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. 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 cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma. In another embodiment, the method treats diseases or conditions of the lung associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema.

    摘要翻译： 本发明涉及作为rho相关蛋白激酶抑制剂的合成桥联双环化合物。 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细胞骨架重组相关的疾病或病症的方法。 该方法包括向受试者施用治疗有效量的式I的Rho激酶抑制性化合物，其中所述量有效地影响肌动球蛋白相互作用，例如通过导致细胞松弛和细胞 - 基底粘连的改变。 在一个实施方案中，该方法治疗增加的眼内压，例如原发性开角型青光眼。 在另一个实施方案中，该方法治疗与过度细胞增殖，重塑，炎症，血管收缩，支气管收缩，气道高反应性和水肿相关的肺的疾病或病症。

    Orally bioavailable compounds and methods for inhibiting platelet aggregation
    16.
    发明授权
    Orally bioavailable compounds and methods for inhibiting platelet aggregation 失效
    口服生物可利用的化合物和抑制血小板聚集的方法

    公开(公告)号：US07504497B2

    公开(公告)日：2009-03-17

    申请号：US11595837

    申请日：2006-11-09

    申请人： James G. Douglass, III ,  Paul S. Watson ,  Carl A. Samuelson ,  Christopher S. Crean

    发明人： James G. Douglass, III ,  Paul S. Watson ,  Carl A. Samuelson ,  Christopher S. Crean

    IPC分类号： C07H19/16 ,  A01N43/04 ,  A61K31/70

    CPC分类号： A61K31/519 ,  A61F2250/0067 ,  A61K31/52 ,  A61K31/522 ,  A61K31/7076 ,  A61K31/727 ,  A61K45/06 ,  C07H19/16 ,  A61K2300/00

    摘要： This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a non-nucleotide compound, preferably a P2Y12 receptor antagonist compound, wherein said amount is effective to inhibit platelet aggregation. The compounds useful for this invention include compounds of general Formulae III, IIIa, and IIIb, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae IIIa and IIIb, which are potent and have a good oral bioavailability.

    摘要翻译： 本发明涉及一种预防或治疗与血小板聚集有关的疾病或病症的方法。 该方法还涉及治疗血栓形成或相关病症的方法。 该方法包括向受试者施用包含有效量的非核苷酸化合物，优选P2Y12受体拮抗剂化合物的药物组合物，其中所述量有效抑制血小板聚集。 可用于本发明的化合物包括通式III，IIIa和IIIb的化合物，或其盐，水合物和溶剂化物。 本发明还提供新的式IIIa和IIIb化合物，它们是有效的并且具有良好的口服生物利用度。

    PROCESS FOR THE PREPARATION OF 3,4-DISUBSTITUTED-THIAZOLIDIN-2-ONES
    17.
    发明申请
    PROCESS FOR THE PREPARATION OF 3,4-DISUBSTITUTED-THIAZOLIDIN-2-ONES 失效
    制备3,4代替噻唑烷-2-酮的方法

    公开(公告)号：US20080287683A1

    公开(公告)日：2008-11-20

    申请号：US12182918

    申请日：2008-07-30

    申请人： Jonathan B. DeCamp ,  Paul S. Watson ,  Jin She

    发明人： Jonathan B. DeCamp ,  Paul S. Watson ,  Jin She

    IPC分类号： C07D277/04

    CPC分类号： C07D277/14 ,  C07C319/06 ,  C07C323/58

    摘要： The present invention is directed to practical high-yielding synthetic processes for preparing 3,4-disubstituted-thiazolidin-2-ones, which do not compromise the absolute stereochemical integrity of the compounds. The present invention is also directed to novel compounds of 3,4-disubstituted-thiazolidin-2-ones. The compounds prepared by the present invention are useful in the synthesis and manufacture of compounds (such as latrunculins and/or their analogs) for treating diseases or conditions associated with inhibiting actin polymerization.

    摘要翻译： 本发明涉及用于制备3,4-二取代 - 噻唑烷-2-酮的实用的高产合成方法，其不损害化合物的绝对立体化学完整性。 本发明还涉及3,4-二取代 - 噻唑烷-2-酮的新化合物。 通过本发明制备的化合物可用于合成和制备用于治疗与抑制肌动蛋白聚合相关的疾病或病症的化合物（例如软核灰蛋白和/或其类似物）。

    Process for the preparation of 3,4-disubstituted-thiazolidin-2-ones
    19.
    发明授权
    Process for the preparation of 3,4-disubstituted-thiazolidin-2-ones 失效
    制备3,4-二取代 - 噻唑烷-2-酮的方法

    公开(公告)号：US07947850B2

    公开(公告)日：2011-05-24

    申请号：US12182918

    申请日：2008-07-30

    申请人： Jonathan B. DeCamp ,  Paul S. Watson ,  Jin She

    发明人： Jonathan B. DeCamp ,  Paul S. Watson ,  Jin She

    IPC分类号： C07C323/58

    CPC分类号： C07D277/14 ,  C07C319/06 ,  C07C323/58

    摘要： The present invention is directed to practical high-yielding synthetic processes for preparing 3,4-disubstituted-thiazolidin-2-ones, which do not compromise the absolute stereochemical integrity of the compounds. The present invention is also directed to novel compounds of 3,4-disubstituted-thiazolidin-2-ones. The compounds prepared by the present invention are useful in the synthesis and manufacture of compounds (such as latrunculins and/or their analogs) for treating diseases or conditions associated with inhibiting actin polymerization.

    摘要翻译： 本发明涉及用于制备3,4-二取代 - 噻唑烷-2-酮的实用的高产合成方法，其不损害化合物的绝对立体化学完整性。 本发明还涉及3,4-二取代 - 噻唑烷-2-酮的新化合物。 通过本发明制备的化合物可用于合成和制备用于治疗与抑制肌动蛋白聚合相关的疾病或病症的化合物（例如软核灰蛋白和/或其类似物）。