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    Orally bioavailable compounds and methods for inhibiting platelet aggregation
    4.
    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。

    Pyrimidine-based non-nucleotide composition and method for inhibiting platelet aggregation
    6.
    发明授权
    Pyrimidine-based non-nucleotide composition and method for inhibiting platelet aggregation 失效
    基于嘧啶的非核苷酸组合物和抑制血小板聚集的方法

    公开(公告)号：US07932376B2

    公开(公告)日：2011-04-26

    申请号：US11413600

    申请日：2006-04-28

    申请人： James G. Douglass, III ,  Paul S. Watson ,  Sammy R. Shaver ,  Krzysztof Bednarski

    发明人： James G. Douglass, III ,  Paul S. Watson ,  Sammy R. Shaver ,  Krzysztof Bednarski

    IPC分类号： C07H19/06 ,  C07H19/067 ,  C07D239/47 ,  A61K31/7068 ,  A61K31/506 ,  A61P7/02

    CPC分类号： C07D493/04 ,  C07D405/04 ,  C07H19/12

    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 pyrimidine-based 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 I and Ia-Ic, or tautomers, salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae I and Ia-Ic.

    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嘧啶类化合物，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I和Ia-Ic的化合物，或其互变异构体，盐，水合物和溶剂合物。 本发明还提供式I和Ia-1c的新型化合物。

    BRIDGED BICYCLIC RHO KINASE INHIBITOR COMPOUNDS, COMPOSITIONS AND USE
    9.
    发明申请
    BRIDGED BICYCLIC RHO KINASE INHIBITOR COMPOUNDS, COMPOSITIONS AND USE 有权
    BRIDGED BICYCLIC RHO激酶抑制剂化合物，组合物和用途

    公开(公告)号：US20130281485A1

    公开(公告)日：2013-10-24

    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。

    Cytoskeletal active compounds, composition and use
    10.
    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。