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    Pyrimidine-based non-nucleotide composition and method for inhibiting platelet aggregation
    1.
    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。

    Composition and method for inhibiting platelet aggregation
    2.
    发明授权
    Composition and method for inhibiting platelet aggregation 有权
    抑制血小板聚集的组合物和方法

    公开(公告)号：US07132408B2

    公开(公告)日：2006-11-07

    申请号：US10814007

    申请日：2004-03-30

    申请人： José L. Boyer ,  James G. Douglass, III ,  Sammy R. Shaver ,  Krzysztof Bednarski ,  Benjamin R. Yerxa ,  Gillian M. Olins

    发明人： José L. Boyer ,  James G. Douglass, III ,  Sammy R. Shaver ,  Krzysztof Bednarski ,  Benjamin R. Yerxa ,  Gillian M. Olins

    IPC分类号： A01N43/04 ,  A61K31/70

    CPC分类号： C07H19/20 ,  A61K31/675 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/7084 ,  C07H19/04 ,  C07H19/10 ,  C07H19/207 ,  C07H21/00

    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. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y12 receptor antagonist compound, wherein said amount is effective to bind the P2Y12 receptors on platelets and inhibit ADP-induced platelet aggregation. The P2Y12 receptor antagonist compounds useful for this invention include mononucleoside 5′-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates of general Formula I, or salts thereof. The present invention also provides novel compounds of mononucleoside 5′-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates. The present invention further provides pharmaceutical formulations comprising mononucleoside 5′-monophosphates, mononucleoside polyphosphates, or dinucleoside polyphosphates.

    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的方法。 该方法包括向受试者施用包含治疗有效量的P2Y 12受体拮抗剂化合物的药物组合物，其中所述量有效结合血小板上的P2Y 12 / 抑制ADP诱导的血小板聚集。 可用于本发明的P2Y 12受体拮抗剂化合物包括单核苷5'-单磷酸酯，单核苷多聚磷酸酯和通式I的二核苷多磷酸盐或其盐。 本发明还提供了单核苷5'-单磷酸酯，单核苷多磷酸盐和二核苷多磷酸的新型化合物。 本发明还提供了包含单核苷5'-单磷酸酯，单核苷多磷酸盐或二核苷多磷酸盐的药物制剂。

    P2Y6 RECEPTOR AGONISTS FOR TREATING LUNG DISEASES
    7.
    发明申请
    P2Y6 RECEPTOR AGONISTS FOR TREATING LUNG DISEASES 有权
    P2Y6受体激素治疗肺疾病

    公开(公告)号：US20110054163A1

    公开(公告)日：2011-03-03

    申请号：US12939934

    申请日：2010-11-04

    申请人： José L. Boyer ,  Sammy R. Shaver ,  James G. Douglass, III ,  Catherine C. Redick

    发明人： José L. Boyer ,  Sammy R. Shaver ,  James G. Douglass, III ,  Catherine C. Redick

    IPC分类号： C07H19/067

    CPC分类号： A61K31/7072 ,  A61K31/708 ,  A61K31/7084

    摘要： This invention is directed to a method of enhancing or facilitating the clearance or the lung mucus secretions in a subject. This invention is also directed to a method of facilitating the hydration of the lung mucus secretions in a subject. This invention is further directed to a method of preventing or treating diseases or conditions associated with impaired lung or airway function in a human or other mammal. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y6 receptor agonist compound, wherein said amount is effective to activate the P2Y6 receptors on the luminal surface of lung epithelia. The P2Y6 receptor agonist compounds useful for this invention include mononucleoside 5′-diphosphates, dinucleoside monophosphate, dinucleoside diphosphates, or dinucleoside triphosphates of general Formula I, or salts, solvates, hydrates thereof. This invention is also directed to novel P2Y6 receptor agonist compounds.

    摘要翻译： 本发明涉及增强或促进受试者中的清除或肺粘液分泌的方法。 本发明还涉及促进受试者中肺粘液分泌物水合的方法。 本发明进一步涉及预防或治疗与人或其他哺乳动物的肺或气道功能受损有关的疾病或病症的方法。 该方法包括向受试者施用包含治疗有效量的P2Y6受体激动剂化合物的药物组合物，其中所述量有效激活肺上皮细胞腔表面上的P2Y6受体。 可用于本发明的P2Y6受体激动剂化合物包括单核苷5'-二磷酸，二核苷单磷酸，二核苷二磷酸或通式I的二核苷三磷酸，或其盐，溶剂合物，水合物。 本发明还涉及新颖的P2Y6受体激动剂化合物。

    P2Y6 receptor agonists for treating lung diseases
    8.
    发明授权
    P2Y6 receptor agonists for treating lung diseases 有权
    用于治疗肺部疾病的P2Y6受体激动剂

    公开(公告)号：US07851456B2

    公开(公告)日：2010-12-14

    申请号：US11478338

    申请日：2006-06-28

    申请人： José L. Boyer ,  Sammy R. Shaver ,  James G. Douglass, III ,  Catherine C. Redick

    发明人： José L. Boyer ,  Sammy R. Shaver ,  James G. Douglass, III ,  Catherine C. Redick

    IPC分类号： A01N43/04 ,  A61K31/70

    CPC分类号： A61K31/7072 ,  A61K31/708 ,  A61K31/7084

    摘要： This invention is directed to a method of enhancing or facilitating the clearance of the lung mucus secretions in a subject. This invention is also directed to a method of facilitating the hydration of the lung mucus secretions in a subject. This invention is further directed to a method of preventing or treating diseases or conditions associated with impaired lung or airway function in a human or other mammal. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y6 receptor agonist compound, wherein said amount is effective to activate the P2Y6 receptors on the luminal surface of lung epithelia. The P2Y6 receptor agonist compounds useful for this invention include mononucleoside 5′-diphosphates, dinucleoside monophosphate, dinucleoside diphosphates, or dinucleoside triphosphates of general Formula I, or salts, solvates, hydrates thereof.

    摘要翻译： 本发明涉及增强或促进受试者中肺粘液分泌物清除的方法。 本发明还涉及促进受试者中肺粘液分泌物水合的方法。 本发明进一步涉及预防或治疗与人或其他哺乳动物的肺或气道功能受损有关的疾病或病症的方法。 该方法包括向受试者施用包含治疗有效量的P2Y6受体激动剂化合物的药物组合物，其中所述量有效激活肺上皮细胞腔表面上的P2Y6受体。 可用于本发明的P2Y6受体激动剂化合物包括单核苷5'-二磷酸，二核苷单磷酸，二核苷二磷酸或通式I的二核苷三磷酸，或其盐，溶剂合物，水合物。

    DRUG-ELUTING STENTS COATED WITH P2Y12 RECEPTOR ANTAGONIST COMPOUND
    9.
    发明申请
    DRUG-ELUTING STENTS COATED WITH P2Y12 RECEPTOR ANTAGONIST COMPOUND 失效
    用P2Y12受体拮抗剂化合物包衣的药物给药

    公开(公告)号：US20080287671A1

    公开(公告)日：2008-11-20

    申请号：US12182935

    申请日：2008-07-30

    申请人： Jose L. Boyer ,  James G. Douglass, III ,  Sammy R. Shaver

    发明人： Jose L. Boyer ,  James G. Douglass, III ,  Sammy R. Shaver

    IPC分类号： C07H19/20

    CPC分类号： C07H19/04 ,  A61K31/675 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/7084 ,  C07H19/10 ,  C07H19/20 ,  C07H19/207 ,  C07H21/00

    摘要： The present invention provides a P2Y12 receptor antagonist compound-eluting stent, wherein the stent is coated with one or more P2Y12 receptor antagonist compounds or a pharmaceutically acceptable salt, solvate, or hydrate thereof. When the stent is placed in a narrowed or damaged arterial vessel, a therapeutically effective amount of the P2Y12 receptor antagonist compound is eluted continuously from the stent to the local environment of the stent. The P2Y12 receptor antagonist compound-eluting stents are useful in preventing thrombosis and restenosis, and are effective in inhibiting the contraction of vascular smooth muscle cells, inhibiting cell proliferation, and reducing inflammation.

    摘要翻译： 本发明提供P2Y 12受体拮抗剂化合物洗脱支架，其中支架涂覆有一种或多种P2Y 12受体拮抗剂化合物或其药学上可接受的盐，溶剂化物， 或其水合物。 当支架置于狭窄或损伤的动脉血管中时，治疗有效量的P2Y 12受体拮抗剂化合物从支架连续洗脱至支架的局部环境。 P2Y 12受体拮抗剂化合物洗脱支架可用于预防血栓形成和再狭窄，并且有效抑制血管平滑肌细胞的收缩，抑制细胞增殖和减少炎症。

    P2Y6 receptor agonists for treating lung diseases
    10.
    发明授权
    P2Y6 receptor agonists for treating lung diseases 有权
    用于治疗肺部疾病的P2Y6受体激动剂

    公开(公告)号：US08158776B2

    公开(公告)日：2012-04-17

    申请号：US12939934

    申请日：2010-11-04

    申请人： José L. Boyer ,  Sammy R. Shaver ,  James G. Douglass, III ,  Catherine C. Redick

    发明人： José L. Boyer ,  Sammy R. Shaver ,  James G. Douglass, III ,  Catherine C. Redick

    IPC分类号： C07H19/04 ,  C07H19/20

    CPC分类号： A61K31/7072 ,  A61K31/708 ,  A61K31/7084

    摘要： This invention is directed to a method of enhancing or facilitating the clearance or the lung mucus secretions in a subject. This invention is also directed to a method of facilitating the hydration of the lung mucus secretions in a subject. This invention is further directed to a method of preventing or treating diseases or conditions associated with impaired lung or airway function in a human or other mammal. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y6 receptor agonist compound, wherein said amount is effective to activate the P2Y6 receptors on the luminal surface of lung epithelia. The P2Y6 receptor agonist compounds useful for this invention include mononucleoside 5′-diphosphates, dinucleoside monophosphate, dinucleoside diphosphates, or dinucleoside triphosphates of general Formula I, or salts, solvates, hydrates thereof. This invention is also directed to novel P2Y6 receptor agonist compounds.

    摘要翻译： 本发明涉及增强或促进受试者中的清除或肺粘液分泌的方法。 本发明还涉及促进受试者中肺粘液分泌物水合的方法。 本发明进一步涉及预防或治疗与人或其他哺乳动物的肺或气道功能受损有关的疾病或病症的方法。 该方法包括向受试者施用包含治疗有效量的P2Y6受体激动剂化合物的药物组合物，其中所述量有效激活肺上皮细胞腔表面上的P2Y6受体。 可用于本发明的P2Y6受体激动剂化合物包括单核苷5'-二磷酸，二核苷单磷酸，二核苷二磷酸或通式I的二核苷三磷酸，或其盐，溶剂合物，水合物。 本发明还涉及新颖的P2Y6受体激动剂化合物。