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    METHOD FOR TREATING INFLAMMATORY CONDITIONS
    1.
    发明申请
    METHOD FOR TREATING INFLAMMATORY CONDITIONS 审中-公开
    治疗炎症症状的方法

    公开(公告)号：US20100160250A1

    公开(公告)日：2010-06-24

    申请号：US12641208

    申请日：2009-12-17

    申请人： James G. Douglass, III ,  Sammy R. Shaver ,  Tomas Navratil ,  José L. Boyer ,  Carl A. Samuelson ,  Jonathan B. DeCamp

    发明人： James G. Douglass, III ,  Sammy R. Shaver ,  Tomas Navratil ,  José L. Boyer ,  Carl A. Samuelson ,  Jonathan B. DeCamp

    IPC分类号： A61K31/70 ,  C07H19/167

    CPC分类号： A61K31/7068 ,  A61K31/7076

    摘要： This invention provides a method for inhibiting the release of interleukin-1β in a mammal. This invention also provides a method for preventing or treating pulmonary diseases, ophthalmic diseases, and autoimmune diseases that are associated with inflammation or inflammatory conditions. The invention also provides a method for preventing or treating neurodegenerative diseases, or pain in a mammal. The method comprises administering to a mammal in need thereof a therapeutically effective amount of a mononucleoside compound, which is an antagonist of P2X7 receptor.

    摘要翻译： 本发明提供了抑制白细胞介素-1bb的释放的方法。 在哺乳动物中。 本发明还提供了预防或治疗与炎症或炎症状况相关的肺部疾病，眼科疾病和自身免疫性疾病的方法。 本发明还提供了预防或治疗哺乳动物神经变性疾病或疼痛的方法。 该方法包括向有需要的哺乳动物施用治疗有效量的作为P2X7受体拮抗剂的单核苷化合物。

    Drug-eluting stents coated with P2Y12 receptor antagonist compound
    2.
    发明授权
    Drug-eluting stents coated with P2Y12 receptor antagonist compound 失效
    药物洗脱支架涂有P2Y12受体拮抗剂化合物

    公开(公告)号：US07618949B2

    公开(公告)日：2009-11-17

    申请号：US12182935

    申请日：2008-07-30

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

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

    IPC分类号： A01N43/04 ,  A61K31/70

    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P2Y12受体拮抗剂化合物洗脱支架，其中支架涂覆有一种或多种P2Y12受体拮抗剂化合物或其药学上可接受的盐，溶剂合物或水合物。 当支架置于狭窄或损伤的动脉血管中时，将治疗有效量的P2Y12受体拮抗剂化合物从支架连续洗脱至支架的局部环境。 P2Y12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。

    DEGRADATION-RESISTANT MONONUCLEOSIDE PHOSPHATE COMPOUNDS
    3.
    发明申请
    DEGRADATION-RESISTANT MONONUCLEOSIDE PHOSPHATE COMPOUNDS 失效
    耐腐蚀单核苷酸磷酸酯化合物

    公开(公告)号：US20090076256A1

    公开(公告)日：2009-03-19

    申请号：US12208265

    申请日：2008-09-10

    申请人： James G. Douglass, III ,  Benjamin R. Yerxa ,  Sammy R. Shaver ,  Ward M. Peterson ,  Edward G. Brown ,  Christopher S. Crean ,  Jose L. Boyer

    发明人： James G. Douglass, III ,  Benjamin R. Yerxa ,  Sammy R. Shaver ,  Ward M. Peterson ,  Edward G. Brown ,  Christopher S. Crean ,  Jose L. Boyer

    IPC分类号： C07H19/20

    CPC分类号： C07H19/10 ,  C07H19/20

    摘要： The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation-resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation-resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides. The mononucleoside phosphate compounds of the present invention are useful in preventing and treating epithelial tissue diseases or diseases or disorders associated with platelet aggregation.

    摘要翻译： 本发明涉及具有二核苷酸药物益处的单核苷磷酸化合物。 这些单核苷酸磷酸酯可以由已经通过在聚磷酸酯单核苷酸的末端磷酸酯上连接降解抗性取代基而被修饰的单核苷酸制成。 通过连接该降解抗性的取代基，降解的稳定性与某些二核苷酸的匹配或超过某些二核苷酸。 本发明的单核苷磷酸化合物可用于预防和治疗与血小板聚集有关的上皮组织疾病或疾病或病症。

    Composition and method for inhibiting platelet aggregation
    5.
    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。

    Drug-eluting stents coated with non-nucleotide P2Y12 receptor antagonist compound
    7.
    发明授权
    Drug-eluting stents coated with non-nucleotide P2Y12 receptor antagonist compound 失效
    涂有非核苷酸P2Y12受体拮抗剂化合物的药物洗脱支架

    公开(公告)号：US07749981B2

    公开(公告)日：2010-07-06

    申请号：US11267941

    申请日：2005-11-04

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

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

    IPC分类号： A01N43/04 ,  A61K31/70

    CPC分类号： A61K31/519 ,  A61F2/82 ,  A61F2250/0067 ,  A61K31/52 ,  A61K31/522 ,  A61K31/7076 ,  A61K31/727 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention provides a drug-eluting stent, wherein the stent is coated with one or more non-nucleotide 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： 本发明提供一种药物洗脱支架，其中支架涂覆有一种或多种非核苷酸P2Y12受体拮抗剂化合物或其药学上可接受的盐，溶剂合物或水合物。 当支架置于狭窄或损伤的动脉血管中时，将治疗有效量的P2Y12受体拮抗剂化合物从支架连续洗脱至支架的局部环境。 P2Y12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。

    METHOD OF TREATING INFLAMMATION
    9.
    发明申请
    METHOD OF TREATING INFLAMMATION 审中-公开
    治疗炎症的方法

    公开(公告)号：US20070249556A1

    公开(公告)日：2007-10-25

    申请号：US11737633

    申请日：2007-04-19

    申请人： Kurt E. Brubaker ,  Sammy R. Shaver ,  James G. Douglass

    发明人： Kurt E. Brubaker ,  Sammy R. Shaver ,  James G. Douglass

    IPC分类号： A61K31/7076

    CPC分类号： A61K31/7076

    摘要： This invention provides methods of preventing and/or treating diseases or conditions associated with inflammation in a mammal, particularly a human. The method comprises administering to a mammal in need thereof an effective amount of a compound of Formula I, IA, or IB, wherein said amount is effective to inhibit inflammation. The invention also provides methods for inhibiting chemotaxis of leukocytes.

    摘要翻译： 本发明提供了预防和/或治疗哺乳动物，特别是人类与炎症有关的疾病或病症的方法。 该方法包括向有需要的哺乳动物施用有效量的式I，IA或IB化合物，其中所述量有效抑制炎症。 本发明还提供了抑制白细胞趋化性的方法。

    P2Y6 RECEPTOR AGONISTS FOR TREATING LUNG DISEASES
    10.
    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。