Composition and method for inhibiting platelet aggregation
    1.
    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

    IPC分类号: A01N43/04 A61K31/70

    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。

    Pyrimidine-based non-nucleotide composition and method for inhibiting platelet aggregation
    4.
    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

    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。

    DEGRADATION-RESISTANT MONONUCLEOSIDE PHOSPHATE COMPOUNDS
    5.
    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

    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。

    Drug-eluting stents coated with P2Y12 receptor antagonist compound
    8.
    发明授权
    Drug-eluting stents coated with P2Y12 receptor antagonist compound 失效
    用P2Y 12受体拮抗剂化合物涂覆的药物洗脱支架

    公开(公告)号:US07452870B2

    公开(公告)日:2008-11-18

    申请号:US11267834

    申请日:2005-11-04

    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。

    Drug-eluting stents coated with non-nucleotide P2Y12 receptor antagonist compound
    10.
    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

    IPC分类号: A01N43/04 A61K31/70

    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。