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    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。

    Composition and method for inhibiting platelet aggregation
    6.
    发明授权
    Composition and method for inhibiting platelet aggregation 失效
    抑制血小板聚集的组合物和方法

    公开(公告)号：US07018985B1

    公开(公告)日：2006-03-28

    申请号：US09643138

    申请日：2000-08-21

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

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

    IPC分类号： A61K31/70 ,  C07H19/20

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

    摘要： The present invention provides novel compounds of dinucleotide polyphosphates and the method of preventing or treating diseases or conditions associated with platelet aggregation. The method comprises administering systemically to a patient a pharmaceutical comprising a purinergic P2τ receptor antagonist, in an amount effective to elevate its extracellular concentration to bind to P2τ receptors and inhibit P2τ receptor-mediated platelet aggregation. Methods of systemic administration include injection by intravenous, intramuscular, intrasternal and intravitreal routes, infusion, transdermal administration, oral administration, rectal administration and intra-operative instillation.

    摘要翻译： 本发明提供新的二核苷酸多磷酸化合物，以及预防或治疗与血小板聚集有关的疾病或病症的方法。 所述方法包括以有效提高其细胞外浓度结合P2A受体并且抑制P2的药物全身给予患者包含嘌呤能P2A受体拮抗剂的药物 受体介导的血小板聚集。 全身给药方法包括通过静脉注射，肌内注射，胸骨内和玻璃体内注射，输液，透皮给药，口服给药，直肠给药和术中滴注。

    Method for treating pain
    7.
    发明授权
    Method for treating pain 失效
    治疗疼痛的方法

    公开(公告)号：US06881725B2

    公开(公告)日：2005-04-19

    申请号：US10355699

    申请日：2003-01-31

    申请人： Benjamin R. Yerxa ,  Ward M. Peterson ,  Christopher S. Crean

    发明人： Benjamin R. Yerxa ,  Ward M. Peterson ,  Christopher S. Crean

    IPC分类号： C07H19/20 ,  A61K31/675 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/7084 ,  A61P23/00 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  C07H19/207 ,  C07H21/00 ,  A61K31/70

    CPC分类号： A61K31/7076 ,  A61K31/675 ,  A61K31/7072 ,  A61K31/7084 ,  Y10S514/851

    摘要： The present invention is directed to a method of treating pain. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a P2X receptor antagonist. The methods of the present invention are useful in reducing pain, such as traumatic pain, neuropathic pain, organ pain and pain associated with diseases. The P2X receptor antagonists particularly useful for this invention are mononucleoside polyphosphate derivatives or dinucleoside polyphosphate derivatives of general Formula I. The compounds of the present method can be used alone to treat pain. The compounds of the present method can also be used in conjunction with other therapeutic agents or adjunctive therapies commonly used to treat pain, thus enhancing the overall pain-reducing effect in a subject in need of such treatment.

    摘要翻译： 本发明涉及治疗疼痛的方法。 该方法包括向受试者施用包含有效量的P2X受体拮抗剂的药物组合物。 本发明的方法可用于减轻疼痛，例如创伤性疼痛，神经性疼痛，器官疼痛和与疾病相关的疼痛。 特别可用于本发明的P2X受体拮抗剂是通式I的单核苷多磷酸衍生物或二核苷多磷酸衍生物。本发明方法的化合物可单独用于治疗疼痛。 本发明方法的化合物还可以与通常用于治疗疼痛的其它治疗剂或辅助疗法结合使用，从而增强需要这种治疗的受试者的整体疼痛减轻作用。

    Method for reducing intraocular pressure using indole derivatives
    9.
    发明授权
    Method for reducing intraocular pressure using indole derivatives 失效
    使用吲哚衍生物降低眼内压的方法

    公开(公告)号：US06730707B2

    公开(公告)日：2004-05-04

    申请号：US09915486

    申请日：2001-07-25

    申请人： Jesus J. Pintor ,  Maria A. Peral ,  Ward M. Peterson ,  Robert Plourde, Jr. ,  Edward G. Brown ,  Benjamin R. Yerxa

    发明人： Jesus J. Pintor ,  Maria A. Peral ,  Ward M. Peterson ,  Robert Plourde, Jr. ,  Edward G. Brown ,  Benjamin R. Yerxa

    IPC分类号： A61K4732

    CPC分类号： A61K31/404 ,  A61K31/4045 ,  A61K31/55 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention provides a method of reducing intraocular pressure by administering pharmaceutical compositions comprising indole derivatives. The pharmaceutical compositions useful in this invention comprise indole derivatives and melatonin analogs of Formulae I-IV. A preferred embodiment is a method of lowering intraocular pressure using 5-(methoxycarbonylamino)-N-acetyltryptamine (5-MCA-NAT), also known as GR 135531, which has a prolonged duration of action and greater efficacy in lowering intraocular pressure compared to melatonin. The present invention further provides a method of treating disorders associated with ocular hypertension, and a method of treating various forms of glaucoma; the method comprises administering an effective dose of a pharmacuetical composition comprising an indole derivative with or without agents commonly used to treat such disorders.

    摘要翻译： 本发明提供通过给药包含吲哚衍生物的药物组合物降低眼内压的方法。 用于本发明的药物组合物包含式I-IV的吲哚衍生物和褪黑素类似物。 优选的实施方案是使用5-（甲氧基羰基氨基）-N-乙酰基色胺（5-MCA-NAT）（也称为GR135531）降低眼内压的方法，其具有延长的作用时间和降低眼内压的更高功效， 褪黑激素 本发明还提供了治疗与高眼压相关的疾病的方法和治疗各种形式的青光眼的方法; 该方法包括施用有效剂量的药物组合物，所述药物组合物包含吲哚衍生物，所述药物组合物含或不含通常用于治疗所述疾病的试剂。