公开(公告)号：US20070123544A1

公开(公告)日：2007-05-31

申请号：US10576859

申请日：2004-10-21

申请人： Robert Plourde ,  Sammy Shaver ,  Melwyn Abreo ,  Lorenzo Alfaro-Lopez ,  Yangho Feng ,  Tatyana Khasanova ,  Mark Holladay ,  Christopher Crean

发明人： Robert Plourde ,  Sammy Shaver ,  Melwyn Abreo ,  Lorenzo Alfaro-Lopez ,  Yangho Feng ,  Tatyana Khasanova ,  Mark Holladay ,  Christopher Crean

IPC分类号： A61K31/52 ,  A61K31/519

CPC分类号： A61K31/519 ,  A61K31/52

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/or pain associated with diseases. The P2X receptor antagonists useful for this invention are non-nucleotide compounds of general Formula I. Compounds of Formula I can be used alone to treat pain. Compounds of Formula I can also be used in conjunction with other therapeutic agents or adjunctive therapies commonly used to treat pain, thus enhancing the therapeutic effect of pain reduction.

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少疼痛，例如创伤性疼痛，神经性疼痛，器官疼痛和/或与疾病相关的疼痛。 可用于本发明的P2X受体拮抗剂是通式I的非核苷酸化合物。式I化合物可单独用于治疗疼痛。 式I化合物也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，从而增强疼痛减轻的治疗效果。

公开(公告)号：US20070244068A1

公开(公告)日：2007-10-18

申请号：US11285221

申请日：2005-11-21

申请人： James Douglass ,  Benjamin Yerxa ,  Sammy Shaver ,  Ward Peterson ,  Edward Brown ,  Christopher Crean ,  Jose Boyer

发明人： James Douglass ,  Benjamin Yerxa ,  Sammy Shaver ,  Ward Peterson ,  Edward Brown ,  Christopher Crean ,  Jose Boyer

IPC分类号： A61K31/7052 ,  A61P1/00 ,  A61P11/00 ,  A61P27/02 ,  A61P29/00 ,  A61P37/08 ,  A61P7/02 ,  C07H19/052 ,  C07H19/06

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。

公开(公告)号：US20070093446A1

公开(公告)日：2007-04-26

申请号：US11595837

申请日：2006-11-09

申请人： James Douglass ,  Paul Watson ,  Carl Samuelson ,  Christopher Crean

发明人： James Douglass ,  Paul Watson ,  Carl Samuelson ,  Christopher Crean

IPC分类号： A61K31/7076 ,  A61K31/52 ,  C07H19/16 ,  C07D473/02

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P2Y 12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。