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1. 发明申请

US20070244068A1 Degradation-resistant mononucleoside phosphate compounds 失效
标题翻译：降解抗性单核苷磷酸化合物
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。

2. 发明申请

US20080103304A1 NON-NUCLEOTIDE COMPOSITION AND METHOD FOR INHIBITING PLATELET AGGREGATION 失效
标题翻译：非核苷酸组合物和抑制血小板聚集的方法
公开(公告)号：US20080103304A1
公开(公告)日：2008-05-01
申请号：US11969539
申请日：2008-01-04
申请人： Robert Plourde , Sammy Shaver , James Douglass , Paul Watson , Jose Boyer , Chi Tu , Melwyn Abreo , Lorenzo Alfaro-Lopez , Yangbo Feng , Daniel Harvey , Tatyana Khasonova
发明人： Robert Plourde , Sammy Shaver , James Douglass , Paul Watson , Jose Boyer , Chi Tu , Melwyn Abreo , Lorenzo Alfaro-Lopez , Yangbo Feng , Daniel Harvey , Tatyana Khasonova
IPC分类号： C07D473/00
CPC分类号： C07D519/00 , A61F2250/0067 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/7076 , A61K31/727 , A61K45/06 , 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 I and III-XII, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae I and III-XII.
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I和III-XII的化合物，或其盐，水合物和溶剂合物。本发明还提供式I和III-XII的新型化合物。

3. 发明申请

US20050267134A1 Non-nucleotide composition and method for inhibiting platelet aggregation 失效
标题翻译：非核苷酸组合物和抑制血小板聚集的方法
公开(公告)号：US20050267134A1
公开(公告)日：2005-12-01
申请号：US11124619
申请日：2005-05-05
申请人： Robert Plourde, , Sammy Shaver , James Douglass, , Paul Watson , Jose Boyer , Chi Tu , Melwyn Abreo , Lorenzo Alfaro-Lopez , Yangbo Feng , Daniel Harvey , Tatyana Khasanova
发明人： Robert Plourde, , Sammy Shaver , James Douglass, , Paul Watson , Jose Boyer , Chi Tu , Melwyn Abreo , Lorenzo Alfaro-Lopez , Yangbo Feng , Daniel Harvey , Tatyana Khasanova
IPC分类号： A61K31/519 , A61K31/522 , A61K31/7076 , A61K31/727 , A61K45/06 , C07D473/12 , A61K31/52
CPC分类号： C07D519/00 , A61F2250/0067 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/7076 , A61K31/727 , A61K45/06 , 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, preferably in a reversible manner. The compounds useful for this invention include compounds of general Formulae I and III-XII, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae I and III-XII.
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，优选以可逆的方式。可用于本发明的化合物包括通式I和III-XII的化合物，或其盐，水合物和溶剂合物。本发明还提供式I和III-XII的新型化合物。

4. 发明申请

US20070015726A1 P2Y6 receptor agonists for treating lung diseases 有权
标题翻译：用于治疗肺部疾病的P2Y6受体激动剂
公开(公告)号：US20070015726A1
公开(公告)日：2007-01-18
申请号：US11478338
申请日：2006-06-28
申请人： Jose Boyer , Sammy Shaver , James Douglass , Catherine Redick
发明人： Jose Boyer , Sammy Shaver , James Douglass , Catherine Redick
IPC分类号： A61K31/7072 , A61K31/7076
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P2Y 6受体激动剂化合物的药物组合物，其中所述量有效激活管腔上的P2Y 6受体肺上皮表面。可用于本发明的P2Y 6受体激动剂化合物包括单核苷5'-二磷酸酯，二核苷单磷酸酯，二核苷二磷酸酯或通式I的二核苷三磷酸盐，或其盐，溶剂合物，水合物。

5. 发明申请

US20060122143A1 Drug-eluting stents coated with P2Y12 receptor antagonist compound 失效
标题翻译：药物洗脱支架涂有P2Y12受体拮抗剂化合物
公开(公告)号：US20060122143A1
公开(公告)日：2006-06-08
申请号：US11267834
申请日：2005-11-04
申请人： Jose Boyer , James Douglass , Sammy Shaver
发明人： Jose Boyer , James Douglass , Sammy Shaver
IPC分类号： A61K31/7076 , A61K31/7072 , C07H19/04 , A61K31/675
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。

6. 发明申请

US20060121086A1 Drug-eluting stents coated with non-nucleotide P2Y12 receptor antagonist compound 失效
标题翻译：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：US20060121086A1
公开(公告)日：2006-06-08
申请号：US11267941
申请日：2005-11-04
申请人： Jose Boyer , James Douglass , Sammy Shaver
发明人： Jose Boyer , James Douglass , Sammy Shaver
IPC分类号： A61K31/519 , A61K31/52 , A61F2/00
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-mucleotide 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：本发明提供药物洗脱支架，其中支架涂覆有一种或多种非核苷酸P2Y 12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，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。

7. 发明申请

US20070123544A1 Non-nucleotide compositions and method for treating pain 失效
标题翻译：非核苷酸组合物和治疗疼痛的方法
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。

8. 发明申请

US20060258614A1 Pyrimidine-based non-nucleotide composition and method for inhibiting platelet aggregation 失效
标题翻译：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：US20060258614A1
公开(公告)日：2006-11-16
申请号：US11413600
申请日：2006-04-28
申请人： James Douglass , Paul Watson , Sammy Shaver , Krzysztof Bednarski
发明人： James Douglass , Paul Watson , Sammy Shaver , Krzysztof Bednarski
IPC分类号： A61K31/7072 , A61K31/513 , C07H19/12 , C07D405/02
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。

9. 发明申请

US20050159388A1 Non-nucleotide compositions and method for inhibiting platelet aggregation 失效
标题翻译：非核苷酸组合物和抑制血小板聚集的方法
公开(公告)号：US20050159388A1
公开(公告)日：2005-07-21
申请号：US10971766
申请日：2004-10-21
申请人： Robert Plourde , Sammy Shaver , Melwyn Abreo , Lorenzo Alfaro-Lopez , Yangbo Feng , Daniel Harvey , Tatyana Khasanova , Chi Tu
发明人： Robert Plourde , Sammy Shaver , Melwyn Abreo , Lorenzo Alfaro-Lopez , Yangbo Feng , Daniel Harvey , Tatyana Khasanova , Chi Tu
IPC分类号： A61K31/00 , A61K31/519 , A61K31/522 , A61K31/7076 , A61K31/727 , A61K45/06 , C07D471/04 , C07D493/04 , C07D519/00
CPC分类号： C07D471/04 , A61K31/00 , A61K31/519 , A61K31/522 , A61K31/7076 , A61K31/727 , A61K45/06 , C07D493/04 , C07D519/00 , 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 I and III-XI, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds according to Formulae I and III-XI.
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I和III-XI的化合物，或其盐，水合物和溶剂合物。本发明还提供了根据式I和III-XI的新化合物。

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