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1. 发明授权

US07435724B2 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：US07435724B2
公开(公告)日：2008-10-14
申请号：US11285221
申请日：2005-11-21
申请人： James G. Douglass, III , Benjamin R. Yerxa , Sammy R. Shaver , Ward M. Peterson , Edward G. Brown , Christopher S. Crean , José L. Boyer
发明人： James G. Douglass, III , Benjamin R. Yerxa , Sammy R. Shaver , Ward M. Peterson , Edward G. Brown , Christopher S. Crean , José L. Boyer
IPC分类号： A01N43/04 , A61K31/70
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. 发明授权

US07612047B2 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：US07612047B2
公开(公告)日：2009-11-03
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 , José L. Boyer
发明人： James G. Douglass, III , Benjamin R. Yerxa , Sammy R. Shaver , Ward M. Peterson , Edward G. Brown , Christopher S. Crean , José L. Boyer
IPC分类号： A01N43/04 , A61K31/70
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。

3. 发明申请

US20090076256A1 DEGRADATION-RESISTANT MONONUCLEOSIDE PHOSPHATE COMPOUNDS 失效
标题翻译：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。

4. 发明授权

US07132408B2 Composition and method for inhibiting platelet aggregation 有权
标题翻译：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。

5. 发明申请

US20100197913A1 NON-NUCLEOTIDE COMPOSITION FOR INHIBITING PLATELET AGGREGATION 失效
标题翻译：非核苷酸组合物抑制电极聚集
公开(公告)号：US20100197913A1
公开(公告)日：2010-08-05
申请号：US12552465
申请日：2009-09-02
申请人： Robert Plourde, JR. , Sammy R. Shaver , James G. Douglass, III , Paul S. Watson , José L. Boyer , Chi Tu , Melwyn A. Abreo , Lorenzo J. Alfaro-Lopez , Yangbo Feng , Daniel F. Harvey , Tatyana V. Khasonova
发明人： Robert Plourde, JR. , Sammy R. Shaver , James G. Douglass, III , Paul S. Watson , José L. Boyer , Chi Tu , Melwyn A. Abreo , Lorenzo J. Alfaro-Lopez , Yangbo Feng , Daniel F. Harvey , Tatyana V. Khasonova
IPC分类号： C07D473/34
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。

6. 发明授权

US07749981B2 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：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。

7. 发明授权

US07943760B2 Non-nucleotide composition for inhibiting platelet aggregation 失效
标题翻译：用于抑制血小板聚集的非核苷酸组合物
公开(公告)号：US07943760B2
公开(公告)日：2011-05-17
申请号：US12552465
申请日：2009-09-02
申请人： Robert Plourde, Jr. , Sammy R. Shaver , James G. Douglass, III , Paul S. Watson , José L. Boyer , Chi Tu , Melwyn A. Abreo , Lorenzo J. Alfaro-Lopez , Yangbo Feng , Daniel F. Harvey , Tatyana V. Khasonova
发明人： Robert Plourde, Jr. , Sammy R. Shaver , James G. Douglass, III , Paul S. Watson , José L. Boyer , Chi Tu , Melwyn A. Abreo , Lorenzo J. Alfaro-Lopez , Yangbo Feng , Daniel F. Harvey , Tatyana V. Khasonova
IPC分类号： C07H19/16 , A01N43/04 , A61K31/70
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。

8. 发明授权

US07592445B2 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：US07592445B2
公开(公告)日：2009-09-22
申请号：US11969539
申请日：2008-01-04
申请人： Robert Plourde, Jr. , Sammy R. Shaver , James G. Douglass, III , Paul S. Watson , José L. Boyer , Chi Tu , Melwyn A. Abreo , Lorenzo J. Alfaro-Lopez , Yangbo Feng , Daniel F. Harvey , Tatyana V. Khasonova
发明人： Robert Plourde, Jr. , Sammy R. Shaver , James G. Douglass, III , Paul S. Watson , José L. Boyer , Chi Tu , Melwyn A. Abreo , Lorenzo J. Alfaro-Lopez , Yangbo Feng , Daniel F. Harvey , Tatyana V. Khasonova
IPC分类号： C07H19/16 , A01N43/04 , A61K31/70
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 compounds of Formulae III and V, useful for treating diseases or conditions associated with platelet aggregation.
摘要翻译：本发明涉及式III和V的化合物，其可用于治疗与血小板聚集有关的疾病或病症。

9. 发明授权

US07452870B2 Drug-eluting stents coated with P2Y12 receptor antagonist compound 失效
标题翻译：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
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 , C07H19/00 , C07H19/22
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。

10. 发明申请

US20110054163A1 P2Y6 RECEPTOR AGONISTS FOR TREATING LUNG DISEASES 有权
标题翻译： 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。

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