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91. 发明申请

US20090203653A1 Compositions and Methods Using Apocynin Compounds and Nitric Oxide Donors 失效
标题翻译：使用Apocynin化合物和一氧化氮供体的组合物和方法
公开(公告)号：US20090203653A1
公开(公告)日：2009-08-13
申请号：US11664604
申请日：2005-10-03
申请人： David S. Garvey
发明人： David S. Garvey
IPC分类号： A61K31/085 , A61K31/12 , A61K31/655 , A61K31/345 , A61K31/4184 , A61K31/4178 , A61K31/41 , A61K31/55 , A61K31/40 , A61K31/472 , A61K31/502 , A61P9/00
CPC分类号： A61K31/12 , A61K31/198 , A61K2300/00
摘要： The invention describes novel compositions comprising at least one apocynin compound or a pharmaceutically acceptable salt thereof, and at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The invention also provides novel kits comprising at least one apocynin compound or a pharmaceutically acceptable salt thereof, and at least one nitric oxide donor compound, and, optionally, at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating gastrointestinal disorders; (h) treating inflammatory disorders; and (j) treating respiratory disorders. The apocynin compound may preferably be apocynin. The nitric oxide donor compound may preferably be isosorbide dinitrate and/or isosorbide mononitrate.
摘要翻译：本发明描述了包含至少一种助播肽化合物或其药学上可接受的盐和至少一种一氧化氮供体以及任选的至少一种治疗剂的新型组合物。本发明还提供了包含至少一种助播肽化合物或其药学上可接受的盐以及至少一种一氧化氮供体化合物和任选的至少一种治疗剂的新型试剂盒。本发明还提供了（a）治疗心血管疾病的方法; （b）治疗血管性疾病; （c）治疗糖尿病; （d）治疗由氧化应激引起的疾病; （e）治疗内皮功能障碍; （f）治疗由内皮功能障碍引起的疾病; （g）治疗胃肠疾病; （h）治疗炎症性疾病; 和（j）治疗呼吸系统疾病。 apocynin化合物可优选为apocynin。一氧化氮供体化合物可优选为硝酸异山梨酯和/或单硝酸异山梨酯。

92. 发明申请

US20090042819A1 Organic nitric oxide donor salts of antimicrobial compounds, compositions and methods of use 审中-公开
标题翻译：抗微生物化合物的有机一氧化氮供体盐，组合物和使用方法
公开(公告)号：US20090042819A1
公开(公告)日：2009-02-12
申请号：US11883445
申请日：2006-02-16
申请人： James L. Ellis , David S. Garvey , Chia-En Lin
发明人： James L. Ellis , David S. Garvey , Chia-En Lin
IPC分类号： A61K31/7036 , C07H15/234 , C07D205/085 , A61K31/427 , C07D215/56 , A61K31/4709 , C07D477/00 , A61K31/397 , A61P31/04
CPC分类号： C07H5/04 , C07H5/06 , C07H15/00 , C07H17/00
摘要： The invention describes novel organic nitric oxide donor salts of a antimicrobial compounds, and novel compositions and kits comprising at least one organic nitric oxide donor salt of an antimicrobial compound, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating bacterial infections; (b) treating viral infections; (c) treating fungal infections; and (d) treating lesions. In one embodiment the antimicrobial compounds of the invention are aztreonam, ciprofloxacin, doripenam, duramycin and tobramycin. The organic nitric oxide donors that form salts are preferably organic nitrates, organic nitrites, nitrosothiols, thionitrites and heterocyclic nitric oxide donors. The heterocyclic nitric oxide donors are preferably furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines. The methods of the invention are preferably for the treatment of bacterial infections associated with pulmonary diseases such as cystic fibrosis and for treating Bacillus anthracis infections.
摘要翻译：本发明描述了抗微生物化合物的新型有机一氧化氮供体盐，以及包含至少一种抗微生物化合物的有机一氧化氮供体盐，和任选地至少一种一氧化氮增强化合物和/或至少一种治疗剂。本发明还提供了（a）治疗细菌感染的方法; （b）治疗病毒感染; （c）治疗真菌感染; 和（d）治疗病变。在一个实施方案中，本发明的抗微生物化合物是氨曲南，环丙沙星，多瑞培南，杜氏霉素和妥布霉素。形成盐的有机一氧化氮供体优选为有机硝酸盐，有机亚硝酸盐，亚硝基硫醇，硫堇啶和杂环一氧化氮供体。杂环一氧化氮供体优选呋喃香糖，苏氨酸亚胺，氧杂三唑-5-酮和/或氧杂三唑-5-亚胺。本发明的方法优选用于治疗与肺部疾病如囊性纤维化相关的细菌感染和用于治疗炭疽芽孢杆菌感染。

93. 发明申请

US20080293702A1 Nitric Oxide Enhancing Pyruvate Compounds, Compositions and Methods of Use 审中-公开
标题翻译：一氧化氮增强丙酮酸盐化合物，组合物和使用方法
公开(公告)号：US20080293702A1
公开(公告)日：2008-11-27
申请号：US12096867
申请日：2006-12-19
申请人： David S. Garvey
发明人： David S. Garvey
IPC分类号： A61K31/546 , C07D271/08 , A61K31/4245 , A61K31/42 , C07D273/00 , C07D413/04 , A61K31/5377 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12
CPC分类号： A61K31/421 , A61K31/537
摘要： The invention provides novel compositions and kits comprising at least one nitric oxide enhancing pyruvate compound, or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension (n) treating reperfusion injury following ischemia; and/or (m) preserving tissues, organs, organ parts and/or limbs. The nitric oxide enhancing pyruvate compounds comprise at least one nitroxide group.
摘要翻译：本发明提供了包含至少一种一氧化氮增强丙酮酸化合物或其药学上可接受的盐，和任选的至少一种一氧化氮增强化合物和/或至少一种治疗剂的新型组合物和试剂盒。本发明还提供了（a）治疗心血管疾病的方法; （b）治疗血管性疾病; （c）治疗糖尿病; （d）治疗由氧化应激引起的疾病; （e）治疗内皮功能障碍; （f）治疗由内皮功能障碍引起的疾病; （g）治疗肝硬化; （h）治疗先兆子痫; （j）治疗骨质疏松症; （k）治疗肾病; （l）治疗外周血管疾病; （m）治疗门静脉高压（n）治疗缺血后再灌注损伤; 和/或（m）保存组织，器官，器官部分和/或肢体。一氧化氮增强丙酮酸化合物包含至少一个氮氧自由基。

94. 发明申请

US20080287407A1 Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 审中-公开
标题翻译：一氧化氮释放丙酮酸盐化合物，组合物和使用方法
公开(公告)号：US20080287407A1
公开(公告)日：2008-11-20
申请号：US10581340
申请日：2004-12-10
申请人： David S. Garvey , Xinqin Fang , Subhash P. Khanapure , Ramani R. Ranatunga , Shiow-Jyi Wey
发明人： David S. Garvey , Xinqin Fang , Subhash P. Khanapure , Ramani R. Ranatunga , Shiow-Jyi Wey
IPC分类号： A61K31/585 , C07D211/60 , A61K31/445 , A61K31/164 , C07C233/13 , A61K31/4245 , C07D271/08 , A61P9/00 , A61P9/10 , A61P9/12 , A61P3/10
CPC分类号： C07C203/04 , C07C219/22 , C07C235/74 , C07D211/46 , C07D271/08 , C07D273/00 , C07D333/32
摘要： The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
摘要翻译：本发明描述了新的亚硝基化和/或亚硝基化的丙酮酸盐化合物及其药学上可接受的盐，以及包含至少一种亚硝基化和/或亚硝基化丙酮酸盐化合物的新组合物，以及任选的至少一种捐赠，转移或释放一氧化氮的化合物，一氧化氮的内源性合成，提高内源性内源性松弛因子水平，或者是一氧化氮合成酶的底物和/或至少一种治疗剂。本发明还提供了包含至少一种丙酮酸化合物和至少一种捐赠，转移或释放一氧化氮的化合物的新型组合物，提高内源性内皮衍生的舒张因子水平，刺激一氧化氮的内源性合成，或是一氧化氮合酶的底物和/或至少一种治疗剂。本发明还提供了包含至少一种丙酮酸盐化合物，其任选被亚硝化和/或亚硝基化的新的试剂盒，以及任选的至少一种一氧化氮供体和/或至少一种治疗剂。本发明还提供了治疗由氧化应激，糖尿病，缺血后的再灌注损伤，组织，器官，器官部分和/或肢体的保存引起的疾病的方法。

95. 发明申请

US20080268014A1 Furoxan Compounds, Compositions and Methods of Use 失效
标题翻译：呋喃糖化合物，组合物和使用方法
公开(公告)号：US20080268014A1
公开(公告)日：2008-10-30
申请号：US12093561
申请日：2006-11-16
申请人： David S. Garvey , Ramani R. Ranatunge
发明人： David S. Garvey , Ramani R. Ranatunge
IPC分类号： A61K9/00 , C07D271/08 , A61K31/4245 , A61P9/00 , A61K31/502 , A61K33/00
CPC分类号： C07D271/08
摘要： The invention provides novel furoxan compounds, or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one compound, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for (a) treating cardiovascular diseases; (b) inhibiting platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device; (c) treating pathological conditions resulting from abnormal cell proliferation; (d) treating transplantation rejections, (e) treating autoimmune, inflammatory, proliferative, hyperproliferative or vascular diseases; (f) reducing scar tissue or for inhibiting wound contraction; (g) treating diseases resulting from oxidative stress; (h) treating endothelial dysfunctions; and (j) treating diseases caused by endothelial dysfunctions.
摘要翻译：本发明提供了新的呋喃糖化合物或其药学上可接受的盐，以及包含至少一种化合物和任选的至少一种一氧化氮增强化合物和/或至少一种治疗剂的新组合物。本发明的化合物和组合物也可以结合到基质上。本发明还提供了（a）治疗心血管疾病的方法; （b）抑制由血液暴露于医疗器械引起的血小板聚集和血小板粘附; （c）治疗由异常细胞增殖引起的病理状况; （d）治疗移植排斥，（e）治疗自身免疫性，炎症性，增殖性，过度增殖性或血管性疾病; （f）减少瘢痕组织或抑制伤口收缩; （g）治疗由氧化应激引起的疾病; （h）治疗内皮功能障碍; 和（j）治疗由内皮功能障碍引起的疾病。

96. 发明授权

US07442802B2 Cyclooxygenase-2 selective inhibitors, compositions and methods of use 失效
标题翻译：环氧合酶-2选择性抑制剂，组合物和使用方法
公开(公告)号：US07442802B2
公开(公告)日：2008-10-28
申请号：US11418187
申请日：2006-05-05
申请人： Upul K. Bandarage , Richard A. Earl , Maiko Ezawa , Xinqin Fang , David S. Garvey , Subhash P. Khanapure , Ramani R. Ranatunge , Stewart K. Richardson , Joseph D. Schroeder , Cheri A. Stevenson , Shiow-Jyi Wey
发明人： Upul K. Bandarage , Richard A. Earl , Maiko Ezawa , Xinqin Fang , David S. Garvey , Subhash P. Khanapure , Ramani R. Ranatunge , Stewart K. Richardson , Joseph D. Schroeder , Cheri A. Stevenson , Shiow-Jyi Wey
IPC分类号： A61K31/415 , C07D231/12
CPC分类号： C07D231/12 , C07D261/08 , C07D401/04
摘要： The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
摘要翻译：本发明描述了新型环氧合酶2（COX-2）选择性抑制剂和包含至少一种环氧合酶2（COX-2）选择性抑制剂的新型组合物，以及任选地至少一种捐赠，转移或释放一氧化氮的化合物，刺激内源性合成的一氧化氮，提高内源性内源性释放因子水平，或者是一氧化氮合酶的底物和/或至少一种治疗剂。本发明还提供了包含至少一种COX-2选择性抑制剂，任选地亚硝基化和/或亚硝基化的新的试剂盒，以及任选的至少一种一氧化氮供体，和/或任选的至少一种治疗剂。本发明的新型环加氧酶2选择性抑制剂可以任选地亚硝化和/或亚硝化。本发明还提供了治疗炎症，疼痛和发烧的方法; 用于治疗和/或改善COX-2选择性抑制剂的胃肠性质; 促进伤口愈合; 用于治疗和/或预防肾和/或呼吸毒性; 用于治疗和/或预防由环氧合酶-2水平升高引起的其他疾病; 并用于改善COX-2选择性抑制剂的心血管外形。

97. 发明授权

US07220749B2 Nitrosated and/or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use 失效
标题翻译：亚硝化和/或亚硝基化的环氧合酶-2选择性抑制剂，组合物和使用方法
公开(公告)号：US07220749B2
公开(公告)日：2007-05-22
申请号：US10718060
申请日：2003-06-10
申请人： L. Gordon Letts , David S. Garvey
发明人： L. Gordon Letts , David S. Garvey
IPC分类号： A61K31/495 , A61K31/216 , A61K31/34 , C07D241/04 , C07D493/04 , C07C229/42
CPC分类号： C07D295/185 , A61K45/06 , C07C229/42 , C07C317/18 , C07C323/12 , C07D493/04
摘要： The invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent. The invention also provides novel compositions comprising at least one COX-2 selective inhibitor, that is optionally sitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.
摘要翻译：本发明描述了新的亚硝化和/或亚硝基化的环氧合酶2（COX-2）选择性抑制剂和包含至少一种亚硝化和/或亚硝基化的环氧合酶2（COX-2）选择性抑制剂的新组合物，和任选的至少一种可以提供的化合物，转移或释放一氧化氮，刺激一氧化氮的内源性合成，升高内源性内源性松弛因子水平，或者是一氧化氮合酶的底物和/或任选的至少一种治疗剂。本发明还提供了包含至少一种COX-2选择性抑制剂（其任选被亚硝化和/或亚硝基化）和任选地至少一种一氧化氮供体和/或至少一种治疗剂的新型组合物。

98. 发明授权

US07211590B2 Nitrosated proton pump inhibitors, compositions and methods of use 失效
标题翻译：亚硝化质子泵抑制剂，组合物和使用方法
公开(公告)号：US07211590B2
公开(公告)日：2007-05-01
申请号：US10631782
申请日：2003-08-01
申请人： Xinqin Fang , David S. Garvey , L. Gordon Letts
发明人： Xinqin Fang , David S. Garvey , L. Gordon Letts
IPC分类号： C07D401/04 , A61K31/44
CPC分类号： C07D401/12
摘要： The invention describes novel nitrosated proton pump inhibitor compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated proton pump inhibitor compound, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti-Helicobacter pylori properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating bacterial infections and/or viral infections.
摘要翻译：本发明描述了新的亚硝化质子泵抑制剂化合物及其药学上可接受的盐，以及包含至少一种亚硝化质子泵抑制剂化合物和任选的至少一种捐赠，转移或释放一氧化氮的化合物，刺激内源性硝酸合成的新型组合物氧化物，提高内源性内源性水平的内源性松弛因子，或者是一氧化氮合酶的底物和/或至少一种治疗剂。本发明还提供了包含至少一种亚硝化质子泵抑制剂化合物和至少一种捐赠，转移或释放一氧化氮的化合物的新型组合物，提高内源性内皮衍生的松弛因子水平，刺激一氧化氮的内源性合成或是底物用于一氧化氮合酶和/或至少一种治疗剂。本发明还提供了包含至少一种亚硝化质子泵抑制剂化合物和任选的至少一种一氧化氮供体和/或至少一种治疗剂的新型试剂盒。本发明还提供了治疗胃肠道疾病的方法; 促进溃疡愈合; 减少溃疡复发; 改善胃保护性质，抗幽门螺旋杆菌性质或质子泵抑制剂的抗酸性; 降低或减少与使用非甾体抗炎化合物相关的胃肠道毒性; 治疗细菌感染和/或病毒感染。

99. 发明授权

US07138430B2 Nitrosated and nitrosylated nebivolol and its metabolites, compositions and methods of use 失效
标题翻译：硝基化和亚硝基化奈比洛尔及其代谢物，组合物和使用方法
公开(公告)号：US07138430B2
公开(公告)日：2006-11-21
申请号：US10695644
申请日：2003-10-29
申请人： David S. Garvey
发明人： David S. Garvey
IPC分类号： A61K31/352 , C07D311/04
CPC分类号： A61K31/353 , C07D311/22 , C07D311/58
摘要： The invention describes novel nitrosated and/or nitrosylated nebivolol, novel nitrosated and/or nitrosylated metabolites of nebivolol and novel compositions comprising at least one nitrosated and/or nitrosylated nebivolol and/or at least one nitrosated and/or nitrosylated metabolite of nebivolol, and, optionally, at least one nitric oxide donor and/or at least one antioxidant or a pharmaceutically acceptable salt thereof, and/or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and/or at least one nitrosated compound used to treat cardiovascular diseases. The invention also provides novel compositions comprising nebivolol and/or at least one metabolite of nebivolol and at least one nitric oxide donor, and, optionally, at least one antioxidant or a pharmaceutically acceptable salt thereof, and/or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and/or at least one nitrosated compound used to treat cardiovascular diseases. The compounds and compositions of the invention can also be bound to a matrix. The nitric oxide donor is a compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof. The invention also provides methods for treating and/or preventing vascular diseases characterized by nitric oxide insufficiency; and for treating and/or preventing Raynaud's syndrome; and for treating and/or preventing cardiovascular diseases or disorders.
摘要翻译：本发明描述新的亚硝基化和/或亚硝基化的奈比洛尔，奈比洛尔的新亚硝化和/或亚硝基化代谢物和新组合物，其包含至少一种亚硝基和/或亚硝基化的奈必洛尔和/或至少一种亚硝基和/或亚硝基化的奈必洛尔代谢物，任选地，至少一种一氧化氮供体和/或至少一种抗氧化剂或其药学上可接受的盐，和/或至少一种用于治疗心血管疾病的化合物或其药学上可接受的盐，和/或至少一种使用的亚硝化化合物治疗心血管疾病。本发明还提供新的组合物，其包含奈比洛尔和/或至少一种奈比洛尔代谢物和至少一种一氧化氮供体，以及任选的至少一种抗氧化剂或其药学上可接受的盐，和/或至少一种用于治疗的化合物心血管疾病或其药学上可接受的盐，和/或用于治疗心血管疾病的至少一种亚硝化化合物。本发明的化合物和组合物也可以结合到基质上。一氧化氮供体是一种捐赠，转移或释放一氧化氮的化合物，提高内源性内皮衍生的松弛因子水平，刺激一氧化氮的内源性合成，或是一氧化氮合酶的底物，并且可以优选为硝酸异山梨酯和/或异山梨醇一硝酸盐抗氧化剂可优选为肼屈嗪化合物或其药学上可接受的盐。本发明还提供治疗和/或预防以一氧化氮不足为特征的血管疾病的方法; 并用于治疗和/或预防雷诺氏综合征; 并用于治疗和/或预防心血管疾病或病症。

100. 发明授权

US06930113B2 Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use 失效
公开(公告)号：US06930113B2
公开(公告)日：2005-08-16
申请号：US10216886
申请日：2002-08-13
申请人： David S. Garvey , Inigo Saenz de Tejada , Richard A. Earl , Subhash P. Khanapure
发明人： David S. Garvey , Inigo Saenz de Tejada , Richard A. Earl , Subhash P. Khanapure
IPC分类号： A61K31/075 , A61K31/137 , A61K31/198 , A61K31/4015 , A61K31/4188 , A61K31/444 , A61K31/4745 , A61K31/4985 , A61K31/501 , A61K31/519 , A61K31/52 , A61K31/522 , C07D207/12 , C07D213/89 , C07D215/227 , C07D237/04 , C07D279/04 , C07D401/02 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/04 , C07D403/10 , C07D471/04 , C07D471/14 , C07D473/30 , C07D487/02 , C07D487/04 , C07D487/14
CPC分类号： A61K31/195 , A61K31/075 , A61K31/21 , A61K31/34 , A61K31/40 , A61K31/44 , A61K31/47 , A61K31/4709 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/519 , A61K45/06 , C07D405/14 , C07D487/04
摘要： The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing diseases induced by the increased metabolism of cyclic guanosine 3′,5′-monophosphate (cGMP), such as hypertension, pulmonary hypertension, congestive heart failure, renal failure, myocardial infraction, stable, unstable and variant (Prinzmetal) angina, atherosclerosis, cardiac edema, renal insufficiency, nephrotic edema, hepatic edema, stroke, asthma, bronchitis, chronic obstructive pulmonary disease (COPD), cystic fibrosis, dementia, immunodeficiency, premature labor, dysmenorrhoea, benign prostatic hyperplasis (BPH), bladder outlet obstruction, incontinence, conditions of reduced blood vessel patency, e.g., postpercutaneous transluminal coronary angioplasty (post-PTCA), peripheral vascular disease, allergic rhinitis, glucoma, and diseases characterized by disorders of gut motility, e.g., irritable bowel syndrome (IBS).

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