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1. 发明授权

US07772278B2 Nitrosated and nitrosylated prostaglandins, compositions and methods of use 失效
标题翻译：亚硝化和亚硝酰化前列腺素，组合物和使用方法
公开(公告)号：US07772278B2
公开(公告)日：2010-08-10
申请号：US12237117
申请日：2008-09-24
申请人： David S. Garvey , Ricky D. Gaston , L. Gordon Letts , Inigo Saenz de Tejada , Sang William Tam , Manuel Worcel
发明人： David S. Garvey , Ricky D. Gaston , L. Gordon Letts , Inigo Saenz de Tejada , Sang William Tam , Manuel Worcel
IPC分类号： A61K31/557 , C07C405/00
CPC分类号： A61K31/5575
摘要： The invention describes novel nitrosated and/or nitrosylated prostaglandins, and novel compositions comprising at least one nitrosated and/or nitrosylated prostaglandin, and, optionally, 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 vasoactive agent. The invention also provides novel compositions comprising at least one prostaglandin and at least one S-nitrosothiol compound, and, optionally, at least one vasoactive agent. The prostaglandin is preferably a prostaglandin E1 compound, more preferably alprostadil, and the S-nitrosothiol compound is preferably S-nitrosoglutathione. The 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 cerebrovascular disorders, cardiovascular disorders, benign prostatic hyperplasia (BPH), glaucoma, peptic ulcers or for inducing abortions.
摘要翻译：本发明描述了新的亚硝化和/或亚硝基化的前列腺素，以及包含至少一种亚硝化和/或亚硝基化的前列腺素的新组合物，以及任选的至少一种捐赠，转移或释放一氧化氮的化合物，提高内源性内皮水平的放松因子，刺激一氧化氮的内源性合成或是一氧化氮合酶的底物和/或至少一种血管活性剂。本发明还提供了包含至少一种前列腺素和至少一种S-亚硝基硫醇化合物和任选的至少一种血管活性剂的新型组合物。前列腺素优选为前列腺素E1化合物，更优选前列地尔，S-亚硝基硫醇化合物优选为S-亚硝基谷胱甘肽。本发明还提供用于治疗或预防男性和女性的性功能障碍的方法，用于增强男性和女性的性反应，以及用于治疗或预防脑血管疾病，心血管疾病，良性前列腺增生（BPH），青光眼，消化性溃疡或诱导堕胎

2. 发明授权

US07754772B2 Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use 有权
标题翻译：硝化非甾体抗炎化合物，组合物和使用方法
公开(公告)号：US07754772B2
公开(公告)日：2010-07-13
申请号：US11134358
申请日：2005-05-23
申请人： Richard A. Earl , Maiko Ezawa , Xinqin Fang , David S. Garvey , Ricky D. Gaston , Subhash P. Khanapure , L. Gordon Letts , Chia-En Lin , Ramani R. Ranatunge , Stewart K. Richardson , Joseph D. Schroeder , Cheri A. Stevenson , Shiow-Jyi Wey
发明人： Richard A. Earl , Maiko Ezawa , Xinqin Fang , David S. Garvey , Ricky D. Gaston , Subhash P. Khanapure , L. Gordon Letts , Chia-En Lin , Ramani R. Ranatunge , Stewart K. Richardson , Joseph D. Schroeder , Cheri A. Stevenson , Shiow-Jyi Wey
IPC分类号： A61K31/135 , C07C203/04
CPC分类号： C07D493/04 , C07C291/02 , C07C311/17 , C07C317/18 , C07C323/12 , C07C327/28 , C07D209/18 , C07D211/22 , C07D211/56
摘要： The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, 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 NSAID, 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 NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.
摘要翻译：本发明描述了新型亚硝化非甾体抗炎药（NSAID）及其药学上可接受的盐，以及包含至少一种亚硝化NSAID的新组合物，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NSAID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，或是一氧化氮的底物合酶和/或至少一种治疗剂。本发明还提供了包含至少一种亚硝化NSAID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炎症，疼痛和发烧的方法; 用于治疗胃肠道疾病; 促进伤口愈合; 用于治疗和/或预防由使用非甾体抗炎化合物引起的胃肠道，肾脏和/或呼吸道毒性物质; 用于治疗炎性疾病状态和/或病症; 并用于治疗和/或预防眼科疾病和/或病症。

3. 发明授权

US07595313B2 Nitric oxide donating diuretic compounds, compositions and methods of use 失效
标题翻译：一氧化氮供应利尿剂，组合物和使用方法
公开(公告)号：US07595313B2
公开(公告)日：2009-09-29
申请号：US12136531
申请日：2008-06-10
申请人： David S. Garvey , L. Gordon Letts , Richard A. Earl , Maiko Ezawa , Xinqin Fang , Ricky D. Gaston , Subhash P. Khanapure , Chia-En Lin , Ramani R. Ranatunge , Cheri A. Stevenson , Shiow-Jyi Wey
发明人： David S. Garvey , L. Gordon Letts , Richard A. Earl , Maiko Ezawa , Xinqin Fang , Ricky D. Gaston , Subhash P. Khanapure , Chia-En Lin , Ramani R. Ranatunge , Cheri A. Stevenson , Shiow-Jyi Wey
IPC分类号： C07D285/24 , C07D417/04 , C07D513/10 , A61K31/549
CPC分类号： C07D285/30 , C07D285/28 , C07D285/32 , C07D417/04 , C07D417/06 , C07D513/10
摘要： The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts 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 conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia. The nitric oxide enhancing diuretic compounds comprise at least one nitric oxide enhancing group linked to the diuretic compound through one or more sites such as carbon, oxygen and/or nitrogen via a bond or moiety that cannot be hydrolyzed.
摘要翻译：本发明描述了包含至少一种一氧化氮增强利尿剂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）处理由过量水和/或电解质滞留导致的条件的方法; （二）治疗心血管疾病; （c）治疗血管性疾病; （d）治疗糖尿病; （e）治疗由氧化应激引起的疾病; （f）治疗内皮功能障碍; （g）治疗由内皮功能障碍引起的疾病; （h）治疗肝硬化; （j）治疗先兆子痫; （k）治疗骨质疏松症; （l）治疗肾病; （m）治疗外周血管疾病; （n）治疗门静脉高压; （o）治疗中枢神经系统疾病; （p）治疗代谢综合征; （q）治疗性功能障碍; 和（r）高脂血症。一氧化氮增强利尿化合物包含通过一个或多个位点如碳，氧和/或氮通过不能水解的键或部分与利尿剂化合物连接的至少一个一氧化氮增强基团。

4. 发明申请

US20120058989A1 ANTIBACTERIAL FLUOROQUINOLONE ANALOGS 审中-公开
标题翻译：抗生素荧光素类似物
公开(公告)号：US20120058989A1
公开(公告)日：2012-03-08
申请号：US13082269
申请日：2011-04-07
申请人： Allan S. Wagman , Heinz E. Moser , Glenn A. McEnroe , James B. Aggen , Martin S. Linsell , Adam A. Goldblum , John H. Griffin , Lloyd J. Simons , Thomas R. Belliotti , Christina R. Harris , Toni-Jo Poel , Michael J. Melnick , Ricky D. Gaston
发明人： Allan S. Wagman , Heinz E. Moser , Glenn A. McEnroe , James B. Aggen , Martin S. Linsell , Adam A. Goldblum , John H. Griffin , Lloyd J. Simons , Thomas R. Belliotti , Christina R. Harris , Toni-Jo Poel , Michael J. Melnick , Ricky D. Gaston
IPC分类号： A61K31/553 , A61P31/04 , C07D498/14 , C07D471/14 , A61K31/55 , A61K31/5517
CPC分类号： C07D471/14 , C07D498/14 , C07D513/14
摘要： Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein A, B, D, E, G, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译：公开了具有抗菌活性的化合物。该化合物具有以下结构（I）：包括其立体异构体，药学上可接受的盐和前药，其中A，B，D，E，G，R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所定义。还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。

5. 发明申请

US20100137291A1 NITROSATED NONSTEROIDAL ANTIINFLAMMATORY COMPOUNDS, COMPOSITIONS AND METHODS OF USE 有权
公开(公告)号：US20100137291A1
公开(公告)日：2010-06-03
申请号：US12636316
申请日：2009-12-11
申请人： Richard A. EARL , Maiko EZAWA , Xinqin FANG , David S. GARVEY , Ricky D. GASTON , Subhash P. KHANAPURE , L. Gordon LETTS , Chia-En LIN , Ramani R. RANATUNGA , Stewart K. RICHARDSON , Joseph D. SCHROEDER , Cheri A. STEVENSON , Shiow-Jyi WEY
发明人： Richard A. EARL , Maiko EZAWA , Xinqin FANG , David S. GARVEY , Ricky D. GASTON , Subhash P. KHANAPURE , L. Gordon LETTS , Chia-En LIN , Ramani R. RANATUNGA , Stewart K. RICHARDSON , Joseph D. SCHROEDER , Cheri A. STEVENSON , Shiow-Jyi WEY
IPC分类号： A61K31/5415 , A61K31/437 , A61K31/436 , A61K31/426 , A61K31/421 , A61K31/416 , A61K31/404 , A61K31/40 , A61K31/381 , C07D279/22 , C07D263/56 , C07D231/56 , C07D231/10 , C07D491/052 , C07D209/34 , C07D209/12 , C07D333/22 , A61P35/00 , A61P1/00 , A61P29/00
CPC分类号： C07D493/04 , C07C291/02 , C07C311/17 , C07C317/18 , C07C323/12 , C07C327/28 , C07D209/18 , C07D211/22 , C07D211/56
摘要： The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, 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 NSAID, 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 NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.

6. 发明申请

US20090088366A1 NITROSATED AND NITROSYLATED PROSTAGLANDINS, COMPOSITIONS AND METHODS OF USE 失效
标题翻译：硝基和硝基化前体，组合物和使用方法
公开(公告)号：US20090088366A1
公开(公告)日：2009-04-02
申请号：US12237117
申请日：2008-09-24
申请人： David S. Garvey , Ricky D. Gaston , Inigo Saenz de Tejada , Sang William Tam , Manuel Worcel
发明人： David S. Garvey , Ricky D. Gaston , Inigo Saenz de Tejada , Sang William Tam , Manuel Worcel
IPC分类号： A61K38/02 , A61K31/215 , A61K31/4164 , A61K31/4375 , A61P15/00 , A61K31/496 , A61K31/7076
CPC分类号： A61K31/5575
摘要： The invention describes novel nitrosated and/or nitrosylated prostaglandins, and novel compositions comprising at least one nitrosated and/or nitrosylated prostaglandin, and, optionally, 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 vasoactive agent. The invention also provides novel compositions comprising at least one prostaglandin and at least one S-nitrosothiol compound, and, optionally, at least one vasoactive agent. The prostaglandin is preferably a prostaglandin E1 compound, more preferably alprostadil, and the S-nitrosothiol compound is preferably S-nitrosoglutathione. The 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 cerebrovascular disorders, cardiovascular disorders, benign prostatic hyperplasia (BPH), glaucoma, peptic ulcers or for inducing abortions.
摘要翻译：本发明描述了新的亚硝化和/或亚硝基化的前列腺素，以及包含至少一种亚硝化和/或亚硝基化的前列腺素的新组合物，以及任选的至少一种捐赠，转移或释放一氧化氮的化合物，提高内源性内皮水平的放松因子，刺激一氧化氮的内源性合成或是一氧化氮合酶的底物和/或至少一种血管活性剂。本发明还提供了包含至少一种前列腺素和至少一种S-亚硝基硫醇化合物和任选的至少一种血管活性剂的新型组合物。前列腺素优选为前列腺素E1化合物，更优选前列地尔，S-亚硝基硫醇化合物优选为S-亚硝基谷胱甘肽。本发明还提供用于治疗或预防男性和女性的性功能障碍的方法，用于增强男性和女性的性反应，以及用于治疗或预防脑血管疾病，心血管疾病，良性前列腺增生（BPH），青光眼，消化性溃疡或诱导堕胎

7. 发明授权

US07449595B2 Nitrosated and nitrosylated prostaglandins, compositions and methods of use 失效
标题翻译：亚硝化和亚硝酰化前列腺素，组合物和使用方法
公开(公告)号：US07449595B2
公开(公告)日：2008-11-11
申请号：US11641050
申请日：2006-12-19
申请人： David S. Garvey , Ricky D. Gaston , L. Gordon Letts , Inigo Saenz de Tejada , Sang William Tam , Manuel Worcel
发明人： David S. Garvey , Ricky D. Gaston , L. Gordon Letts , Inigo Saenz de Tejada , Sang William Tam , Manuel Worcel
IPC分类号： C07C405/00 , A61K31/557
CPC分类号： A61K31/5575
摘要： The invention describes novel nitrosated and/or nitrosylated prostaglandins, and novel compositions comprising at least one nitrosated and/or nitrosylated prostaglandin, and, optionally, 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 vasoactive agent. The invention also provides novel compositions comprising at least one prostaglandin and at least one S-nitrosothiol compound, and, optionally, at least one vasoactive agent. The prostaglandin is preferably a prostaglandin E1 compound, more preferably alprostadil, and the S-nitrosothiol compound is preferably S-nitrosoglutathione. The 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 cerebrovascular disorders, cardiovascular disorders, benign prostatic hyperplasia (BPH), glaucoma, peptic ulcers or for inducing abortions.
摘要翻译：本发明描述了新的亚硝化和/或亚硝基化的前列腺素，以及包含至少一种亚硝化和/或亚硝基化的前列腺素的新组合物，以及任选的至少一种捐赠，转移或释放一氧化氮的化合物，提高内源性内皮水平的放松因子，刺激一氧化氮的内源性合成或是一氧化氮合酶的底物和/或至少一种血管活性剂。本发明还提供了包含至少一种前列腺素和至少一种S-亚硝基硫醇化合物和任选的至少一种血管活性剂的新型组合物。前列腺素优选为前列腺素E 1化合物，更优选前列地尔，S-亚硝基硫醇化合物优选为S-亚硝基谷胱甘肽。本发明还提供用于治疗或预防男性和女性的性功能障碍的方法，用于增强男性和女性的性反应，以及用于治疗或预防脑血管疾病，心血管疾病，良性前列腺增生（BPH），青光眼，消化性溃疡或诱导堕胎

8. 发明授权

US07176238B1 Nitrostated and nitrosylated prostaglandins, compositions and methods of use 失效
标题翻译：硝基化和亚硝酰化前列腺素，组合物和使用方法
公开(公告)号：US07176238B1
公开(公告)日：2007-02-13
申请号：US09516194
申请日：2000-03-01
申请人： David S. Garvey , Ricky D. Gaston , L. Gordon Letts , Inigo Saenz de Tejada , Sang William Tam , Manuel Worcel
发明人： David S. Garvey , Ricky D. Gaston , L. Gordon Letts , Inigo Saenz de Tejada , Sang William Tam , Manuel Worcel
IPC分类号： A61K31/557 , C07C405/00
CPC分类号： A61K31/5575
摘要： The present invention describes novel nitrosated and/or nitrosylated prostaglandins, and novel compositions comprising at least one nitrosated and/or nitrosylated prostaglandin, and, optionally, 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 vasoactive agent. The present invention also provides novel compositions comprising at least one prostaglandin and at least one S-nitrosothiol compound, and, optionally, at least one vasoactive agent. The prostaglandin is preferably a prostaglandin E1 compound, more preferably alprostadil, and the S-nitrosothiol compound is preferably S-nitrosoglutathione. 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 cerebrovascular disorders, cardiovascular disorders, benign prostatic hyperplasia (BPH), glaucoma, peptic ulcers or for inducing abortions. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.
摘要翻译：本发明描述了新的亚硝基化和/或亚硝基化的前列腺素，以及包含至少一种亚硝基化和/或亚硝基化的前列腺素的新组合物，以及任选的至少一种捐赠，转移或释放一氧化氮的化合物，提高内源性的内皮水平舒张因子，刺激一氧化氮的内源性合成或者是一氧化氮合酶的底物和/或至少一种血管活性剂。本发明还提供了包含至少一种前列腺素和至少一种S-亚硝基硫醇化合物和任选的至少一种血管活性剂的新型组合物。前列腺素优选为前列腺素E 1化合物，更优选前列地尔，S-亚硝基硫醇化合物优选为S-亚硝基谷胱甘肽。本发明还提供了治疗或预防男性和女性性功能障碍的方法，用于增强男性和女性的性反应，以及用于治疗或预防脑血管疾病，心血管疾病，良性前列腺增生（BPH），青光眼，消化性溃疡或诱导堕胎。本发明的化合物和/或组合物也可以以药物试剂盒的形式提供。

9. 发明授权

US06825185B2 Substituted aryl compounds as novel cyclooxygenase-2 selective inhibitors, compositions and methods of use 失效
公开(公告)号：US06825185B2
公开(公告)日：2004-11-30
申请号：US10730979
申请日：2003-12-10
申请人： Subhash P. Khanapure , David S. Garvey , Richard A. Earl , Maiko Ezawa , Xinqin Fang , Ricky D. Gaston
发明人： Subhash P. Khanapure , David S. Garvey , Richard A. Earl , Maiko Ezawa , Xinqin Fang , Ricky D. Gaston
IPC分类号： A61K3133
CPC分类号： C07D319/08 , A61K45/06 , C07D317/56 , C07D319/18 , C07D319/20 , C07D405/06
摘要： The invention describes novel substituted aryl compounds that are 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, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhibitors, isoprostane inhibitors, and mixtures thereof. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, 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 toxicity or other toxicities; 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.

10. 发明授权

US08304409B2 Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use 有权
标题翻译：硝化非甾体抗炎化合物，组合物和使用方法
公开(公告)号：US08304409B2
公开(公告)日：2012-11-06
申请号：US12636329
申请日：2009-12-11
申请人： Richard A. Earl , Maiko Ezawa , Xinqin Fang , David S. Garvey , Ricky D. Gaston , Subhash P. Khanapure , L. Gordon Letts , Chia-En Lin , Ramani R. Ranatunge , Stewart K. Richardson , Joseph D. Schroeder , Cheri A. Stevenson , Shiow-Jyi Wey
发明人： Richard A. Earl , Maiko Ezawa , Xinqin Fang , David S. Garvey , Ricky D. Gaston , Subhash P. Khanapure , L. Gordon Letts , Chia-En Lin , Ramani R. Ranatunge , Stewart K. Richardson , Joseph D. Schroeder , Cheri A. Stevenson , Shiow-Jyi Wey
IPC分类号： A61K31/54 , A61K31/44 , A61K31/445 , A61K31/425 , A61K31/42 , A61K31/415 , A61K31/335 , A61K31/24 , A61K31/12
CPC分类号： C07D493/04 , C07C291/02 , C07C311/17 , C07C317/18 , C07C323/12 , C07C327/28 , C07D209/18 , C07D211/22 , C07D211/56
摘要： The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, 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 NSAID, 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 NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.
摘要翻译：本发明描述了新型亚硝化非甾体抗炎药（NSAID）及其药学上可接受的盐，以及包含至少一种亚硝化NSAID的新组合物，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NSAID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，或是一氧化氮的底物合酶和/或至少一种治疗剂。本发明还提供了包含至少一种亚硝化NSAID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炎症，疼痛和发烧的方法; 用于治疗胃肠道疾病; 促进伤口愈合; 用于治疗和/或预防由使用非甾体抗炎化合物引起的胃肠道，肾脏和/或呼吸道毒性物质; 用于治疗炎性疾病状态和/或病症; 并用于治疗和/或预防眼科疾病和/或病症。

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