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1. 发明授权

US5667764A Compounds, compositions and methods for binding bio-affecting substances to surface membranes of bio-particles 失效
标题翻译：将生物影响物质与生物颗粒的表面膜结合的化合物，组合物和方法
公开(公告)号：US5667764A
公开(公告)日：1997-09-16
申请号：US884432
申请日：1992-05-15
申请人： Gregory A. Kopia , Paul K. Horan , Brian D. Gray , David E. Troutner , Katharine A. Muirhead , Kamleshkumar A. Sheth , Chia-En Lin , Zhizhou Yu , Bruce D. Jensen , Sue Ellen Slezak
发明人： Gregory A. Kopia , Paul K. Horan , Brian D. Gray , David E. Troutner , Katharine A. Muirhead , Kamleshkumar A. Sheth , Chia-En Lin , Zhizhou Yu , Bruce D. Jensen , Sue Ellen Slezak
IPC分类号： C07D277/64 , A61K35/12 , A61K41/00 , A61K45/00 , A61K47/48 , A61K49/00 , A61K49/06 , A61K49/18 , A61K51/00 , A61K51/04 , A61K51/08 , A61K51/12 , A61P31/00 , A61P35/00 , C07C211/09 , C07C211/13 , C07C229/16 , C07C237/04 , C07C251/38 , C07C323/25 , C07D209/04 , C07D209/08 , C07D219/04 , C07D219/08 , C07D219/14 , C07D263/62 , C07D517/04 , C07K14/00 , C07K14/575 , C07K16/00 , C08B37/00 , C09K3/00 , C07D209/02 , C07D513/04
CPC分类号： C07D209/08 , A61K41/0085 , A61K47/48215 , A61K47/48776 , A61K49/0002 , A61K49/0026 , A61K49/0032 , A61K49/0052 , A61K49/06 , A61K49/18 , A61K49/1896 , A61K51/0497 , A61K51/1258 , C07C229/16 , C07D219/08 , C07D263/62 , C08B37/0075 , A61K2121/00 , A61K2123/00
摘要： Compounds are provided having the capability of binding therapeutically active substances to lipid containing bio-compatible particles, such as cells or viruses. These compounds include a bio-affecting moiety, comprising a therapeutically active substance, which is linked via a linking moiety to at least one hydrocarbon substituent selected so that the compounds is sufficiently non-polar to impart lipid binding capability to the compound. Thus, compounds of the invention are useful for site-selective delivery of therapeutic agents, and retention thereof at the selected site.Methods are provided for using various compounds of the invention in treatment of diseases or other pathological conditions. For example, methods are provided for treatment of: (1) post-angioplasty restenosis; (2) rheumatoid arthritis; (3) tumor cell proliferation, particularly tumor cells associated with ovarian cancer; and (4) psoriasis.
摘要翻译：提供具有将治疗活性物质结合到含脂质的生物相容性颗粒例如细胞或病毒的能力的化合物。这些化合物包括生物影响部分，其包含治疗活性物质，其通过连接部分与选择的至少一个烃取代基连接，使得化合物足够非极性以赋予化合物脂质结合能力。因此，本发明的化合物可用于治疗剂的选择性递送及其在选定部位的保留。提供了使用本发明的各种化合物治疗疾病或其他病理状况的方法。例如，提供了治疗以下方法：（1）后血管成形术再狭窄; （2）类风湿关节炎; （3）肿瘤细胞增殖，特别是与卵巢癌相关的肿瘤细胞; 和（4）牛皮癣。

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

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。

5. 发明授权

US07238814B2 Compositions of S-nitrosothiols and methods of use 失效
标题翻译： S-亚硝基硫醇的组成和使用方法
公开(公告)号：US07238814B2
公开(公告)日：2007-07-03
申请号：US10781705
申请日：2004-02-20
申请人： Przemyslaw A. Marek , Andzrej M. Trocha , Chia-En Lin , Ramani R. Ranatunge , Stewart K. Richardson
发明人： Przemyslaw A. Marek , Andzrej M. Trocha , Chia-En Lin , Ramani R. Ranatunge , Stewart K. Richardson
IPC分类号： C07D209/56 , C07D263/00 , A61K31/395 , A61K31/421
CPC分类号： A61B5/4368 , A61B5/015 , A61K49/0004 , Y10S514/929
摘要： The invention describes compositions and kits comprising 4-aza-4-(2-methyl-2-sulfanylpropyl) tricyclo(5.2.1.0 )dec-8-ene-3,5-dione; 4-aza-4-(2-methyl-2-(nitrosothio)propyl) tricyclo(5.2.1.0 )dec-8-ene-3,5-dione; 4-{1-methyl-1-((2,4,6-trimethoxyphenyl)methylthio)ethyl}-1,3-oxazolidin-2-one; 2-aAmino-3-methyl-3-((2,4,6-trimethoxyphenyl)methylthio)butan-1-ol; 4-(1-methyl-1-(nitrosothio)ethyl)-1,3-oxazolidin-2-one; or pharmaceutically acceptable salts thereof. The compositions of the invention can further comprise at least one penetration enhancer, 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.
摘要翻译：本发明描述了包含4-氮杂-4-（2-甲基-2-硫烷基丙基）三环（5.2.1.0 2,6）癸-8-烯-3,5-二酮的组合物和试剂盒; 4-氮杂-4-（2-甲基-2-（亚硝基硫基）丙基）三环（5.2.1.0 2,6）癸-8-烯-3,5-二酮; 4- {1-甲基-1 - （（2,4,6-三甲氧基苯基）甲硫基）乙基} -1,3-恶唑烷-2-酮; 2-（2-氨基-3-甲基-3 - （（2,4,6-三甲氧基苯基）甲硫基）丁-1-醇; 4-（1-甲基-1-（亚硝基硫代）乙基）-1,3-恶唑烷-2-酮; 或其药学上可接受的盐。本发明的组合物可进一步包含至少一种渗透增强剂，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成酶和/或至少一种血管活性剂。

6. 发明授权

US07256205B2 Nitrosated and nitrosylated H2 receptor antagonist compounds, compositions and methods of use 失效
标题翻译：亚硝化和亚硝基化H 2受体拮抗剂化合物，组合物和使用方法
公开(公告)号：US07256205B2
公开(公告)日：2007-08-14
申请号：US11518231
申请日：2006-09-11
申请人： David S. Garvey , L. Gordon Letts , Chia-En Lin , Tiansheng Wang
发明人： David S. Garvey , L. Gordon Letts , Chia-En Lin , Tiansheng Wang
IPC分类号： C07D277/42 , A61K31/426
CPC分类号： C07D233/54 , C07D233/64 , C07D277/48 , C07D295/092 , C07D295/096
摘要： The invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 group, 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 nonsteroidal antiinflammatory drug, antacid, bismuth-containing reagent or anti-viral agent. The invention also describes methods for treating and/or preventing gastrointestinal disorders; improving gastroprotective properties of H2 receptor antagonists; decreasing the recurrence of ulcers; facilitating ulcer healing; preventing and/or treating inflammations and microbial infections, ophthalmic diseases and disorders, multiple sclerosis, and viral infections; and decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds.
摘要翻译：本发明描述了新的亚硝化和/或亚硝基化的H 2 O 2受体拮抗剂化合物，以及包含至少一种H 2受体拮抗剂化合物的新组合物，其任选被至少一个NO 和/或NO 2个基团，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，提高内源性内皮水平的内源性松弛因子，或者是一氧化氮合酶的底物和/或至少一种非甾体抗炎药，抗酸剂，含铋试剂或抗病毒剂。本发明还描述了治疗和/或预防胃肠道疾病的方法; 改善H 2受体拮抗剂的胃保护性质; 减少溃疡复发; 促进溃疡愈合; 预防和/或治疗炎症和微生物感染，眼科疾病和病症，多发性硬化和病毒感染; 并减少或减少与使用非甾体抗炎化合物相关的胃肠道毒性。

7. 发明申请

US20070004788A1 Nitrosated and nitrosylated H2 receptor antagonist compounds, compositions and methods of use 失效
公开(公告)号：US20070004788A1
公开(公告)日：2007-01-04
申请号：US11518231
申请日：2006-09-11
申请人： David Garvey , L. Letts , Chia-En Lin , Tiansheng Wang
发明人： David Garvey , L. Letts , Chia-En Lin , Tiansheng Wang
IPC分类号： A61K31/426
CPC分类号： C07D233/54 , C07D233/64 , C07D277/48 , C07D295/092 , C07D295/096
摘要： The invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 group, 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 nonsteroidal antiinflammatory drug, antacid, bismuth-containing reagent or anti-viral agent. The invention also describes methods for treating and/or preventing gastrointestinal disorders; improving gastroprotective properties of H2 receptor antagonists; decreasing the recurrence of ulcers; facilitating ulcer healing; preventing and/or treating inflammations and microbial infections, ophthalmic diseases and disorders, multiple sclerosis, and viral infections; and decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds.

8. 发明授权

US06936627B2 Nitrosated and nitrosylated H2 receptor antagonist compounds, compositions and methods of use 失效
公开(公告)号：US06936627B2
公开(公告)日：2005-08-30
申请号：US10282071
申请日：2002-10-29
申请人： David S. Garvey , L. Gordon Letts , Chia-En Lin , Tiansheng Wang
发明人： David S. Garvey , L. Gordon Letts , Chia-En Lin , Tiansheng Wang
IPC分类号： C07D295/08 , A61K31/198 , A61K31/222 , A61K31/29 , A61K31/341 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/4164 , A61K31/426 , A61K31/445 , A61K31/4453 , A61K31/55 , A61K45/06 , A61P1/04 , A61P17/00 , A61P27/02 , A61P27/06 , A61P27/16 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/18 , C07D233/54 , C07D233/64 , C07D277/28 , C07D277/48 , C07D277/52 , C07D295/096 , C07D307/52 , C07D233/56
CPC分类号： C07D233/54 , C07D233/64 , C07D277/48 , C07D295/092 , C07D295/096
摘要： The invention describes novel nitrosated and/or nitrosylated H2 receptor antagonist compounds, and novel compositions comprising at least one H2 receptor antagonist compound that is optionally substituted with at least one NO and/or NO2 group, 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 nonsteroidal antiinflammatory drug, antacid, bismuth-containing reagent or anti-viral agent. The invention also describes methods for treating and/or preventing gastrointestinal disorders; improving gastroprotective properties of H2 receptor antagonists; decreasing the recurrence of ulcers; facilitating ulcer healing; preventing and/or treating inflammations and microbial infections, ophthalmic diseases and disorders, multiple sclerosis, and viral infections; and decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds.

9. 发明授权

US06656966B2 Nitrosated and nitrosylated taxanes, compositions and methods of use 失效
公开(公告)号：US06656966B2
公开(公告)日：2003-12-02
申请号：US09886494
申请日：2001-06-22
申请人： David S. Garvey , L. Gordon Letts , Chia-En Lin , Stewart K. Richardson , Tiansheng Wang
发明人： David S. Garvey , L. Gordon Letts , Chia-En Lin , Stewart K. Richardson , Tiansheng Wang
IPC分类号： A61K31337
CPC分类号： C07D409/12 , A61K31/335 , A61K45/06 , A61K47/54 , A61K47/55 , A61K47/555 , B82Y5/00 , C07D305/14 , Y10S977/775 , Y10S977/907 , Y10S977/915 , Y10S977/926 , A61K2300/00
摘要： The present invention describes novel nitrosated and/or nitrosylated taxanes, and novel compositions comprising at least one nitrosated and/or nitrosylated taxane, 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 therapeutic agent. The present invention also provides novel compositions comprising at least one taxane 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 compounds and compositions of the present invention can also be bound to a matrix. The present invention also provides methods for treating or preventing cardiovascular diseases and disorders, autoimmune diseases, pathological conditions resulting from abnormal cell proliferation, polycystic kidney disease, inflammatory disease, preserving organs and/or tissues or to inhibit wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis, by administering nitrosated and/or nitrosylated taxane or parent taxanes in combination with nitric oxide donors that are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions.

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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