专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

21. 发明授权

US07129251B2 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：US07129251B2
公开(公告)日：2006-10-31
申请号：US11180790
申请日：2005-07-14
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： C07D295/14 , A61K31/445 , A61P1/04
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。

22. 发明授权

US06706724B2 Substituted aryl compounds as novel cyclooxygenase-2 selective inhibitors, compositions and methods of use 失效
公开(公告)号：US06706724B2
公开(公告)日：2004-03-16
申请号：US10024046
申请日：2001-12-21
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： A61K31435
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.

23. 发明授权

US06693122B2 Nitrosated and nitrosylated potassium channel activators, compositions and methods of use 失效
标题翻译：亚硝化和亚硝基化钾通道激活剂，组合物和使用方法
公开(公告)号：US06693122B2
公开(公告)日：2004-02-17
申请号：US10154916
申请日：2002-05-28
申请人： David S. Garvey , Inigo Saenz de Tejada
发明人： David S. Garvey , Inigo Saenz de Tejada
IPC分类号： A61K3144
CPC分类号： C07D213/82 , A61K31/4406 , A61K31/455
摘要： The present invention describes novel nitrosated and/or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and/or nitrosylated potassium channel activator, 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 potassium channel activator, 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 vasoactive agent. 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 cardiovascular disorders, cerebrovascular disorders, hypertension, asthma, baldness, urinary incontinence, epilepsy, sleep disorders, gastrointestinal disorders, migraines, irritable bowel syndrome and sensitive skin.
摘要翻译：本发明描述了新的亚硝化和/或亚硝基化的钾通道激活剂，以及包含至少一种亚硝化和/或亚硝基化钾通道活化剂的新组合物，以及任选的至少一种捐赠，转移或释放一氧化氮的化合物，提高内源性水平的内皮衍生的松弛因子，刺激一氧化氮的内源性合成或者是一氧化氮合酶和/或至少一种血管活性剂的底物。本发明还提供了包含至少一种钾通道活化剂和至少一种捐赠，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，或者是用于一氧化氮合酶和/或至少一种血管活性剂。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，以及治疗或预防心血管疾病，脑血管障碍，高血压，哮喘，秃发，尿失禁，癫痫，睡眠障碍胃肠道疾病，偏头痛，肠易激综合征和敏感性皮肤。

24. 发明授权

US06514934B1 Imidazoline &agr;-adrenergic receptor antagonist compounds in combination with nitric oxide donors, compositions and methods of use 失效
标题翻译：咪唑啉α-肾上腺素能受体拮抗剂化合物与一氧化氮供体的组合物和使用方法
公开(公告)号：US06514934B1
公开(公告)日：2003-02-04
申请号：US09280540
申请日：1999-03-30
申请人： David S. Garvey , Joseph D. Schroeder , Inigo Saenz de Tejada
发明人： David S. Garvey , Joseph D. Schroeder , Inigo Saenz de Tejada
IPC分类号： A61K3800
CPC分类号： C07D459/00 , A61K45/06 , C07C381/00 , C07D211/62 , C07D233/24 , C07D239/95 , C07D401/04 , C07D405/12 , Y10S514/929 , Y10S514/968
摘要： The present invention is directed to nitrosated or nitrosylated &agr;-adrenergic receptor antagonists, compositions comprising &agr;-adrenergic receptor antagonists that are optionally substituted with at least one NO or NO2 moiety and compounds that donate, transfer or release nitric oxide or elevate levels of endogenous endothelium-derived relaxing factor, and methods for treating sexual dysfunctions in males and females.
摘要翻译：本发明涉及亚硝基化或亚硝基化的α-肾上腺素能受体拮抗剂，其包含任选被至少一个NO或NO 2部分取代的α-肾上腺素能受体拮抗剂的组合物和捐赠，转移或释放一氧化氮或升高内源性内皮水平的化合物来源的放松因子，以及治疗男性和女性性功能障碍的方法。

25. 发明授权

US06294517B1 Compositions and kits comprising alpha-adrenergic receptor antagonists and nitric oxide donors and methods of use 失效
标题翻译：包含α-肾上腺素能受体拮抗剂和一氧化氮供体的组合物和试剂盒及使用方法
公开(公告)号：US06294517B1
公开(公告)日：2001-09-25
申请号：US09145143
申请日：1998-09-01
申请人： David S. Garvey , Joseph D. Schroeder , Inigo Saenz de Tejada
发明人： David S. Garvey , Joseph D. Schroeder , Inigo Saenz de Tejada
IPC分类号： A01N4354
CPC分类号： C07D459/00 , A61K45/06 , C07C381/00 , C07D211/62 , C07D233/24 , C07D239/95 , C07D401/04 , C07D405/12 , Y10S514/929 , Y10S514/968
摘要： The present invention describes novel compositions and kits comprising alpha-adrenergic receptor antagonists and compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, or stimulate nitric oxide synthesis. In preferred embodiments, the alpha-adrenergic receptor antagonist is an alkaloid selected from the group consisting of rauwolscine, corynanthine, yohimbine, apoyohimbine, beta-yohimbine, yohimbol, pseudoyohimbine and epi-3&agr;-yohimbine, and the compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, or stimulates nitric oxide synthesis is selected from the group consisting of L-arginine, S-nitroso-N-acetylcysteine, S-nitroso-captopril, S-nitroso-homocysteine, S-nitroso-cysteine and S-nitroso-glutathione. In other embodiments, the present invention describes novel compositions comprising yohimbine and L-arginine. In still other embodiments, the invention describes novel compositions comprising yohimbine and L-arginine where the yohimbine is derived from yohimbe bark or Rauwolfia root. The novel compositions of the invention are useful for treating impotence in males and females.
摘要翻译：本发明描述了包含α-肾上腺素能受体拮抗剂和捐赠，转移或释放一氧化氮，提高内源性松弛因子的内源水平或刺激一氧化氮合成的化合物的新型组合物和试剂盒。在优选的实施方案中，α-肾上腺素能受体拮抗剂是选自以下的生物碱：羊尿苷，色氨酸，育亨宾，去氨嘌呤，β-育亨宾，育亨宾，假蛋黄嘌呤和epi-3α-育亨宾，以及捐赠，转移或释放的化合物一氧化氮提高内源性舒张因子的内源水平，或刺激一氧化氮合成选自L-精氨酸，S-亚硝基-N-乙酰半胱氨酸，S-亚硝基卡托普利，S-亚硝基高半胱氨酸，S 亚硝基半胱氨酸和S-亚硝基 - 谷胱甘肽。在其它实施方案中，本发明描述了包含育亨宾和L-精氨酸的新型组合物。在其它实施方案中，本发明描述了包含育亨宾和L-精氨酸的新型组合物，其中育亨宾衍生自yohimbe树皮或Rauwolfia根。本发明的新型组合物可用于治疗男性和女性的阳。。

26. 发明授权

US06172068B2 Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses 失效
公开(公告)号：US06172068B2
公开(公告)日：2001-01-09
申请号：US09247322
申请日：1999-02-10
申请人： David S. Garvey , Inigo Saenz de Tejada
发明人： David S. Garvey , Inigo Saenz de Tejada
IPC分类号： C07D40104
CPC分类号： C07D487/04 , C07D405/14
摘要： Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i. e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.

27. 发明授权

US06172060B2 Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses 失效
公开(公告)号：US06172060B2
公开(公告)日：2001-01-09
申请号：US09247296
申请日：1999-02-10
申请人： David S. Garvey , Inigo Saenz de Tejada
发明人： David S. Garvey , Inigo Saenz de Tejada
IPC分类号： C07D20712
CPC分类号： C07D487/04 , C07D405/14
摘要： Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.

28. 发明授权

US5824669A Nitrosated and nitrosylated compounds and compositions and their use for treating respiratory disorders 失效
标题翻译：亚硝化和亚硝化化合物及其组合物及其用于治疗呼吸系统疾病的用途
公开(公告)号：US5824669A
公开(公告)日：1998-10-20
申请号：US620882
申请日：1996-03-22
申请人： David S. Garvey , L. Gordon Letts , H. Burt Renfroe , Stewart K. Richardson
发明人： David S. Garvey , L. Gordon Letts , H. Burt Renfroe , Stewart K. Richardson
IPC分类号： A61K31/00 , A61K31/56 , A61K31/58 , A61K45/00 , A61P11/00 , C07C313/36 , C07D311/22 , C07D451/06 , C07D451/10 , C07D471/04 , C07J5/00 , C07J7/00 , C07J31/00 , C07J71/00
CPC分类号： C07D451/06 , C07C313/36 , C07D311/22 , C07D451/10 , C07D471/04 , C07J31/00 , C07J5/00 , C07J7/00 , C07J71/00 , C07J71/0031
摘要： Disclosed are (i) compounds of a steroid, a .beta.-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO.sub.2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, .beta.-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO.sub.2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO.sup.+) or nitroxyl (NO.sup.-), or as the neutral species, nitric oxide (NO.circle-solid.) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.
摘要翻译：公开的是（i）直接或间接连接到NO或NO 2基团或刺激NO或EDRF的内源性产生的组的类固醇，β-拮抗剂，抗胆碱能药，肥大细胞稳定剂和磷酸二酯酶（PDE）抑制剂的化合物体内; （ii）类固醇，β-激动剂，抗胆碱能药物，肥大细胞稳定剂和PDE抑制剂的组合物，其可任选地被至少一个NO或NO 2部分或刺激体内NO或EDRF内源性产生的基团取代;以及化合物捐赠，转移或释放一氧化氮作为带电物种，即亚硝酸盐（NO +）或硝酰基（NO-），或作为中性物质，一氧化氮（NO + 574）或刺激体内NO或EDRF的内源性产生 ; 和（iii）用于预防和/或治疗呼吸系统疾病。

29. 发明授权

US5409946A Isoxazole, isothiazole and pyrazole compounds that enhance cognitive function 失效
标题翻译：异恶唑，异噻唑和吡唑化合物，增强认知功能
公开(公告)号：US5409946A
公开(公告)日：1995-04-25
申请号：US118079
申请日：1993-09-08
申请人： David S. Garvey , George M. Carrera, Jr. , Stephen P. Arneric , Youe-Kong Shue , Nan-Horng Lin , Yun He , Edmund L. Lee , Suzanne A. Lebold
发明人： David S. Garvey , George M. Carrera, Jr. , Stephen P. Arneric , Youe-Kong Shue , Nan-Horng Lin , Yun He , Edmund L. Lee , Suzanne A. Lebold
IPC分类号： A61K31/40 , A61K31/415 , A61K31/42 , A61K31/422 , A61K31/425 , A61K31/427 , A61K31/44 , A61P25/00 , A61P25/22 , A61P25/28 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D211/80
CPC分类号： C07D417/04 , C07D413/04
摘要： Novel isoxazole isothiazole and pyrazole compounds of the formula: ##STR1## wherein A, R.sup.1, and R.sup.2 are specifically defined, or pharmaceutical salts thereof, are selective and potent cholinergic ligands at neuronal nicotinic receptors, useful in the treatment of cognitive, neurological and mental disorders characterized by decreased cholinergic function, as well as in the treatment of alcohol intoxication and petit real absence epilepsy.
摘要翻译：新颖的异恶唑异噻唑和吡唑化合物具有下式：其中A，R1和R2具体定义，或其药学上可接受的神经元烟碱受体中选择性和有效的胆碱能配体，可用于治疗认知，神经和精神以胆碱能功能下降为特征的疾病，以及治疗酒精中毒和小型实际不存在癫痫。

30. 发明申请

US20110003784A1 Opsin-binding ligands, compositions and methods of use 有权
标题翻译：组氨酸 - 结合配体，组合物和使用方法
公开(公告)号：US20110003784A1
公开(公告)日：2011-01-06
申请号：US12802898
申请日：2010-06-16
申请人： David S. Garvey , Gregory J. LaRosa , Jeremy R. Greenwood , Mark L. Brewer , Tan Quach , Jamie B. Côté , Judd Berman
发明人： David S. Garvey , Gregory J. LaRosa , Jeremy R. Greenwood , Mark L. Brewer , Tan Quach , Jamie B. Côté , Judd Berman
IPC分类号： A61K31/397 , C07C61/22 , C07C233/58 , C07D295/104 , C07D243/24 , C07D241/04 , C07D207/36 , C12N5/071 , A61K31/19 , A61K31/16 , A61K31/4453 , A61K31/5375 , A61K31/5513 , A61K31/495 , A61K31/40 , A61P27/02 , C07K14/00
CPC分类号： C07D295/215 , C07B59/002 , C07B2200/05 , C07C233/10 , C07C275/14 , C07C2601/16 , C07D205/04 , C07D207/12 , C07D207/14 , C07D211/38 , C07D241/04 , C07D241/08 , C07D243/08 , C07D295/182 , C07D295/185 , C07D295/194 , C07D295/205 , C07D295/26 , C07D491/10 , C07D493/08
摘要： Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.
摘要翻译：公开了所述化合物的化合物和组合物以及化合物的使用方法，用于治疗与视蛋白蛋白质错位定位相关的眼科疾病，突变视蛋白蛋白质的错误折叠和积聚在眼睛中的毒性视觉循环产物的产生。还描述了用于这些方法的化合物和组合物，单独或与其它治疗剂组合。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式