公开(公告)号：US20050250758A1

公开(公告)日：2005-11-10

申请号：US11180790

申请日：2005-07-14

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： 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

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。

公开(公告)号：US20070238740A1

公开(公告)日：2007-10-11

申请号：US10568819

申请日：2004-08-20

申请人： David Garvey ,  L. Letts ,  Manuel Worcel

发明人： David Garvey ,  L. Letts ,  Manuel Worcel

IPC分类号： A61K31/41 ,  A61K31/4164 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K31/519 ,  C07D233/42 ,  C07D233/54 ,  C07D239/22 ,  C07D257/04 ,  C07D401/10 ,  C07D403/10 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07D403/10 ,  C07C205/40 ,  C07D233/68 ,  C07D235/18 ,  C07D257/04 ,  C07D307/52 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04

摘要： The invention describes novel nitrosated and/or nitrosylated cardiovascular compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated cardiovascular compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one cardiovascular compound of the invention, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor 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; and (k) treating nephropathy. The nitrosated and/or nitrosylated cardiovascular compounds are preferably nitrosated and/or nitrosylated aldosterone antagonists, nitrosated and/or nitrosylated angiotensin II antagonists, nitrosated and/or nitrosylated calcium channel blockers, nitrosated and/or nitrosylated endothelin antagonists, nitrosated and/or nitrosylated hydralazine compounds, nitrosated and/or nitrosylated neutral endopeptidase inhibitors and nitrosated and/or nitrosylated renin inhibitors.

摘要翻译： 本发明描述了新的亚硝化和/或亚硝基化的心血管化合物或其药学上可接受的盐，以及包含至少一种亚硝化和/或亚硝基化的心血管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组合物 。 本发明还提供了包含至少一种本发明的心血管化合物，其任选被亚硝化和/或亚硝基化的新组合物和试剂盒，以及任选的至少一种一氧化氮供体化合物和/或至少一种治疗剂。 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; 和（k）治疗肾病。 亚硝化和/或亚硝基化的心血管化合物优选为亚硝化和/或亚硝基化的醛固酮拮抗剂，亚硝化和/或亚硝酰化的血管紧张素II拮抗剂，亚硝化和/或亚硝酰化的钙通道阻断剂，亚硝化和/或亚硝基化的内皮素拮抗剂，亚硝化和/ 化合物，亚硝化和/或亚硝基化的中性内肽酶抑制剂和亚硝化和/或亚硝基化的肾素抑制剂。

公开(公告)号：US20070010571A1

公开(公告)日：2007-01-11

申请号：US10569077

申请日：2004-08-20

申请人： David Garvey ,  L. Letts ,  Manuel Worcel ,  Ricky Gaston

发明人： David Garvey ,  L. Letts ,  Manuel Worcel ,  Ricky Gaston

IPC分类号： A61K31/405 ,  A61K31/138 ,  C07D209/20

CPC分类号： C07D493/04 ,  C07D407/04 ,  C07K5/06026

摘要： The invention describes novel nitrosated and/or nitrosylated cardiovascular compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated cardiovascular compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at,least one cardiovascular compound of the invention, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor 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; and (k) treating nephropathy. The nitrosated and/or nitrosylated cardiovascular compounds are preferably nitrosated and/or nitrosylated P-adrenergic antagonists, nitrosated and/or nitrosylated angiotensinconverting enzyme (ACE) inhibitors, nitrosated and/or nitrosylated anti-hyperlipidemic compounds, and nitrosated and/or nitrosylated antithrombotic and vasodilator compounds.

摘要翻译： 本发明描述了新的亚硝化和/或亚硝基化的心血管化合物或其药学上可接受的盐，以及包含至少一种亚硝化和/或亚硝基化的心血管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组合物 。 本发明还提供了包含至少一种本发明的心血管化合物，其任选被亚硝化和/或亚硝基化的新组合物和试剂盒，以及任选的至少一种一氧化氮供体化合物和/或至少一种治疗剂。 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; 和（k）治疗肾病。 亚硝化和/或亚硝基化的心血管化合物优选为亚硝化和/或亚硝化的P-肾上腺素能拮抗剂，亚硝化和/或亚硝化的血管紧张素转换酶（ACE）抑制剂，亚硝化和/或亚硝化的抗高脂血症化合物，以及亚硝化和/或亚硝化的抗血栓形成和/ 血管扩张剂化合物。