公开(公告)号：US20070060571A1

公开(公告)日：2007-03-15

申请号：US11599519

申请日：2006-11-15

申请人： Ramani Bandarage ,  Upul Bandarage ,  Xinqin Fang ,  David Garvey ,  L. Letts ,  Joseph Schroeder ,  Sang Tam

发明人： Ramani Bandarage ,  Upul Bandarage ,  Xinqin Fang ,  David Garvey ,  L. Letts ,  Joseph Schroeder ,  Sang Tam

IPC分类号： A61K31/55 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

CPC分类号： C07D207/333 ,  C07C317/46 ,  C07C381/00 ,  C07D209/12 ,  C07D209/18 ,  C07D231/12 ,  C07D231/14 ,  C07D233/64 ,  C07D237/14 ,  C07D261/08 ,  C07D263/20 ,  C07D307/58 ,  C07D311/12 ,  C07D413/12 ,  C07D471/04

摘要： The present invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) 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 present invention also provides novel compositions comprising at least one parent COX-2 inhibitor and at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The present invention also provides kits and methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity; and for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2.

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）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）抑制剂的新组合物，和任选的至少一种可以提供， 转移或释放一氧化氮，刺激一氧化氮的内源性合成，提高内皮衍生的松弛因子的内源水平，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母体COX-2抑制剂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。 本发明还提供用于治疗炎症，疼痛和发烧的试剂盒和方法; 用于治疗和/或改善COX-2抑制剂的胃肠性质; 促进伤口愈合; 用于治疗和/或预防肾毒性; 并且用于治疗和/或预防由环氧合酶-2水平升高引起的其它疾病。

公开(公告)号：US20050038029A1

公开(公告)日：2005-02-17

申请号：US10930901

申请日：2004-09-01

申请人： David Garvey ,  L. Letts ,  H. Renfroe ,  Sang Tam

发明人： David Garvey ,  L. Letts ,  H. Renfroe ,  Sang Tam

IPC分类号： C07D417/04 ,  A61K31/00 ,  A61K31/19 ,  A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61K31/54 ,  A61K31/541 ,  A61K38/00 ,  A61K45/00 ,  A61P1/00 ,  A61P1/04 ,  A61P29/00 ,  A61P43/00 ,  C07C203/00 ,  C07C327/28 ,  C07C381/00 ,  C07D209/28 ,  C07D417/12 ,  C07J41/00 ,  C07K5/02 ,  C07D487/02 ,  A61K31/503

CPC分类号： C07D417/12 ,  A61K31/343 ,  A61K31/60 ,  A61K38/00 ,  C07C203/00 ,  C07C327/28 ,  C07C381/00 ,  C07D209/28 ,  C07J41/0055 ,  C07K5/0215 ,  A61K2300/00

摘要： Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.

摘要翻译： 已被一氧化氮基团取代的非甾体抗炎药; 组合物，其包含（i）非甾体抗炎药，其可以任选地被一氧化氮基团取代，和（ii）直接捐赠，转移或释放一氧化氮基团（优选作为带电物质，特别是亚硝基鎓）的化合物; 并且公开了使用该组合物治疗炎症，疼痛，胃肠道损伤和/或发烧的方法。 这些化合物和组合物可以防止非甾体类抗炎药引起的胃肠道，肾脏和其他毒性。

公开(公告)号：US20060276439A1

公开(公告)日：2006-12-07

申请号：US11505905

申请日：2006-08-18

申请人： David Garvey ,  L. Letts ,  H. Renfroe ,  Sang Tam

发明人： David Garvey ,  L. Letts ,  H. Renfroe ,  Sang Tam

IPC分类号： A61K31/60 ,  A61K31/343

CPC分类号： C07D417/12 ,  A61K31/343 ,  A61K31/60 ,  A61K38/00 ,  C07C203/00 ,  C07C327/28 ,  C07C381/00 ,  C07D209/28 ,  C07J41/0055 ,  C07K5/0215 ,  A61K2300/00

摘要： Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.

公开(公告)号：US20070112067A1

公开(公告)日：2007-05-17

申请号：US11641050

申请日：2006-12-19

申请人： David Garvey ,  Ricky Gaston ,  L. Letts ,  Inigo de Tejada ,  Sang Tam ,  Manuel Worcel

发明人： David Garvey ,  Ricky Gaston ,  L. Letts ,  Inigo de Tejada ,  Sang Tam ,  Manuel Worcel

IPC分类号： A61K31/21 ,  C07C203/02

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