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1. 发明申请

WO2004004648A3 NITROSATED NONSTEROIDAL ANTIINFLAMMATORY COMPOUNDS, COMPOSITIONS AND METHODS OF USE 审中-公开
公开(公告)号：WO2004004648A3
公开(公告)日：2004-01-15
申请号：PCT/US2003/021026
申请日：2003-07-03
申请人： NITROMED, INC. , EARL, Richard, A. , EZAWA, Maiko , FANG, Xinqin , GARVEY, David, S. , GASTON, Ricky, D. , KHANAPURE, Subhash, P. , LETTS, Gordon, L. , LIN, Chia-En , RANATUNGE, Ramani, R. , RICHARDSON, Stewart, K. , SCHROEDER, Joseph, D. , STEVENSON, Cheri, A. , WEY, Shiow-Jyi
发明人： EARL, Richard, A. , EZAWA, Maiko , FANG, Xinqin , GARVEY, David, S. , GASTON, Ricky, D. , KHANAPURE, Subhash, P. , LETTS, Gordon, L. , LIN, Chia-En , RANATUNGE, Ramani, R. , RICHARDSON, Stewart, K. , SCHROEDER, Joseph, D. , STEVENSON, Cheri, A. , WEY, Shiow-Jyi
IPC分类号： C07D333/22
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.

2. 发明申请

WO2004098538A2 NITROSATED AND NITROSYLATED COMPOUNDS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：硝基和硝基化合物，组合物和使用方法
公开(公告)号：WO2004098538A2
公开(公告)日：2004-11-18
申请号：PCT/US2004/007943
申请日：2004-03-15
申请人： NITROMED, INC. , EARL, Richard, A. , GARVEY, David, S. , GASTON, Ricky, D. , LIN, Chia-En , RANATUNGE, Ramani, R. , RICHARDSON, Stewart, K. , STEVENSON, Cheri, A.
发明人： EARL, Richard, A. , GARVEY, David, S. , GASTON, Ricky, D. , LIN, Chia-En , RANATUNGE, Ramani, R. , RICHARDSON, Stewart, K. , STEVENSON, Cheri, A.
IPC分类号： A61K
CPC分类号： C07J17/00 , C07J1/00 , C07J31/006 , C07J41/0044 , C07J43/00 , C07J43/003
摘要： The invention describes novel nitrosated and/or nitrosylated compounds of the invention, and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated compound of the invention, and, optionally, at least one nitric oxide donor compound and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one compound of the invention, that is optionally nitrosated and/or nitrosylated, and at least one nitric oxide donor compound and/or at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating cardiovascular diseases, for inhibiting platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating pathological conditions resulting from abnormal cell proliferation; transplantation rejections, autoimmune, inflammatory, proliferative, hyperproliferative or vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis by administering at least one compound of the invention that is optionally nitrosated and/or nitrosylated, 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. The compounds of the invention are preferably estradiol compounds, troglitazone compounds, tranilast compounds, retinoic acid compounds, resveratol compounds, myophenolic acid compounds, acid compounds, anthracenone compounds and trapidil compounds.
摘要翻译：本发明描述了本发明的新型亚硝化和/或亚硝基化化合物及其药学上可接受的盐，以及包含至少一种本发明的亚硝基化和/或亚硝化化合物和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。本发明还提供了包含至少一种本发明的化合物，其任选被亚硝化和/或亚硝基化的新化合物，以及至少一种一氧化氮供体化合物和/或至少一种治疗剂。本发明的化合物和组合物也可以结合到基质上。本发明还提供治疗心血管疾病的方法，用于抑制由血液暴露于医疗器械引起的血小板聚集和血小板粘附，用于治疗由异常细胞增殖引起的病理状况; 移植排斥，自身免疫，炎症，增殖，过度增生或血管疾病; 用于减少瘢痕组织或抑制伤口收缩，特别是预防和/或治疗再狭窄的方法，通过给予至少一种任选地亚硝化和/或亚硝基化的本发明化合物与能释放硝酸的一氧化氮供体组合在生理条件下氧化或间接地将一氧化氮递送或转移到靶位点。本发明的化合物优选是雌二醇化合物，曲格列酮化合物，曲尼司特化合物，视黄酸化合物，白藜芦醇化合物，肌醇酸化合物，酸化合物，蒽酮化合物和捕获剂化合物。

3. 发明申请

WO2004002409A2 CYCLOOXYGENASE-2 SELECTIVE INHIBITORS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译： CYCLOOXGENASE-2选择性抑制剂，组合物和使用方法
公开(公告)号：WO2004002409A2
公开(公告)日：2004-01-08
申请号：PCT/US2003/019850
申请日：2003-06-25
申请人： NITROMED, INC. , BANDARAGE, Upul, K. , EARL, Richard, A. , EZAWA, Maiko , FANG, Xinqin , GARVEY, David, S. , KHANAPURE, Subhash, P. , RANATUNGE, Ramani, R. , RICHARDSON, Stewart, K. , SCHROEDER, Joseph, D. , STEVENSON, Cheri, A. , WEY, Shiow-Jyi
发明人： BANDARAGE, Upul, K. , EARL, Richard, A. , EZAWA, Maiko , FANG, Xinqin , GARVEY, David, S. , KHANAPURE, Subhash, P. , RANATUNGE, Ramani, R. , RICHARDSON, Stewart, K. , SCHROEDER, Joseph, D. , STEVENSON, Cheri, A. , WEY, Shiow-Jyi
IPC分类号： A61K
CPC分类号： C07D231/12 , C07D261/08 , C07D401/04
摘要： The invention describes novel 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 at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, 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 and/or respiratory toxicity; 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.
摘要翻译：本发明描述了新颖的环加氧酶2（COX-2）选择性抑制剂和包含至少一种环氧合酶2（COX-2）选择性抑制剂和任选地至少一种化合物的新型组合物，或释放一氧化氮，刺激一氧化氮的内源性合成，提高内源性内皮细胞衍生的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选择性抑制剂（任选亚硝化和/或亚硝基化）和任选地至少一种一氧化氮供体和/或任选地至少一种治疗剂的新型试剂盒。本发明的新型环加氧酶2选择性抑制剂可以任选地亚硝化和/或亚硝基化。本发明还提供治疗炎症，疼痛和发热的方法; 用于治疗和/或改善COX-2选择性抑制剂的胃肠道特性; 用于促进伤口愈合; 用于治疗和/或预防肾和/或呼吸毒性; 用于治疗和/或预防由环氧合酶-2水平升高引起的其他疾病; 并用于改善COX-2选择性抑制剂的心血管特征。

4. 发明申请

WO2003086282A3 NITRIC OXIDE DONORS, COMPOSITIONS AND METHODS OF USE 审中-公开
公开(公告)号：WO2003086282A3
公开(公告)日：2003-10-23
申请号：PCT/US2003/010562
申请日：2003-04-07
申请人： NITROMED, INC. , FANG, Xinqin , GARVEY, David, S. , GASTON, Ricky, D. , LIN, Chia-En , RANATUNGA, Ramani, R. , RICHARDSON, Stewart, K. , WANG, Tiansheng , WANG, Weiheng , WEY, Shiow-Jyi
发明人： FANG, Xinqin , GARVEY, David, S. , GASTON, Ricky, D. , LIN, Chia-En , RANATUNGA, Ramani, R. , RICHARDSON, Stewart, K. , WANG, Tiansheng , WANG, Weiheng , WEY, Shiow-Jyi
IPC分类号： C07D235/00
摘要： The invention describes novel nitric oxide donors and novel compositions comprising at least one nitric oxide donor. The invention also provides novel compositions comprising at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating cardiovascular diseases, for the inhibition of platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating pathological conditions resulting from abnormal cell proliferation; transplantation rejections, autoimmune, inflammatory, proliferative, hyperproliferative, vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis by administering the nitric oxide donor optionally in combination with at least one therapeutic agent. The invention also provides methods for treating inflammation, pain, fever, gastrointestinal disorders, respiratory disorders and sexual dysfunctions. The nitric oxide donors donate, transfer or release nitric oxide, and/or elevate endogenous levels of endothelium-derived relaxing factor, and/or stimulate endogenous synthesis of nitric oxide and/or are substrates for nitric oxide synthase and are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions. The therapeutic agent can optionally be substituted with at least one NO and/or NO 2 group (i.e., nitrosylated and/or nitrosated). The invention also provides novel compositions and kits comprising at least one nitric oxide donor and/or at least one therapeutic agent.

5. 发明申请

WO2004010945A2 CYCLOOXYGENASE- 2 SELECTIVE INHIBITORS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译： CYCLOOXYGENASE-2选择性抑制剂，组合物和使用方法
公开(公告)号：WO2004010945A2
公开(公告)日：2004-02-05
申请号：PCT/US2003/023605
申请日：2003-07-29
申请人： NITROMED, INC. , GARVEY, David, S. , KHANAPURE, Subhash, P. , RANATUNGE, Ramani, R. , RICHARDSON, Stewart, K. , SCHROEDER, Joseph, D.
发明人： GARVEY, David, S. , KHANAPURE, Subhash, P. , RANATUNGE, Ramani, R. , RICHARDSON, Stewart, K. , SCHROEDER, Joseph, D.
IPC分类号： A61K
CPC分类号： C07D213/55 , C07D213/50 , C07D231/12 , C07D231/14
摘要： The invention describes novel 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 endotheliumderived relaxing factor 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 COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, 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 and/or respiratory toxicity; 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.
摘要翻译：本发明描述了新颖的环加氧酶2（COX-2）选择性抑制剂和包含至少一种环氧合酶2（COX-2）选择性抑制剂和任选地至少一种化合物的新型组合物，或释放一氧化氮，刺激一氧化氮的内源性合成，提高内皮细胞和内皮细胞水平的内皮细胞衍生的舒张因子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选择性抑制剂（任选亚硝化和/或亚硝基化）和任选地至少一种一氧化氮供体和/或任选地至少一种治疗剂的新型试剂盒。本发明的新型环加氧酶2选择性抑制剂可以任选地亚硝化和/或亚硝基化。本发明还提供治疗炎症，疼痛和发热的方法; 用于治疗和/或改善COX-2选择性抑制剂的胃肠道特性; 用于促进伤口愈合; 用于治疗和/或预防肾和/或呼吸毒性; 用于治疗和/或预防由环氧合酶-2水平升高引起的其他疾病; 并用于改善COX-2选择性抑制剂的心血管特征。

6. 发明申请

WO2004002420A3 OXIME AND/OR HYDRAZONE CONTAINING NITROSATED AND/OR NITROSYLATED CYCLOOXIGENASE-2 SELECTIVE INHIBITORS, COMPOSITIONS AND METHODS OF USE 审中-公开
公开(公告)号：WO2004002420A3
公开(公告)日：2004-01-08
申请号：PCT/US2003/020421
申请日：2003-06-30
申请人： NITROMED, INC. , GARVEY, David, S. , RANATUNGE, Ramani, R. , RICHARDSON, Stewart, K.
发明人： GARVEY, David, S. , RANATUNGE, Ramani, R. , RICHARDSON, Stewart, K.
IPC分类号： C07C251/32
摘要： The invention describes novel cyclooxygenase 2(COX-2) selective inhibitors having at least one oxime group or hydrazone group and novel compositions comprising at least one cyclooxigenase 2(COX-2) selective inhibitor having at least one oxime group or hydrazone 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 therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor having at least one oxime group or hydrazone group, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxigenase 2 selective inhibitors of the invention having at least one oxime group or hydrazone group 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 and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxigenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

7. 发明申请

WO2006099416A1 2-METHYL INDOLE CYCLOOXYGENASE-2 SELECTIVE INHIBITORS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译： 2-甲基吲哚环糊精选择性抑制剂，组合物和使用方法
公开(公告)号：WO2006099416A1
公开(公告)日：2006-09-21
申请号：PCT/US2006/009127
申请日：2006-03-13
申请人： NITROMED, INC. , WEY, Shiow-Jyi , GARVEY, David, S. , FANG, Xinqin , RICHARDSON, Stewart, K.
发明人： WEY, Shiow-Jyi , GARVEY, David, S. , FANG, Xinqin , RICHARDSON, Stewart, K.
IPC分类号： C07D209/18
CPC分类号： C07F9/5728 , C07D209/12 , C07D209/16
摘要： The invention describes compositions and kits comprising 2-methyl indole cyclooxygenase 2 (COX-2) selective inhibitors or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The 2-methyl indole cyclooxygenase 2 selective inhibitors can be optionally substituted with at least one nitric oxide enhancing group. The invention also provides methods for (a) treating inflammation, pain and fever; (b) treating gastrointestinal disorders and/or improving the gastrointestinal properties of COX-2 selective inhibitors; (c) facilitating wound healing; (d) treating renal and/or respiratory toxicities; (e) treating disorders resulting from elevated levels of cyclooxygenase-2; (f) improving the cardiovascular profile of COX-2 selective inhibitors; (g) treating diseases resulting from oxidative stress; (h) treating endothelial dysfunctions; (j) treating diseases caused by endothelial dysfunctions; (k) treating inflammatory disease states and/or disorders; (1) treating ophthalmic disorders; and (m) treating peripheral vascular diseases. The nitric oxide enhancing groups are organic nitrates, organic nitrites, nitrosothiols, thionitrites, thionitrates, NONOates, heterocyclic nitric oxide donors and/or nitroxides. The heterocyclic nitric oxide donors are furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines.
摘要翻译：本发明描述了包含2-甲基吲哚环加氧酶2（COX-2）选择性抑制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组合物和试剂盒。 2-甲基吲哚环氧合酶2选择性抑制剂可以任选地被至少一个一氧化氮增强基团取代。本发明还提供了（a）治疗炎症，疼痛和发烧的方法; （b）治疗胃肠道疾病和/或改善COX-2选择性抑制剂的胃肠性质; （c）促进伤口愈合; （d）治疗肾脏和/或呼吸毒性; （e）治疗由环氧合酶-2水平升高引起的疾病; （f）改善COX-2选择性抑制剂的心血管状态; （g）治疗由氧化应激引起的疾病; （h）治疗内皮功能障碍; （j）治疗由内皮功能障碍引起的疾病; （k）治疗炎性疾病状态和/或病症; （1）治疗眼科疾病; 和（m）治疗外周血管疾病。一氧化氮增强基团是有机硝酸盐，有机亚硝酸盐，亚硝基硫醇，硫堇，硫酸盐，非硝酸盐，杂环一氧化氮供体和/或氮氧化物。杂环一氧化氮供体是呋喃糖，苏氨酸，恶三唑-5-酮和/或氧杂三唑-5-亚胺。

8. 发明公开

EP1539679A2 OXIME AND/OR HYDRAZONE CONTAINING NITROSATED AND/OR NITROSYLATED CYCLOOXIGENASE-2 SELECTIVE INHIBITORS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：肟和/或HYDRAZONHALTIGE，NITRO镀锌和/或亚硝基化环氧合酶-2选择性抑制剂，组合物和使用方法
公开(公告)号：EP1539679A2
公开(公告)日：2005-06-15
申请号：EP03742299.5
申请日：2003-06-30
申请人： Nitromed, Inc.
发明人： GARVEY, David, S. , RANATUNGE, Ramani, R. , RICHARDSON, Stewart, K.
IPC分类号： C07C251/32 , C07C251/72
CPC分类号： C07D231/12
摘要： The invention describes novel cyclooxygenase 2(COX-2) selective inhibitors having at least one oxime group or hydrazone group and novel compositions comprising at least one cyclooxigenase 2(COX-2) selective inhibitor having at least one oxime group or hydrazone 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 therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor having at least one oxime group or hydrazone group, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxigenase 2 selective inhibitors of the invention having at least one oxime group or hydrazone group 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 and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxigenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

9. 发明公开

EP0904266A1 NITROSATED AND NITROSYLATED COMPOUNDS AND COMPOSITIONS AND THEIR USE FOR TREATING RESPIRATORY DISORDERS 失效
标题翻译： NITRO和镀锌亚硝基化合物和制剂及其用于呼吸系统疾病的治疗
公开(公告)号：EP0904266A1
公开(公告)日：1999-03-31
申请号：EP97916818.0
申请日：1997-03-19
申请人： Nitromed, Inc.
发明人： GARVEY, David, S. , LETTS, L., Gordon , RENFROE, H., Burt , RICHARDSON, Stewart, K.
IPC分类号： A61K31 , A61K45 , A61P11 , C07C313 , C07D311 , C07D451 , C07D471 , C07J5 , C07J7 , C07J31 , C07J71
CPC分类号： C07D451/06 , C07C313/36 , C07D311/22 , C07D451/10 , C07D471/04 , C07J5/00 , C07J7/00 , C07J31/00 , C07J71/00 , C07J71/0031
摘要： Disclosed are (i) compounds of a steroid, a β-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, β-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 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+) or nitroxyl (NO-), or as the neutral species, nitric oxide (NO) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.

10. 发明公开

EP1542972A2 CYCLOOXYGENASE- 2 SELECTIVE INHIBITORS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：环氧化酶2选择性抑制剂，组合物及其使用方法
公开(公告)号：EP1542972A2
公开(公告)日：2005-06-22
申请号：EP03772004.2
申请日：2003-07-29
申请人： Nitromed, Inc.
发明人： GARVEY, David, S. , KHANAPURE, Subhash, P. , RANATUNGE, Ramani, R. , RICHARDSON, Stewart, K. , SCHROEDER, Joseph, D.
IPC分类号： C07D207/325 , C07D231/06 , C07D237/14 , C07D401/04 , C07D403/04 , C07D405/04 , C07D413/04 , A61K31/40 , A61K31/415 , A61K31/4155 , A61P29/00
CPC分类号： C07D213/55 , C07D213/50 , C07D231/12 , C07D231/14
摘要： The invention describes novel 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 endotheliumderived relaxing factor 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 COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, 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 and/or respiratory toxicity; 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.

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