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    • 1. 发明申请
    • Cyclooxygenase-2 selective inhibitors, compositions and methods of use
    • 环氧合酶-2选择性抑制剂,组合物和使用方法
    • US20070238735A1
    • 2007-10-11
    • US11802161
    • 2007-05-21
    • David GarveySubhash KhanapureRamani RanatungeStewart RichardsonJoseph Schroeder
    • David GarveySubhash KhanapureRamani RanatungeStewart RichardsonJoseph Schroeder
    • A61K31/495A61K31/415C07D213/00C07D241/10
    • C07D213/55C07D213/50C07D231/12C07D231/14
    • The invention provides novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions and kits 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 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.
    • 本发明提供新型环氧合酶2(COX-2)选择性抑制剂和包含至少一种环加氧酶2(COX-2)选择性抑制剂的新型组合物和试剂盒,以及任选地,至少一种捐赠,转移或释放一氧化氮的化合物, 内源性合成一氧化氮,提高内源性内源性松弛因子水平,或是一氧化氮合成酶的底物和/或至少一种治疗剂。 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/或亚硝化。 本发明还提供了治疗炎症,疼痛和发烧的方法; 用于治疗和/或改善COX-2选择性抑制剂的胃肠性质; 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外形。
    • 2. 发明申请
    • Cyclooxygenase-2 selective inhibitors, compositions and methods of use
    • 环氧合酶-2选择性抑制剂,组合物和使用方法
    • US20060194861A1
    • 2006-08-31
    • US11418187
    • 2006-05-05
    • Ipul BandarageRichard EarlMaiko EzawaXinqin FangDavid GarveySubhash KhanapureRamani RanatungeStewart RichardsonJoseph SchroederCheri StevensonShiow-Jyi Wey
    • Ipul BandarageRichard EarlMaiko EzawaXinqin FangDavid GarveySubhash KhanapureRamani RanatungeStewart RichardsonJoseph SchroederCheri StevensonShiow-Jyi Wey
    • C07D231/06A61K31/415
    • C07D231/12C07D261/08C07D401/04
    • 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.
    • 本发明描述了新型环氧合酶2(COX-2)选择性抑制剂和包含至少一种环氧合酶2(COX-2)选择性抑制剂的新型组合物,以及任选地至少一种捐赠,转移或释放一氧化氮的化合物,刺激内源性合成 的一氧化氮,提高内源性内源性释放因子水平,或者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COX-2选择性抑制剂,任选地亚硝基化和/或亚硝基化的新的试剂盒,以及任选的至少一种一氧化氮供体,和/或任选的至少一种治疗剂。 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/或亚硝化。 本发明还提供了治疗炎症,疼痛和发烧的方法; 用于治疗和/或改善COX-2选择性抑制剂的胃肠性质; 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外形。