首页> 外国专利> SYNTHESIS OF PHENYL NITRATE DERIVATIVES OF FREE CARBOXYLIC ACID GROUP CONTAINING NSAIDS AS CYCLOOXYGENZISE INHIBITOR FOR ANTI-FLAMMATORY, ANALGESIC AND SMOOTH MUSCLE RELAXANT ACTIVITY

SYNTHESIS OF PHENYL NITRATE DERIVATIVES OF FREE CARBOXYLIC ACID GROUP CONTAINING NSAIDS AS CYCLOOXYGENZISE INHIBITOR FOR ANTI-FLAMMATORY, ANALGESIC AND SMOOTH MUSCLE RELAXANT ACTIVITY

机译:含NSAIDS的游离羧酸基的硝酸亚硝酸酯衍生物作为环加氧抑制剂的抗炎,镇痛和平滑肌松弛活性

摘要

The present invention describes the synthesis of phenyl nitrate derivatives of free carboxylic acid group containing NSAIDs as cyclooxygenase inhibitor and nitric oxide donors (CINOD) for anti-inflammatory, analgesic and smooth muscle relaxant activity, novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) inhibitor, and, at least one compound that donates, transfers, releases nitric oxide and/or stimulates endogenous synthesis of nitric oxide and/or 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 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.
机译:本发明描述了含有游离羧酸基团的NSAIDs作为环加氧酶抑制剂的硝酸苯基酯衍生物和一氧化氮供体(CINOD)的抗炎,止痛和平滑肌松弛活性,新型环加氧酶2(COX-2)选择性抑制剂和新颖的组合物,其包含至少一种环氧化酶2(COX-2)抑制剂,以及至少一种提供,转移,释放一氧化氮和/或刺激一氧化氮的内源性合成和/或提高内源性内皮源性舒张因子的化合物或者是一氧化氮合酶和/或至少一种治疗剂的底物。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道性能;用于促进伤口愈合;用于治疗和/或预防肾脏和/或呼吸系统毒性;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功能。

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