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ANALGESIC/ANTI-INFLAMMATORY DERIVATIVE FREE OF ANY ULCER FORMATION CAUSING SIDE EFFECTS

机译:不含任何引起副反应的溃疡形成的镇痛/抗炎药衍生物

摘要

The clonixing derivative of formula (I), or 4-nitroxybutyl clonixate, is a novel non-steroidal analogesic-inflammatory product that has an extraordinary good balance between high analogesic/anti-infllmmatory activities and low ulcerogenic adverse effects, mainly as a consequence of a surprinsingly high anti-inflammatory activity (two times that of clonixic acid). Compound (I) is prepared by reaction of 4-chlorobutyl clonixate with silver nitrate in acetonitirle. 4-chlorobutyl clonixate is prepared by reaction of an alakaline clonixate with 1-bromo-4-chlorobutane in acetonitrile. 4-nitroxybutyl clonixate (I) is specially useful as an active principle for the treatment of pain and/or inflammation in mammals.
机译:式(I)的Clonixing衍生物或4-硝基氧丁酸可乐宁是一种新型的非甾体类固醇炎症产品,主要由于以下原因而在高类推/抗炎活性和低致溃疡性不良反应之间取得了非常好的平衡。令人惊讶的高抗炎活性(两倍于可乐尼克酸)。化合物(Ⅰ)是通过使4-氯丁酸丙酮酸与硝酸银在乙腈中反应来制备的。 4-氯丁酸氯膦酸酯是通过使碱性碱的氯膦酸酯与1-溴-4-氯丁烷在乙腈中反应来制备的。 4-氧代己酮可乐宁(I)特别可用作治疗哺乳动物疼痛和/或炎症的有效成分。

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