首页> 外国专利> PHARMACEUTICAL FORMULATIONS CONTAINING 3-(4-CINNAMYL-1-PIPERAZINYL) AMINO DERIVATIVES OF 3-FORMYLRIFAMYCIN SV AND 3-FORMYLRIFAMYCIN S AND A PROCESS OF THEIR PREPARATION

PHARMACEUTICAL FORMULATIONS CONTAINING 3-(4-CINNAMYL-1-PIPERAZINYL) AMINO DERIVATIVES OF 3-FORMYLRIFAMYCIN SV AND 3-FORMYLRIFAMYCIN S AND A PROCESS OF THEIR PREPARATION

机译:包含3-甲酰基利福霉素SV和3-甲酰基利福霉素S的3-(4-亚甲基-1-哌嗪基)氨基衍生物的药物配方及其制备方法

摘要

There is disclosed compounds and pharmaceutical formulations containing 3-(4-cinnamyl-1-piperazinyl)-amino derivatives of 3-formylrifamycin SV and 3-formylrifamycin S accordingtoFormula I and a second formula and a process of their preparation. In FormulaI, R can be H or Na, andR1 is H. The compounds, as active substance, possess high activity againstGram- positive andGram-negative microorganisms, as well as against tuberculous micobacteria(including atypical and rifamycinresistant). The method for the preparation of pharmaceutical formulations isreadily feasible, and doesnot require special equipment for its implementation. The process forpreparing the compounds ischaracterized by high yield and purity, using an environmental clean solvent -ethanol and water in thepreparation and isolation of substances, and the absence of residual organicsolvents in the finalproduct.(see above formula)
机译:公开了含有3-(4-的化合物和药物制剂。肉桂基-1-哌嗪基)3-甲酰基利福霉素SV和3-甲酰基利福霉素S的-氨基衍生物至式I和第二式及其制备方法。在公式中I,R可以是H或Na,并且R1为H。作为活性物质的这些化合物对革兰氏阳性和革兰氏阴性微生物以及结核分枝杆菌(包括非典型药物和利福霉素耐)。制备药物制剂的方法是容易可行,并且确实不需要特殊的设备来执行。的过程制备化合物是使用环境清洁的溶剂,具有高产量和高纯度的特点-乙醇和水物质的制备和分离,以及没有残留的有机物最终溶剂产品。(请参见上面的公式)

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