首页> 外国专利> DERIVATIVES OF IMIDAZOLE, METHODS OF THEIR SYNTHESIS, INTERMEDIATE SUBSTANCES AND PHARMACEUTICAL COMPOSITIONS BASED ON IMIDAZOLE DERIVATIVES

DERIVATIVES OF IMIDAZOLE, METHODS OF THEIR SYNTHESIS, INTERMEDIATE SUBSTANCES AND PHARMACEUTICAL COMPOSITIONS BASED ON IMIDAZOLE DERIVATIVES

机译:咪唑衍生物,其合成方法,中间体和基于咪唑衍生物的药物组合物

摘要

FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention relates to derivatives of imidazole of the general formula (I) where R1 is H, alkoxy-group, 1,3-dioxolane, dioxane, phenyl, benzoyl or phenylethyl where phenyl is substituted possibly with hydroxy-group or C1-C4-alkoxy-group; R2 and R3 are similar or different taken among halogen atom, free carboxy-radical or carboxy-radical esterified with C1-C4-alkyl; formyl, alkyl, phenylthio-group and alkylthio-group that are substituted possibly with one or some radicals taken among halogen atoms, hydroxy-group, C1-C4-alkoxy-group, free or esterified carboxy- -group and phenyl substituted possibly with hydroxy-group or C1-C4-alkoxy-group; Y is phenyl substituted with two radicals forming in common dioxol, one or some halogen atoms. Compounds show antagonistic properties with respect to endothelin receptors. EFFECT: improved method of synthesis, valuable pharmacological properties. 11 cl, 2 tbl, 29 ex
机译:领域:有机化学,化学技术,药学。物质:本发明涉及通式(I)的咪唑的衍生物。<图像文件=“ 00000002.GIF” he =“ 26” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 30” />其中R 1 是H,烷氧基,1,3-二氧戊环,二恶烷,苯基,苯甲酰基或苯乙基,其中苯基可能被羟基或C 1 -C 取代4 -烷氧基; R 2 和R 3 在卤素原子,被C 1 -C <酯化的游离羧基或羧基自由基之间是相似或不同的Sub> 4 -烷基;可能被一个或几个卤素原子,羟基,C 1 -C 4 -烷氧基取代的甲酰基,烷基,苯硫基和烷硫基-基,游离或酯化的羧基和可能被羟基或C 1 -C 4 -烷氧基取代的苯基; Y是被在普通二氧戊环中形成两个或两个卤素原子的基团取代的苯基。化合物对内皮素受体表现出拮抗性质。效果:改进的合成方法,有价值的药理特性。 11厘升,2汤匙,29厘

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