首页> 外国专利> DERIVATIVES OF 4-QUINOLINYL SHOWING ANTI-HELICOBACTERIAL ACTIVITY, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION CONTAINING THEIR AND METHOD OF ITS PREPARING

DERIVATIVES OF 4-QUINOLINYL SHOWING ANTI-HELICOBACTERIAL ACTIVITY, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION CONTAINING THEIR AND METHOD OF ITS PREPARING

机译:具有4-喹啉基的抗肝菌活性衍生物,其合成方法,包含其的药物组合物及其制备方法

摘要

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to new derivatives of quinoline showing anti-Helicobacter activity of the formula (I) , their pharmaceutically acceptable salts with acids, their stereochemically isomeric forms, their quaternary forms and their N-oxides where A means bivalent radical of the formula: -N=CH-CH=CH- (a); -CH= N-CH= CH- (b); -N=N-CH=CH- (c); -N=CH-N=CH- (d); -N=CH-CH=N- (e); -CH= N-N= CH- (f); -N= N-N= CH- (g); -N= N-CH=N- (h); -CH=CH-CH=CH- (i); R1,R2,R2,R4,R5 and R6 each independently means hydrogen, halogen atom, hydroxy-, C1-4-alkyloxy-, C1-4-alkyl-, trifluoromethyl-, amino-, mono- or di-(C1-4-alkyl)-amino- or nitro-group or their pharmaceutically acceptable salts with acids, stereochemical isomeric forms, their quaternary forms or their N-oxides at condition that if one substituent at phenyl-group is a nitro-group then other substituents at the above indicated phenyl-group are distinct from nitro-group. Invention describes new compositions containing the above indicated compounds, methods of synthesis of the above indicated compounds, methods of preparing the above indicated compositions and methods of treatment of patients suffering with disorders or damages caused by Helicobacter infection. EFFECT: improved method of synthesis and preparing, enhanced effectiveness of patient treatment. 9 cl, 5 tbl, 26 ex
机译:领域:有机化学,药学。物质:本发明涉及显示式(I)的抗幽门螺杆菌活性的喹啉新衍生物。<图像文件=“ 00000002.GIF” he =“ 43” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 45” / >,其与酸的药学上可接受的盐,其立体化学异构体形式,其季铵盐形式及其N-氧化物,其中A表示下式的二价基团:-N = CH-CH = CH-(a); -CH = N-CH = CH-(b); -N = N-CH = CH-(c); -N = CH-N = CH-(d); -N = CH-CH = N-(e); -CH = N-N = CH-(f); -N = N-N = CH-(g); -N = N-CH = N-(h); -CH = CH-CH = CH-(i); R 1 ,R 2 ,R 2 ,R 4 ,R 5 和R 6 各自独立地表示氢,卤素原子,羟基-,C 1-4 -烷氧基-,C 1-4 -烷基-,三氟甲基-,氨基-,单-或二-(C 1-4 -烷基)-氨基或硝基基团或它们与酸,立体化学异构体形式,季铵形式或它们的药学上可接受的盐在以下条件下的N-氧化物:如果苯基上的一个取代基是硝基,则上述苯基上的其他取代基与硝基不同。本发明描述了含有上述化合物的新组合物,上述化合物的合成方法,上述组合物的制备方法以及患有由幽门螺杆菌感染引起的疾病或损害的患者的治疗方法。效果:改进的合成和制备方法,增强了患者治疗的有效性。 9厘升,5汤匙,26厘

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