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NOVEL BENZOYL AMINO ACID DERIVS., PHARMACEUTICAL COMPNS. CONTH. THEM AND PROCESS TO PREPARE THEM

机译:新型苯甲酰氨基酸衍生物,药物成分。康思。他们和准备他们的过程

摘要

The peroxidation of lipids inhibiting N-benzoylamino acid derivatives of the general formula (I), CHEM wherein R1 and R2 , which are the same or different, stand for a hydroxyl group optionally bearing an acetyl group; or a C1-6alkoxy group optionally substituted by a phenyl group; R3 represents: hydroxyl group; C1-10alkoxy group; or a C1-4alkoxy group optionally substituted by a phenoxy group optionally bearing a nitrogen-containing substituent; or an -NR4R5 group, where R4 and R5, which are the same or different, mean: hydrogen; hydroxyl group; C1-12alkyl group; C1-4alkyl group optionally substituted by a hydroxyl group or an amino group; R4 and R5 together with the adjacent nitrogen form an optionally substituted 5- or 6-membered heterocyclic group optionally containing an additional nitrogen atom, this heterocyclic group optionally being substituted by an oxo group or an optionally phenyl-substituted C1-4alkyl group or C3-5alkenyl group; and when being piperazine, this heterocyclic group may be substituted also by a diaminopyrimidinyl or di(pyrrolidino)-pyrimidinyl group; and n means an integer from 2 to 15 with the proviso that: when R3 means hydroxyl group and n is 5, as well as one of R1 and R2 means a 4-hydroxyl group, then the other one of R1 and R2 is different from a 3-hydroxyl or 3-methoxy group; and when n is 2 or 3, then R1 and R2 cannot simultaneously stand for 2- and 3-methoxy group, as well as their tautomers, racemates and optically active individual (pure) isomers or mixtures thereof and the salts of these compounds and pharmaceutical compositions containing these compounds.
机译:抑制通式(I)的通式(I)的N-苯甲酰基氨基酸衍生物的脂质的过氧化反应,其中R 1和R 2相同或不同,代表任选带有乙酰基的羟基。或任选被苯基取代的C 1-6烷氧基;或R 3表示:羟基; C1-10烷氧基;或C 1-4烷氧基任选地被任选带有含氮取代基的苯氧基取代;或或-NR 4 R 5基团,其中R 4和R 5相同或不同,表示:氢;羟基C1-12烷基;任选地被羟基或氨基取代的C 1-4烷基; R 4和R 5与相邻的氮一起形成任选取代的5或6元杂环基,任选地含有另外的氮原子,该杂环基任选被氧代基或任选地苯基取代的C 1取代-4烷基或C 3-5烯基;当为哌嗪时,该杂环基也可以被二氨基嘧啶基或二(吡咯烷基)-嘧啶基取代; n是2〜15的整数,条件是:当R 3表示羟基且n为5时,R 1和R 2之一表示4-羟基时,则R 1和R 2的另一个不同于3-羟基或3-甲氧基。当n为2或3时,R 1和R 2不能同时代表2-和3-甲氧基,以及它们的互变异构体,外消旋体和旋光性的单个(纯)异构体或其混合物,以及这些化合物的盐和含有这些化合物的药物组合物。

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