首页> 外国专利> GLUTAMIN AND ASPARGIC ACID DERIVATIVES WITH ANTIGASTRIC ACTIVITIES AND PROCEDURES FOR THEIR PRODUCTION.

GLUTAMIN AND ASPARGIC ACID DERIVATIVES WITH ANTIGASTRIC ACTIVITIES AND PROCEDURES FOR THEIR PRODUCTION.

机译:具有反胃活性的谷氨酰胺和天冬氨酸衍生物及其生产方法。

摘要

Glutamic and aspartic acid derivatives having general formula (I), in which n is 1 or 2, R1 is a phenyl group mono- or di-substituted with chloro, methyl or nitro groups such that hydrogen or the nitro group may be present in positions (2 and 6) of the phenyl group and hydrogen, chloro or the methyl group may be present in positions (3 and 5), and in which R2 is a linear or branched alkyl chain or a cyclo-alkyl group containing from 5 to 9 carbon atoms, the stereochemistry at the chiral centre marked with an asterisk in formula (I) being DL or D, and their pharmaceutically acceptable salts, useful for the therapeutic treatment of conditions induced by hypergastrinaemia. The compounds of the invention in fact show powerful antigastrin ("little gastrin" or G-17) and antipentagastrin activities.
机译:具有通式(I)的谷氨酸和天冬氨酸衍生物,其中n是1或2,R 1是被氯,甲基或硝基单取代或二取代的苯基,使得氢或硝基可以存在于(2和6)中的苯基和氢,氯或甲基可以存在于位置(3和5)中,并且其中R 2是直链或支链烷基链或含有5至9的环烷基碳原子,在式(I)中标有星号的手性中心的立体化学是DL或D及其药学上可接受的盐,可用于治疗由高胃泌素血症引起的疾病。实际上,本发明的化合物显示出强大的抗胃泌素(“小胃泌素”或G-17)和抗戊胃泌素活性。

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