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A method of preparing an inhibitor of angiotensin converting enzyme-

机译:一种制备血管紧张素转化酶抑制剂的方法

摘要

Inhibitors of angiotensin converting enzyme which are physiologically tolerated salts of compounds of the general formula (I) in which R is hydrogen, formyl, acetyl, propanoyl, butanoyl, phenylacetyl, phenylpropanoyl, benzoyl, cyclopentanecarbonyl, tert- butyloxycarbonyl, cyclopentanecarbonyl-L-lysyl, pyro-L- glutamyl-L-lysyl, L-lysyl, L-arginyl or pyro-L-glutamyl, A is phenylalanyl, glycyl, alanyl, tryptophyl, tyrosyl, isoleucyl, leucyl, histidyl or valyl, where the alpha- amino group of these radicals is bonded in the form of an amide bond to the radical R having a meaning other than hydrogen, and phenylalanyl is racemic if R is benzoyl, R1 is hydrogen or methyl, R2 -COOH, L-proline, L-3,4- dehydroproline, D,L-3,4-dehydroproline, L-3- hydroxyproline, L-4-hydroxyproline, L-thiazolidine-4- carboxylic acid or L-5-oxoproline, where the imino group in these radicals is bonded to the adjacent group, Kat is the cation of a base, and n is zero or 1, where R1 is methyl if n is zero. IMAGE
机译:血管紧张素转化酶的抑制剂,是通式(I)化合物的生理耐受盐,其中R为氢,甲酰基,乙酰基,丙酰基,丁酰基,苯乙酰基,苯丙酰基,苯甲酰基,环戊烷羰基,叔丁氧羰基羰基,环戊烷羰基-L-赖氨酰基,吡咯-L-谷氨酰基-L-赖氨酰,L-赖氨酰基,L-精氨酸或吡咯-L-谷氨酰,A为苯丙氨酰基,甘氨酰基,丙氨酰基,色氨酸,酪氨酰基,异亮氨酰基,亮氨酰基,组氨酸或戊基,其中α-氨基这些基团的基团以酰胺键的形式键合到具有氢以外含义的基团R上,并且如果R是苯甲酰基,R 1是氢或甲基,R 2 -COOH,L-脯氨酸,L-3,则苯丙氨酰基是外消旋的。 ,4-脱氢脯氨酸,D,L-3,4-脱氢脯氨酸,L-3-羟脯氨酸,L-4-羟脯氨酸,L-噻唑烷-4-羧酸或L-5-氧代脯氨酸,其中这些基团中的亚氨基为与相邻基团键合的Kat是碱基的阳离子,n为零或1,如果n为零,则R1为甲基。 <图像>

著录项

  • 公开/公告号ES501730A0

    专利类型

  • 公开/公告日1982-04-01

    原文格式PDF

  • 申请/专利权人 UNIV MIAMI;

    申请/专利号ES19810501730

  • 发明设计人

    申请日1981-04-28

  • 分类号C07C101/40;A61K31/195;

  • 国家 ES

  • 入库时间 2022-08-22 13:21:47

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