| 摘要 |
Disclosed herein are novel carboxyalkyldipeptides, their preparation and pharmaceutical compositions containing them. The novel dipeptides are represented by the general formula I (I) where A is selected from: IIa IIb IIc IId IIe with n, p and q being specified values from 0 to 2, B is ¢J!-¢L!-¢M!-; D is IIIa IIIb E is -NH-,-O-, -S-, or -CH2-; G is ? or -SO2-; J is -(CH2)s- or -((CH2)t-W-; where L is chemical bond, specified alkyl, aryl or heterocyclic moieties, M is -(CH2)u- or -((CH2)t-X-(CH2)v)-where n and v are 0-5 and X is -NR9-, -O-, -S-, R1 and R2 are hydrogen, lower alkyl or lower acyl; R3 is hydrogen, lower alkyl, haloloweralkyl, phenylloweralkyl, (cycloalkyl)lower alkyl, aminomethyl, lower alkylaminomethyl, phenylloweralkylaminomethyl, (cycloalkyl)loweralkylaminomethyl, loweralkylthiomethyl, haloloweralkylthiomethyl, 2-, 3- or 4-pyridylloweralkyl, 2-, 4- or 5-thiazolylloweralkyl, 2-, 4- or 5-1H imidazolylloweralkyl, 1-imidazolylloweralkyl, 1morpholinoloweralkyl or hydroxyphenylloweralkyl; R4 is chlorine or CF3; R5 is hydrogen, halogen, lower alkyl, lower acyl, lower alkoxy, haloloweralkyl or phenylloweralkyl; R7 is hydrogen, lower alkyl or aminoloweralkyl; R6 and R8 are hydroxy or specified substituted hydroxy groups. The compounds exhibit angiotensin converting enzyme inhibitory activity and/or diuretic activity P/PASP0357 |
