申请人:BANYU PHARMACEUTICAL CO., LTD.
公开号:EP0309766A2
公开(公告)日:1989-04-05
An N-acylamino acid derivative of the formula:
wherein each of R¹, R², R⁴ and R⁶ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms; each of R³ and R⁵ is hydrogen or lower alkyl; A is -CH(OH)-(CH₂)qR⁷ wherein R⁷ is hydrogen, lower alkyl, cycloalkyl, cyloalkylalkyl, aryl, aralkyl, a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms or -E-R¹⁰ wherein E is -S(O)i- wherein i is 0, 1 or 2, oxygen, -NR¹¹- wherein R¹¹ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or
wherein each of R¹² and R¹³ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R¹⁰ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms provided that when R¹⁰ is hydrogen, i is 0, and q is an integer of from 0 to 5; or -CH₂-CHR⁸-CO-R⁹ wherein R⁸ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containig from 1 to 4 hetero atoms, and R⁹ is hydroxyl, -OX wherein X is alkyl, aryl, lower alkoxycarbonyloxyalkyl or 1-phthalidyl, or -N(Y¹)(Y²) wherein each of Y¹ and Y² is hydrogen, lower alkyl, aryl, aralkyl or cycloalkyl, or Y¹ and Y² form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may contain a further hetero atom; m is 0, 1 or 2; and n is an integer of from 1 to 5, provided that when R¹ is hydrogen, m is 0; or a salt thereof, which is useful as hypotensive drugs.
一种 N-酰基氨基酸衍生物,其式如下
其中 R¹、R²、R⁴ 和 R⁶ 各为氢、低级烷基、环烷基、环烷基烷基、芳基、芳烷基或含有 1 至 4 个杂原子的单环或双环杂环基团;R³ 和 R⁵ 各为氢或低级烷基;A 是 -CH(OH)-(CH₂)qR⁷,其中 R⁷ 是氢、低级烷基、环烷基、环烷基烷基、芳基、芳烷基、含有 1 至 4 个杂原子的单环或双环杂环基团或 -E-R¹⁰ ,其中 E 是 -S(O)i- 其中 i 是 0、1或2、氧、-NR¹¹- 其中R¹¹是氢、低级烷基、环烷基、环烷基烷基、芳基或芳烷基,或
其中 R¹² 和 R¹³ 均为氢、低级烷基、环烷基、环烷基烷基、芳基或芳烷基,且 R¹⁰ 为氢、低级烷基、环烷基、环烷基烷基、芳基、芳烷基或含有 1 至 4 个杂质原子的单环或双环杂环基团,但当 R¹⁰ 为氢时,i 为 0,q 为 0 至 5 的整数;或-CH₂-CHR⁸-CO-R⁹,其中 R⁸ 是氢、低级烷基、环烷基、环烷基烷基、芳基、芳烷基或含有 1 至 4 个杂原子的单环或双环杂环基团,且 R𠞙 是羟基、-OX,其中 X 是烷基、芳基、或-N(Y¹)(Y²),其中 Y¹ 和 Y² 分别为氢、低级烷基、芳基、芳烷基或环烷基,或 Y¹ 和 Y² 与邻近的氮原子一起形成 5 或 6 元杂环基团,该杂环基团可能含有另一个杂原子;m为0、1或2;n为1至5的整数,但当R¹为氢时,m为0;或其盐,可用作降血压药物。