N-acylamino acid derivatives and their use.

摘要

An N-acylamino acid derivative of the formula: <CHEM> wherein each of R<1>, R<2>, R<4> and R<6> is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms; each of R<3> and R<5> is hydrogen or lower alkyl; A is -CH(OH)-(CH2)qR<7> wherein R<7> is hydrogen, lower alkyl, cycloalkyl, cyloalkylalkyl, aryl, aralkyl, a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms or -E-R<1><0> wherein E is -S(O)i- wherein i is 0, 1 or 2, oxygen, -NR<1><1>- wherein R<1><1> is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or <CHEM> wherein each of R<1><2> and R<1><3> is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R<1><0> 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 R<1><0> is hydrogen, i is 0, and q is an integer of from 0 to 5; or -CH2-CHR<8>-CO-R<9> wherein R<8> is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containig from 1 to 4 hetero atoms, and R<9> is hydroxyl, -OX wherein X is alkyl, aryl, lower alkoxycarbonyloxyalkyl or 1-phthalidyl, or -N(Y<1>)(Y<2>) wherein each of Y<1> and Y<2> is hydrogen, lower alkyl, aryl, aralkyl or cycloalkyl, or Y<1> and Y<2> 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 R<1> is hydrogen, m is 0; or a salt thereof, which is useful as hypotensive drugs.