N-acylamino acid derivatives

Details N-acylamino acid derivatives N-acylamino acid derivatives

1992-04-14

1994-06-07

Springer, David B.

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

544168, 544128, C07D41312

Patent

active

053190823

ABSTRACT:
An N-acylamino acid derivative of the formula: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.4 and R.sup.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.sup.3 and R.sup.5 is hydrogen or lower alkyl; A is --CH(OH)--(CH.sub.2).sub.q R.sup.7 wherein R.sup.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.sup.10 wherein E is --S(O).sub.i -- wherein i is 0, 1 or 2, oxygen, --NR.sup.11 -- wherein R.sup.11 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or ##STR2## wherein each of R.sup.12 and R.sup.13 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R.sup.10 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.sup.10 is hydrogen, i is 0, and a is an integer of from 0 to 5; or --CH.sub.2 --CHR.sup.8 --CO--R.sup.9 wherein R.sup.8 is hydrogen, lower alkyl, cycloalkyl, cycloalkylakyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms, and R.sup.9 is hydroxyl, --OX wherein, X is alkyl aryl, lower alkoxycarbonyloxyalkyl or 1-phthalidyl, or --N(Y.sup.1)(Y.sup.2 ) wherein each of Y.sup.1 and Y.sup.2 is hydrogen, lower alkyl, aryl, aralkyl or cycloalkyl, or Y.sup.1 and Y.sup.2 form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may contain a further hetero from; m is 0, 1 or 2; and n is an integer of from 1 to 5, provided that when R.sup.1 is hydrogen, m is 0; or a salt thereof, which is useful as hypotensive drugs.

REFERENCES:
patent: 3875149 (1975-04-01), Woodridge et al.

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