N-substituted butyramide derivatives

Details N-substituted butyramide derivatives N-substituted butyramide derivatives

1990-04-11

1992-03-17

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

514533, 514562, 514563, 558414, 560 9, 560 16, 560 38, 560 39, 560 41, 562426, 562444, 562449, 562450, A61K 3195, A61K 31165, A61K 3119, C07C25550

Patent

active

050969250

ABSTRACT:
Disclosed are compounds of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, 2-imidazoly or 4,5-dihydro-2-imidazolyl or any said grouping substituted by lower alkyl; R and R.sub.o independently represent hydrogen, lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl in which aryl represents phenyl, pyridyl, thienyl, furyl, biphenyl or naphthyl, each unsubstituted or mono- or di-substituted by halogen, lower alkyl, hydroxy, acyloxy, lower alkoxy, trifluoromethyl or cyano; A represents straight chain (C.sub.2 -C.sub.5)-alkylene; or A represents straight chain (C.sub.2 -C.sub.5)-alkylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by amino or acyl-amino, by amino-lower alkyl, by acylamino-lower alkyl, by (C.sub.3 -C.sub.7)-cycloalkyl, by (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, by aryl or aryl-lower alkyl in which aryl represents phenyl or phenyl mono- or disubstituted by halogen, lower alkyl, lower alkoxy, hydroxy, acyloxy, trifluoromethyl or cyano; or A represents phenylene or cyclohexylene; pharmaceutically acceptable prodrug derivatives of any said compounds having a free carboxy group; pharmaceutically acceptable salts of any said compounds with a salt-forming group; methods for synthesis; pharmaceutical compositions thereof; and use thereof as enkephalinase inhibitors.

REFERENCES:
patent: 4052511 (1977-10-01), Cushman et al.
patent: 4105789 (1978-08-01), Ondetti et al.
patent: 4116962 (1978-06-01), Ondetti et al.
patent: 4311705 (1982-01-01), Ondetti et al.
patent: 4374847 (1983-01-01), Gruenfeld
patent: 5021430 (1991-06-01), Ksander

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