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US 4,105,776 AGranted
Proline derivatives and related compounds
AssigneeE. R. Squibb & Sons, Inc.
InventorsMiguel Angel Ondetti, David W. Cushman
Life of this patent
Estimating the term…
Abstract
New proline derivatives and related compounds which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
Claims42
A compound of the formula ##STR37## wherein R is hydroxy, NH.sub.2 or lower alkoxy;
- R.sub.1 and R.sub.4 each is hydrogen, lower alkyl, phenyl or phenyl-lower alkyl;
- R.sub.2 is hydrogen, lower alkyl, phenyl, substituted phenyl wherein the phenyl substituent is halo, lower alkyl or lower alkoxy, phenyl-lower alkyl, diphenyl-lower alkyl, triphenyl-lower alkyl, lower alkylthiomethyl, phenyl-lower alkylthiomethyl, lower alkanoylaminomethyl, ##STR38## R.sub.6 -S- or R.sub.7 ;
- R.sub.3 is hydrogen, hydroxy or lower alkyl;
- R.sub.5 is lower alkyl, phenyl or phenyl-lower alkyl;
- R.sub.6 is lower alkyl, phenyl, substituted phenyl, wherein the phenyl substituent is halo, lower alkyl or lower alkoxy, hydroxy-lower alkyl or amino(carboxy)lower alkyl;
- ##STR39## M is 0 or S;
- m is 2;
- n and p each is 0, 1 or 2;
- and basic salts thereof, said lower alkoxy, lower alkyl and lower alkanoyl groups having up to seven carbon atoms.
6 more elements
A compound of the formula ##STR41## wherein R is hydroxy or lower alkoxy;
- R.sub.1 is hydrogen or lower alkyl;
- R.sub.2 is hydrogen or lower alkanoyl;
- n is 0, 1 or 2;
- and
- physiologically acceptable salts thereof, said lower alkoxy, lower alkyl and lower alkanoyl groups having up to seven carbon atoms.
2 more elements
A compound of the formula ##STR43## wherein R is hydroxy or lower alkoxy;
- R.sub.1 and R.sub.4 each is hydrogen, lower alkyl, phenyl or phenyl-lower alkyl;
- R.sub.2 is hydrogen, lower alkyl, phenyl, substituted phenyl wherein the phenyl substituent is halo, lower alkyl or lower alkoxy, phenyl-lower alkyl, diphenyl-lower alkyl, triphenyl-lower alkyl, lower alkylthiomethyl, phenyl-lower alkylthiomethyl, lower alkanoylamidomethyl, ##STR44## R.sub.6 -S- or R.sub.7 ;
- R.sub.3 is hydrogen, hydroxy or lower alkyl;
- R.sub.5 is lower alkyl, phenyl or phenyl-lower alkyl;
- R.sub.6 is lower alkyl, phenyl, substituted phenyl, wherein the phenyl substituent is halo, lower alkyl or lower alkoxy, hydroxy-lower alkyl or amino(carboxy)lower alkyl;
- ##STR45## M is 0 or S;
- m is 2;
- n and p each is 0, 1 or 2;
- and physiologically acceptable salts thereof, said lower alkoxy, lower alkyl and lower alkanoyl groups having up to seven carbon atoms.
6 more elements
Dependencies are inferred from the claim text.