Phosphonate and phosphonamide endopeptidase inhibitors
AssigneeE. R. Squibb & Sons, Inc.
InventorNorma G. Delaney
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Abstract
Compounds of the formula ##STR1## wherein Y is O or NH and X is ##STR2## will inhibit the action of neutral endopeptidase. As a result, such compounds produce diuresis, natriuresis, and lower blood pressure as well as being useful in the treatment of congestive heart failure, relieving pain, and diarrhea when administered to a mammalian host.
Claims13
A compound of the formula ##STR127## including a pharmaceutically acceptable salt thereof wherein:
- R.sub.1 is straight or branched alkyl of 1 to 4 carbons or ##STR128## R.sub.2 is straight or branched chain alkyl of 1 to 4 carbons, trifluoromethyl, or ##STR129## X is ##STR130## R.sub.3 and R.sub.5 are independently selected from the group consisting of hydrogen, straight or branched chain alkyl of 1 to 4 carbons, and an alkali metal salt ion;
- and
- q is an integer from 1 to 4.
A compound of the formula ##STR131## including a pharmaceutically acceptable salt thereof wherein:
- R.sub.1 is straight or branched chain alkyl of 1 to 4 carbons or ##STR132## R.sub.2 is straight or branched alkyl of 1 to 4 carbons, trifluoromethyl, or ##STR133## X is --NH--(CH.sub.2).sub.2 --COOR.sub.5 ;
- R.sub.3 and R.sub.5 are independently selected from the group consisting of hydrogen, straight or branched chain alkyl of 1 to 4 carbons, and an alkali metal salt ion;
- and
- q is an integer from 1 to 4.
The compound of claim 3, 4-[[(S)-2-[[hydroxy(2-phenylethyl)phosphinyl]amino]-1-oxo-propyl]amino]ben zoic acid, dilithium salt.
Dependencies are inferred from the claim text.