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US 4,716,155 AGranted
Phosphorus containing compounds and hypotensive use thereof
AssigneeE. R. Squibb & Sons, Inc.
InventorsDonald S. Karanewsky, Edward W. Petrillo, Jr.
Life of this patent
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Abstract
Phosphorus containing compounds of the formula ##STR1## wherein X is a substituted or unsubstituted imino or amino acid and A is ##STR2## These compounds possess angiotensin converting enzyme activity and are thus useful as hypertensive agents.
Claims9
A compound of the formula ##STR463## and a pharmaceutically acceptable salt thereof wherein:
- R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, lower alkyl, halo substituted lower alkyl, ##STR464## and amino substituted lower alkyl;
- q is zero or an integer from 1 to 7;
- R.sub.23 is hydrogen, lower alkyl, halo substituted lower alkyl, ##STR465## R.sub.7 is hydrogen, lower alkyl, halogen, keto, hydroxy, ##STR466## a 1- or 2-naphthyl of the formula ##STR467## a 1- or 2-naphthyloxy of the formula ##STR468## or a 1- or 2-naphthylthio of the formula ##STR469## R.sub.8 is keto, halogen, ##STR470## --O--lower alkyl, a 1- or 2-naphthyloxy of the formula ##STR471## or a 1- or 2-naphthylthio of the formula ##STR472## R.sub.9 is keto or ##STR473## R.sub.10 is halogen or --Y--R.sub.16 ;
- R.sub.13 is hydrogen, lower alkyl of 1 to 4 carbons, lower alkoxy or 1 to 4 carbons, lower alkylthio of 1 to 4 carbons, chloro, bromo, fluoro, trifluoromethy;, hydroxy, phenyl, phenoxy, phenylthio, or phenylmethyl;
- R.sub.14 is hydrogen, lower alkyl of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, lower alkylthio of 1 to 4 carbons, chloro, bromo, fluoro, trifluoromethyl, or hydroxy;
- m is zero, one, two or three;
- p is one, two or three provided that p is more than one only if R.sub.13 or R.sub.14 is hydrogen, methyl, methoxy, chloro or fluoro;
- R.sub.15 is hydrogen or lower alkyl of 1 to 4 carbons;
- Y is oxygen or sulfur;
- R.sub.16 is lower alkyl of 1 to 4 carbons or ##STR474## r is an integer from 1 to 4;
- R.sub.3 and R.sub.6 are independently selected from the group consisting of hydrogen, lower alkyl, benzyl, benzhydryl, and ##STR475## wherein R.sub.17 is hydrogen, lower alkyl, or phenyl, and R.sub.18 is hydrogen, lower alkyl, lower alkoxy, phenyl, or R.sub.17 and R.sub.18 taken together are --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.dbd.CH--, or ##STR476## R.sub.19 is lower alkyl, benzyl, or phenethyl;
- and R.sub.20 is hydrogen, lower alkyl, benzyl or phenethyl.
9 more elements
Dependencies are inferred from the claim text.