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US 4,460,579 AGranted
Thiazine and thiazepine containing compounds
AssigneeE. R. Squibb & Sons, Inc.
InventorDonald S. Karanewsky
Life of this patent
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Abstract
This invention is directed to compounds of the formula ##STR1## wherein X is a thiazine or thiazepine selected from ##STR2## These compounds possess angiotensin converting enzyme inhibition activity and are thus useful as hypotensive agents.
Claims18
A compound of the formula ##STR197## and pharmaceutically acceptable salts thereof wherein:
- ##STR198## R.sub.1 is hydrogen, lower alkyl, amino substituted lower alkyl, hydroxy substituted lower alkyl, or halo substituted lower alkyl;
- n is one or two;
- R.sub.5 and R.sub.6 are independently selected from the group consisting of hydrogen, lower alkyl, --(CH.sub.2).sub.m -cycloalkyl wherein said cycloalkyl is a saturated ring of 3 to 7 carbons, and ##STR199## m is zero or an integer from 1 to 4;
- 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, halo, trifluoromethyl, or hydroxy;
- p is an integer from 1 to 3 provided that p is more than one only if R.sub.14 is hydrogen, methyl, methoxy, chloro, or fluoro;
- R.sub.7 is alkyl of 1 to 10 carbons, ##STR200## --(CH.sub.2).sub.s -cycloalkyl wherein cycloalkyl is a saturated ring of 3 to 7 carbons, --(CH.sub.2).sub.t --NH.sub.2 ##STR201## s is zero or an integer from 1 to 7;
- t is an integer from 1 to 8;
- R.sub.9 and R.sub.12 are independently selected from the group consisting of lower alkyl, halo substituted lower alkyl-(CH.sub.2).sub.m -cycloalkyl wherein cycloalkyl is a saturated ring of 3 to 7 carbons, ##STR202## R.sub.8 and R.sub.2 are independently selected from the group consisting of hydrogen, lower alkyl, benzhydryl, an alkali metal ion, an alkaline earth metal ion, and ##STR203## R.sub.10 is hydrogen, lower alkyl, cycloalkyl wherein cycloalkyl is a saturated ring of 3 to 7 carbons or phenyl;
- and
- R.sub.11 is hydrogen, lower alkyl, lower alkoxy, cycloalkyl wherein cycloalkyl is a saturated ring of 3 to 7 carbons, phenyl, benzyl, or phenethyl.
7 more elements
Dependencies are inferred from the claim text.