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US 4,284,561 AGranted
Hydroxamic acid derivatives of mercaptoacyl amino acids
AssigneeE. R. Squibb & Sons, Inc.
InventorsEdward W. Petrillo, Jr., Miguel A. Ondetti
Life of this patent
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Abstract
Hydroxamic acid derivatives of certain mercaptoacyl amino acids inhibit the conversion of angiotensin I to angiotensin II in mammals and are useful for the treatment of hypertension.
Claims19
A compound having the formula ##STR9## wherein R.sub.1 is hydrogen, alkyl, aryl, arylalkyl or ##STR10## wherein R.sub.5 is alkyl or aryl;
- R.sub.2 is hydrogen, alkyl, trifluoromethyl or pentafluoroethyl;
- R.sub.3 is --CH.sub.2 --, --CH(OH)--, --CH(O-alkyl)--, --CH(O-aryl)--, --CH(S-alkyl), --CH(S-aryl), --C(O-alkyl).sub.2, --C(S-alkyl).sub.2, ##STR11## --CCl.sub.2 --, --CF.sub.2 --, --CHCl--, or --CHF-- and R.sub.4 is --CH.sub.2 ;
- or together, R.sub.3 and R.sub.4 are --CH.dbd.CH--;
- and
- n is 0, 1 or 2;
- wherein the term "aryl" refers to phenyl or phenyl substituted with one, two or three halogen, alkyl, alkoxy, hydroxy, ##STR12## nitro, amino, alkylamino, dialkylamino, trifluoromethyl, cyano or carboxyl groups, and the terms "alkyl" and "alkoxy" refer to groups having 1 to 8 carbon atoms.
3 more elements
Dependencies are inferred from the claim text.