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US 4,879,309 AGranted
Mercapto-acylamino acids as antihypertensives
AssigneeSchering Corporation
InventorsRonald J. Doll, Bernard R. Neustadt
Life of this patent
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Abstract
Novel mercapto-acylamino acids useful as analgesic, as well as in the treatment of hypertension and congestive heart failure and combinations of mercapto acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension and congestive heart failure are disclosed.
Claims16
A compound having the structural formula ##STR63## wherein R.sub.1 is H or R.sub.5 CO--;
- R.sub.2 is Y--C.sub.6 H.sub.4 --, Y--C.sub.6 H.sub.4 S--, Y--C.sub.6 H.sub.4 O--, Y--C.sub.6 H.sub.4 CH.sub.2 S--, Y--C.sub.6 H.sub.4 CH.sub.2 O--, .alpha.-naphthyl, .beta.-naphthyl, .beta.-naphthyl, diphenylmethyl or ##STR64## R.sub.3 is --OR.sub.6, --NR.sub.6 R.sub.7 or ##STR65## R.sub.4 is hydrogen, lower alkyl or aryl lower alkyl;
- R.sub.5 is lower alkyl, hydroxylower alkyl, lower alkoxy lower alkyl;
- (di-lower alkyl) amino lower alkyl, Y.sub.1 --C.sub.6 H.sub.4 --lower alkyl, lower alkoxy, Y.sub.1 --C.sub.6 H.sub.4 --, naphthyl;
- R.sub.6 and R.sub.7 are independently hydrogen, lower alkyl or substituted lower alkyl wherein the substituents are selected from the group consisting of 1 or 2 hydroxy groups, 1 or 2 lower alkoxy groups, lower alkoxy lower alkoxy, halogeno, halogeno lower alkoxy, amino, mono- or di-lower alkylamino, aryl, or substituted aryl wherein the substituents on aryl are 1-3 substituents selected from the group consisting of lower alkyl, hydroxy, halogeno, lower alkoxy and amino;
- R.sub.8 is hydrogen, alkyl, carboxyalkyl, mercaptoalkyl, alkylthioalkyl, aminoalkyl, hydroxyalkyl, phenylalkyl, hydroxyphenylalkyl, guanidinoalkyl, or carbamoylalkyl;
- n is 0-3;
- A is ##STR66## X and X.sub.1 are independently a bond, --O--, --S--, or --CH.sub.2 --;
- Y, Y.sub.1 and Y.sub.2 are independently 1 to 3 substituents selected from the group consisting of hydrogen, lower alkyl, cyclolower alkyl, lower alkoxy, OH, F, Cl, Br, I, --CN, --CO.sub.2 H, --CO.sub.2 --lower alkyl, --CH.sub.2 NH.sub.2, --CONH.sub.2 and aryl;
- wherein aryl means mono-cyclic or fused ring bicyclic aromatic groups having 6 to 10 ring members or a pharmaceutically acceptable acid addition salt thereof.
6 more elements
Dependencies are inferred from the claim text.