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US 4,616,088 AGranted
Amino acid ester and amide renin inhibitor
AssigneeE. R. Squibb & Sons, Inc.
InventorsDenis E. Ryono, Edward W. Petrillo, Jr.
Life of this patent
Estimating the term…
Abstract
Compounds of the formula ##STR1## wherein A is ##STR2## intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.
Claims14
A compound of the formula ##STR88## including a pharmaceutically acceptable salt thereof wherein:
- A is ##STR89## R.sub.4 is --NR-R.sub.5 ;
- R.sub.5 is hydrogen, lower alkyl, --(CH.sub.2).sub.m -aryl or --(CH.sub.2).sub.m -heterocyclo;
- m is zero, one, two, three or four;
- R.sub.8 is hydrogen, ##STR90## R.sub.10 is hydrogen, ##STR91## R.sub.2, R.sub.3, R.sub.7 and R.sub.9 are independently selected from the group consisting of hydrogen, lower alkyl, halo substituted lower alkyl, --(CH.sub.2).sub.n --aryl, --(CH.sub.2).sub.n --heterocyclo, --(CH.sub.2).sub.n --OH, --(CH.sub.2).sub.n --NH.sub.2, --(CH.sub.2).sub.n --SH, --(CH.sub.2).sub.n --S-lower alkyl, ##STR92## n is an integer from 1 to 4;
- R.sub.11 is ##STR93## R.sub.1 hydrogen, lower alkyl, --(CH.sub.2).sub.n --aryl, --(CH.sub.2).sub.n --cycloalkyl, ##STR94## the term lower alkyl refers to straight or branched chain radicals having up to seven carbon atoms;
- the term cycloalkyl refers to saturated rings of 4 to 7 carbon atoms;
- the term halogen refers to Cl, Br, and F;
- the term halo substituted lower alkyl refers to such lower alkyl groups in which one or more hydrogens have been replaced by Cl, Br, or F groups;
- the term aryl refers to phenyl, 1-naphthyl, 2-naphthyl, mono substituted phenyl, 1-naphthyl, or 2-naphthyl wherein said substituent is lower alkyl of 1 to 4 carbons, lower alkylthio of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, halogen, hydroxy, amino, --NH-alkyl wherein alkyl is of 1 to 4 carbons, or --N(alkyl).sub.2 wherein alkyl is of 1 to 4 carbons, di or tri substituted phenyl, 1-naphthyl or 2-naphthyl wherein said substituents are methyl, methoxy, methylthio, halogen, or hydroxy;
- and
- the term heterocyclo refers to 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, imidazolyl, and indolyl.
8 more elements
Dependencies are inferred from the claim text.