Sri International

Other

Ronald G Almquist

Atsuro Nakazato

Lawrence Robert Toll

Joseph I De Graw

Cris M Olsen

Novel compounds useful as renin inhibitors are provided. The compounds are hydroxyazido derivatives having the structural formula ##STR1## wherein the substituents R.sub.1 through R.sub.7 are as defined herein. Analogs of these compounds which are ketozaido derivatives are also provided. Additionally disclosed re methods for using the novel compounds to treat hypertension, and pharmaceutical compositions containing the compounds. Of particular interest are formulations for oral administration.

Hydroxyazido derivatives and related compounds as renin inhibitors

A novel atrial peptide-degrading enzyme (ADE) is provided in isolated, purified form. The enzyme has a molecular weight of approximately 160,000 Daltons as measured by gel filtration chromatography, and is effective to cleave atrial peptides such as APII, APIII and ANF. Also provided are novel compounds useful as inhibitors of the enzyme and thus useful as blood pressure lowering agents, pharmaceutical compositions containing the inhibitors, and methods of using the inhibitors.

Isolated atrial peptide-degrading enzyme and novel compounds useful as

Incorporation of a ketomethylene or a hydroxyethylene group in place of the amide linking group between the Pro.sup.9 and Gly.sup.10 residues of LHRH and its analogs improves the oral activity of LHRH or its analogs.

Orally active LHRH analogs

This invention relates to novel analogs of proline terminal tripeptides and related compounds and is typified by ##STR1## The compounds are potent inhibitors of angiotensin converting enzyme and as such are useful as antihypertensive agents.

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Palo Alto, CA, United States of America

Ronald G Almquist