E.i. Dupont De Nemours and Company

The Dupont Merck Pharmaceutical Company

David J Carini

John J Duncia

Pancras C Wong

Gregory J Wells

John Matthew Fevig

Robert J Ardecky

Ruth Richmond Wexler

Celia Dominguez

Charles A Kettner

Joseph Cacciola

Greogry J Wells

Padmaja Mantri

Sheng-Lian O Lee

Zixia Feng

Sung-Eun Yoo

The present invention relates generally to .alpha.-aminoboronic acids and corresponding peptide analogs in which the .alpha.-carbon is substituted with an optionally functionalized piperidine containing alkyl group. These compounds are useful as inhibitors of trypsin-like serine protease enzymes.

Piperidine containing aminobornic acids

This invention relates to Novel .alpha.-aminoacid and .alpha.-aminoboronic acid and corresponding peptide analogs of the following formula: ##STR1##

Amidino and guanidino substituted boronic acid inhibitors of

Substituted imidazoles such as ##STR1## are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure.

Angiotensin II receptor blocking imidazoles

Substituted pyrazoles such as ##STR1## and their pharmaceutically suitable salts are useful as antihypertensive agents and for treatment of congestive heart failure.

Substituted pyrazole angiotensin II antagonists

Disclosed are novel radioiodinated imidazole Angiotensin II antagonists that are useful radioligands. An illustrative compound of this novel class of compounds is 4-chloro-N-[2-[4-hydroxy-3-(iodo-125I)phenyl]ethyl]-2-propyl-1-[[2'-(tetra zol-5-yl)biphenyl-4-yl]methyl]imidazole-5-carboxamide.

Radioiodinated angiotensin receptor antagonists

Substituted imidazoles such as ##STR1## which are useful as angiotensin II receptor inhibitors. These compounds have activity in treating hypertension and congestive heart failure.

Fused aryl substituted imidazole angiotensin II receptor inhibitors

Substituted imidazoles such as 2-butyl-4-chloro-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]-5-(hydroxy methyl)imidazole and 2-butyl-4-chloro-1-[(2'-carboxybiphenyl-4-yl)-methyl]-5-(hydroxymethyl)imi dazole and pharmaceutically acceptable salts thereof are useful for treating chronic renal failure, mediated by angiotensin-II.

Treatment of chronic renal failure with imidazole angiotensin-II

This invention includes substituted pyrroles, pyrazoles and triazoles, processes for their preparation, pharmaceutical compositions containing them, and their use as antihypertensive agents, and as a treatment for congestive heart failure in mammals. The heterocyclic compounds of the invention have the structural formula (I) ##STR1## or pharmaceutically suitable salts thereof.

Substituted 1,2,3 triazole angiotensin II antagonists

Method and composition for preventing NSAID-induced renal failure

Treatment of hypertension with angiotensin II blocking imidazoles

Angiotensin II antagonist antihypertensive compounds such as ##STR1## where R.sup.2 is --CHO or --COOH and R.sup.1 is ethyl have outstanding orally potency.

4-Alkylimidazole derivatives and anti-hypertensive use thereof

Treatment of congestive heart failure with angiotensin 11 receptor

Substituted pyrroles, pyrazoles and triazoles such as ##STR1## and their pharmaceutically suitable salts are useful as antihypertensive agents and for treatment of congestive heart failure.

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Wilmington, DE, United States of America

David J Carini