Usv Pharmaceutical Corporation

Rorer Pharmaceutical Corporation

Aventis Pharma Deutschland, Gmbh

Rhone-poulenc Rorer Pharmaceuticals Inc.

Jeffrey N Barton

John T Suh

John R Regan

Jerry W Skiles

Nai-Yi Wang

William R Ewing

Yong Mi Choi-Sledeski

Paul R Menard

Edward S Neiss

Rack H Chung, Deceased

Michael R Becker

Daniel Michael Green

Yong Gong

Heinz W Pauls

Michael N Chang

Robert L Morris

Julian Roy Levell

Rack H Chung

Henry W Pauls

Laurence W Reilly, Jr

Jack Newman

Daniel G McGarry

Schmuel Ben-Sasson

James J Mencel

Paul Menard

The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide compounds

The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Sulfonic acid sulfonylamino n-(heteroaralkyl)-azaheterocyclylamide compounds

This invention relates to aromatic oligomeric compounds useful in the treatment of cardiovascular, bone metabolic, hypolipidaemic, neuronal, gastrointestinal and elastase-mediated connective tissue degradation disorders and disorders which may be treated by agents effective in binding DNA, to processes for preparation of such oligomeric compounds, to pharmaceutical compositions including such oligomeric compounds, and to their use in the treatment of such disorders.

Aromatic oligomeric compounds useful as mimics of bioactive

Disclosed are novel aryl-substituted benzocycloalkyl-derived 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula: ##STR1## their corresponding dihydroxy acids, and pharmaceutically acceptable salts thereof.

Aryl-substituted benzocycloalkyl-derived anti-atherosclerotic agents

Disclosed are novel benzothiopyranyl derivatives as 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula: ##STR1## their corresponding dihydroxy acids, and pharmaceutically acceptable salts thereof.

Benzothiopyranyl derivatives as HMG-CoA reductase inhibitors

##STR1## and pharmaceutically acceptable salts thereof, wherein: Ar is phenyl, naphthyl, heteroaryl, indole, or fused arylcycloalkyl optionally substituted with hydroxy, halo, CF.sub.3, NO.sub.2, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or aryloxy;

Aryl and heteroaryl substituted cycloalkyl compounds

Compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein: Ar is phenyl, naphthyl, heteroaryl, indole, or fused arylcycloalkyl optionally substituted with hydroxy, halo, CF.sub.3, NO.sub.2, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or aryloxy;

Bisarylamines

Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.

Antihypertensive derivatives

Carboxyalkyl dipeptide compounds

Compounds of the formulae: ##STR1## wherein, Z and Y are each alkylene or oxy-alkylene containing one to about five carbon atoms in the principal chain or said alkylene subtituted with OH, alkanoyloxy, alkoxy, mercapto or alkylmercapto;

Substituted cyclic amines

Compounds of the formulae: ##STR1## wherein, Z and Y are each alkylene or oxy-alkylene containing one to about five carbon atoms in the principal chain or said alkylene substituted with OH, alkanoyloxy, alkoxy, mercapto or alkylmercapto;

Method of hypertensive treatment using phenyl-alkylene-2-pyridyl

Method of using phenyl-alkylene-2-pyridyl derivatives to increase

The (S,S) optical isomer of a compound having the general formula ##STR1## wherein R and R.sub.1-5 are as defined herein, is recovered essentially free of the (R,S) and (S,R) isomers, by forming a solution of the esters of the (S,S) and the (R,S) and/or (S,R) isomers of said compound, selectively precipitating an acid salt (e.g. maleate) of the (S,S) ester from the solution, and treating the precipitate to form the desired free acid.

Process for the separation of (S,S) diastereoisomers

(3S)-2-N-[(1S)-1-Ethoxycarbonyl-1-(2,3-dihydro-1H-inden-2-yl)-methyl]-L-ala nyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is a antihypertensive agent.

Therapeutic dipeptides

Compounds of the formulae: ##STR1## wherein, Z and Y are each alkylene containing one to about five carbon atoms in the principal chain or said alkylene substituted with OH, alkanoyloxy, alkoxy, mercapto or alkylmercapto;

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New York, NY, United States of America

Jeffrey N Barton