Rorer Pharmaceutical Corporation

William H. Rorer, Inc.

Rhone-poulenc Rorer Pharmaceuticals Inc.

Versicor, Inc.

Rorer Pharmaceutical Corporaton

Donald E Kuhla

Henry F Campbell

William L Studt

William C Faith

Stuart A Dodson

Bruce F Molino

Alfred P Spada

John Yelnosky

Kent W Neuenschwander

Scott I Klein

Raymond D Youssefyeh

Raymond Youssefyeh

Thomas Tucker

John R Regan

Robert A Galemmo, Jr

Pamela J Durham

Robert L Smith

James Barnes

Matthew R Powers

Billy J Chou

John E Airey

Joseph G Bruno

Gnanasambandam Kumaravel

Josehp G Bruno

The subject invention features substituted N-heteroaromatic compounds, libraries of substituted N-heteroaromatic compounds, and methods of synthesis thereof. For example, the present invention provides methods for synthesizing substituted N-heteroaromatic compounds, and is particularly amenable to the generation of libraries of substituted N- heteroaromatic compounds by combinatorial chemistry. The methods of the invention generally feature the reaction of O-linked heteroaromatic N-oxides with nucleophiles to produce substituted N-heteroaromatic compounds.

Synthesis of substituted N-heteroaromatic compounds and methods of use

This invention is directed to certain dibenzofurancarboxamides and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinctic activity void of any significant D.sub.2 receptor binding properties. This invention also describes novel processes necessary for their preparation.

Pharmaceutically useful dibenzofurancarboxamides of specific

This invention relates to substituted pyridooxazinone and naphtheridone pyridones which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.

Naphtheridinone- and pyridooxazinone-pyridone compounds, cardiotonic

Compounds useful for increasing cardiotonic contractility in humans or other animals and pharmaceutical compositions including these compounds are disclosed. The compounds have the general structure: ##STR1## where A is ##STR2## R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.9, and R.sub.10 are H, lower alkyl of 1-4 carbon atoms, phenyl, substituted phenyl, phenyl lower alkyl of 1-4 carbon atoms or substituted phenyl lower alkyl of 1-4 carbon atoms; and n is 0 or 1.

Compounds having cardiotonic activity

Disclosed are novel 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof. Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.

HMG-COA reductase inhibitors

This invention is directed to certain dibenzofurancarboxamides and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinetic activity void of any significant D.sub.2 receptor binding properties. This invention also describes novel processes necessary for their preparation.

Hexahydrodibenzofuran carboxylic acid derivatives

This invention relates to pyridyl-pyrazolinone compounds of the formula ##STR1## uses of said compounds as cardiotonic agents including methods for increasing cardia contractility and the treatment of congestive heart failure, pharmaceutical compositions including the same and methods for the preparation thereof.

Pyridyl-pyridazinone and pyridyl-pyrazolinone compounds and their use in

Certain specific substituted 9-N-(1-azabicycolo-[2.2.2.]octan-3-yl)carboxamido-2,3,4,5-tetrahydro-1-ben zoxepins and their valuable use as 5-HT.sub.3 antagonists having CNS and gastric prokinetic activity and void of any significant D.sub.2 receptor binding properties are disclosed. Methods for their preparation also are described.

Benzoxepins as intermediates to 5HT.sub.3 antagonists

This invention relates to substituted pyridooxazinone and naphtheridone pyridazinone and pyrazolone compounds which are useful as cardiotonic agents for the treatment of congestive heart failure, to methods for increasing cardiac contractility using said compounds, and pharmaceutical compositions including the same.

Pyridazinone and pyrazolone compounds, cardiotonic compositions

Novel HMG-CoA reductase inhibitors

Benzodiazinone-pyridazinone and hydroxy-pyrazolyl compounds, cardiotonic

Dibenzofurancarboxamides and their pharmaceutical compositions and

Certain specific substituted 9-N-(1-azabicyclo[3.3.1.]nonan-4-yl)carboxamido-2,3,4,5-tetrahydro-1-benzo xepins and their valuable use as 5-HT.sub.3 antagonists having CNS and gastric prokinetic activity and void of any significant D.sub.2 receptor binding properties are disclosed. Methods for their preparation also are described.

Certain benzoxepins and their pharmaceutical compositions and methods

Compounds useful for increasing cardiotonic contractility in humans or other animals and pharmaceutical compositions including these compounds are disclosed. The compounds have the general structure ##STR1## wherein: A is ##STR2## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.8, R.sub.10, R.sub.11, R.sub.12, R.sub.14, R.sub.15, R.sub.16, R.sub.17, R.sub.18, R.sub.19, R.sub.20, R.sub.21, R.sub.22, R.sub.23 and R.sub.24 are H, lower alkyl of 1-4 carbon atoms, phenyl, substituted phenyl, phenyl lower alkyl of 1-4 carbon atoms or substituted phenyl lower alkyl of 1-4 carbon atoms;

Growing community of inventors

Doylestown, PA, United States of America

Donald E Kuhla