American Home Products Corporation

Rhone-poulenc Rorer Pharmaceuticals Inc.

Wyeth

Aventis Pharma Deutschland, Gmbh

Aventis Pharmaceuticals Inc.

Rorer Pharmaceutical Corporation

Robert L Morris

Anthony C Scotese

Arthur Attilio Santilli

Kent W Neuenschwander

Michael David Collini

Rayomand Jal Unwalla

John W Ullrich

Christopher P Miller

Robert R Singhaus, Jr

David H Kaufman

James C Keith, Jr

Robert D Groneberg

Heather Anne Harris

Keith S Learn

Leo M Albert

Dilip V Amin

Mark A Bobko

Jay Edward Wrobel

William R Ewing

Donald P Strike

Stanley Charles Bell

Alfred P Spada

Christopher J Burns

Timothy Francis Gallagher

Wei He

Heinz W Pauls

Michael R Myers

Stephen M Condon

Ronald Charles Bernotas

Baihua Hu

Joseph M Karpinski

Yong Mi Choi-Sledeski

Aiwen Li

Daniel Gerard McGarry

Jeffrey N Barton

Gregory Bernard Poli

Richard F Labaudiniere

Barbara Hanney

Jean-Francois Sabuco

Michael R Becker

Thomas Caulfield

Anne Minnich

Gerard M McGeehan

John Ziqi Jiang

Ponnal Nambi

Litao Zhang

Michael F Kelley

James Winfield Jetter

Zaid Jayyosi

Roderick S Davis

Elaine Quinet

Wan F Lau

Merle Elloso

This invention is directed to oxoazaheterocycyl compounds which inhibit Factor Xa, to oxoazaheterocycyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa.

Substituted oxoazaheterocyclyl compounds

This invention provides compounds of formula I that are useful in the treatment or inhibition of LXR mediated diseases.

Quinolines and pharmaceutical compositions thereof

This invention provides estrogen receptor modulators of formula I, having the structurewherein

Substituted 2-phenyl benzofurans as estrogenic agents

The use of triaryl acid derivatives of formula (I)and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.

Therapeutic uses of tri-aryl acid derivatives

This invention relates to a class of novel amino bi- and tri-carbocyclic alkane compounds having bis-aryl substitution which exhibit squalene synthase inhibition properties. The bi- and tri-carbocyclic alkane ring contains an amino group and the ring is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

Amino bi- and tri-carbocyclic alkane bis-aryl squalene synthase

This invention relates to polycyclic compounds containing two mono- and/or bicyclic rings and a basic tertiary amino group capable of forming an ammonium ion at biological pH and which reduces levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

Multicyclic tertiary amine polyaromatic squalene syntase inhibitors

Amino Bi- and tri-carbocyclic aklane bis-aryl squalene synthase

This invention relates to polycyclic compounds containing two mono- and/or bicyclic rings and a basic tertiary amino group capable of forming an ammonium ion at biological pH and which reduces levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention. The compounds of this invention are described by the formula ##STR1## where Ar I is phenylene or naphthylene, Ar II is phenyl or naphthyl and A is 1-azabicyclo[2.2.2]octan-3-yl.

Multicyclic tertiary amine polyaromatic squalene synthase inhibitors

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

Compounds of the formula: ##STR1## wherein A is ##STR2## R is mono- or dihalo, amino, nitro, cyano, hydroxy, trifluoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl, lower cycloalkyl, carboxy, alkoxycarbonyl, mono- or di-lower alkyl substituted amino, alkanoylamino, lower alkyl thio, loweralkyl-sulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro;

Thiophene derivatives with antisecretory activity

Compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, cyano or cyano(lower)alkyl;

2-Guanyl-4-(substituted phenyl) thiazole derivatives

7,8-Dihydro-2,5,8-trisubstituted-7-oxo-pyrido[2,3-d]pyrimidine-6-carboxylic acid amide derivatives are gastric anti-secretory agents for treatment of peptic ulcer disease and generally anti-allergic agents useful in the treatment of atopic immediate hypersensitivity reactions.

7,8-Dihydro-2,5

The disclosed 2H-pyrimido[4,5-d][1,3]oxazine-2,4(1H)-dione derivatives are intermediates useful in the production of 7,8-dihydro-2,5,8-trisubstituted-7-oxo-pyrido[2,3-d]pyrimidine-6-carboxyli c acid derivatives which are gastric anti-secretory agents and anti-allergic agents.

2H-Pyrimido[4,5-d][1,3]oxazine-2,4(1H)-dione derivatives

The 5-amino-2,8-dialkyl-7,8-dihydro-7-oxo-pyrido[2,3-d]-pyrimidine-6-carboxyli c acid derivatives of the invention are anti-secretory agents.

5-Amino-2,8-dialkyl-7,8-dihydro-7-oxo-pyrido-[2,3-d]pyrimidine-6

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Wayne, PA, United States of America

Robert L Morris