Syntex (u.s.a.) Inc.

Aryx Therapeutics, Inc.

University of Florida Research Foundation, Incorporated

Other

Cv Therapeutics, Inc.

Syntex LLC

Theron Pharmaceuticals, Inc.

Comentis, Inc.

Jurg R Pfister

Pascal Jean Druzgala

John H Fried

Ian T Harrison

Peter G Milner

Xiaoming Zhang

Doris L Slate

Cyrus K Becker

Luiz Belardinelli

Peter J Scammells

Ray Olsson

Stephen Baker

David John Morgans, Jr

Joseph M Muchowski

Robert J Greenhouse

George Frederic Schreiner

Todd Richard Elworthy

Jack Ackrell

David E Clarke

Eric Brian Sjogren

Meenakshi S Venkatraman

Francisco Javier Lopez-Tapia

John W Patterson

Steven R Schow

Gordon H Jones

Michael C Venuti

Robert T Lum

David Bruce Repke

Gwenaella Rescourio

Angel Guzman

Michael M Wick

Saul Jaime-Figueroa

Jean-Claude G Pascal

Chi-Ho Lee

Helen Y Wu

Tsung-tee Li

John J Bruno

Francisco X Talamas

Robert Alvarez

Marek G Nelson

Dominique Blondet

Tsung-Tee Li

Eric Brian Sjorgren

Gary W Bantle

Arturo Perez-Medrano

Roman Davis

John M Armstrong

Leslie Patmore

Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetylcholine receptor-mediated diseases, such as pulmonary diseases, are provided.

7-azoniabicyclo[2.2.1]heptane derivatives, methods of production, and pharmaceutical uses thereof

The subject invention provides novel compounds and compositions for the safe and effective treatment of gastroesophageal reflux and related conditions. In a preferred embodiment, the compositions of the subject invention comprise esterified cisapride derivatives. These compositions possess potent activity in treating gastroesophageal reflux disease and substantially reduce adverse effects associated with the administration of cisapride. These adverse effects include, but are not limited to, diarrhea, abdominal cramping and elevations of blood pressure and heart rate.

Materials and methods for the treatment of gastroesophageal reflux disease

The subject invention provides useful and novel 5-HT3 antagonists. The subject invention also provides methods for synthesizing the compounds of invention. The invention also provides methods for the treatment of irritable bowel syndrome and other such conditions.

5-HT3 receptor antagonists and methods of use

The subject invention provides novel HMG-CoA-reductase inhibitors. In a preferred embodiment, the HMG-CoA reductase inhibitors of the subject invention can be deactivated to a primary inactive metabolite by hydrolytic enzymes. Compounds of the present invention can be advantageously used to treat patients suffering hypercholesterolemia.

Materials and methods for treating hypercholesterolemia

The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.

Materials and methods for the treatment of diabetes, hyperlipidemia, hypercholesterolemia, and atherosclerosis

10,11-Methanodibenzosuberane derivatives, i.e., the compounds of Formula I: ##STR1## wherein: A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHR.sup.a --CH.sub.2 --, or --CH.sub.2 --CHR.sup.a --CHR.sup.b --CH.sub.2 --, where one of R.sup.a or R.sup.b is H, OH, or lower acyloxy, and the other is H; R.sup.1 is H, F, Cl or Br; R.sup.2 is H, F, Cl or Br; and R.sup.3 is heteroaryl or phenyl optionally substuted with F, Cl, Br, CF.sub.3, CN, NO, or OCHF.sub.2 ; and the pharmaceutically acceptable salts thereof, are useful chemosensitizing agents, e.g., for cancer chemotherapy, particularly for treating multidrug resistance.

10,11-methanodibenzosuberane derivatives

Adenosine and xanthine deriviatives, and compositions comprising those compounds, are potent selective agonists of adenosine receptors. The derivatives and compositions are used to treat conditions, including certain cardiac arrhythmias.

Method for using A.sub.1 adenosine receptor agonists

10,11-Methanodibenzosuberane derivatives, i.e., the compounds of Formula I: ##STR1## wherein: A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHR.sup.a --CH.sub.2 --, or --CH.sub.2 --CHR.sup.a --CHR.sup.b --CH.sub.2 --, where one of R.sup.a or R.sup.b is H, OH, or lower acyloxy, and the other is H;

10, 11-methanodibenzosuberane derivatives

10,11-Methanodibenzosuberane derivatives, i.e., the compounds of Formula I: ##STR1## wherein: A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHR.sup.a --CH.sub.2 --, or --CH.sub.2 --CHR.sup.a --CHR.sup.b --CH.sub.2 --, where one of R.sup.a or R.sup.b is H, OH, or lower acyloxy, and the other is H; R.sup.1 is H, F, Cl or Br; R.sup.2 is H, F, Cl or Br; and R.sup.3 is heteroaryl or phenyl optionally substuted with F, Cl, Br, CF.sub.3, CN, NO.sub.2 or OCHF.sub.2 ; and the pharmaceutically acceptable salts thereof, are useful chemosensitizing agents, e.g., for cancer chemotherapy, particularly for treating multidrug resistance.

Compounds of Formula I: ##STR1## where R.sup.5 is a group selected from Formulae (a), (b), (c) and (d): ##STR2## and the pharmaceutically acceptable salts and N-oxides thereof, are .alpha..sub.1 -adrenergic receptor antagonists useful for the treatment of diseases involving directly or indirectly an obstruction of the lower urinary tract, such as benign prostatic hyperplasia.

Pyrimidinedione, pyrimidinetrione, triazinedione and

Growing community of inventors

Los Altos, CA, United States of America

Jurg R Pfister