Schering Corporation

Maureen Laverty

Duane A Burnett

Harry R Davis

Scott W Altmann

Xiaorui Yao

Michael P Graziano

Suke Wang

Frederick James Monsma, Jr

Elizabeth B Smith

Eric L Gustafson

Xiaoxin Yang

The invention relates to the use of the interaction between the GPR78 polypeptide or the GPR26 polypeptide and their identified ligands and antagonists as the basis for screening methods for the identification of agents that modulate the activity of these receptors, and for diagnostic and therapeutic purposes. The agents identified by the screening methods of the invention have use in the treatment of GPR78- and/or GPR26-mediated disorders, including, but not limited to, neurological disorders (such as anxiety disorders), metabolic disorders, cardiovascular disorders, hormone-related disorders, vascular disorders and hyperproliferative disorders (such as cancer).

Modulators of the orphan G protein-coupled receptors GPR78 and GPR26

The use of azetidinone compounds that are inhibitors of cholesterol absorption as tools for discovering and characterizing proteins involved in trafficking or absorption of cholesterol and/or cholesteryl esters in biological systems is presented. These compounds can serve as tools for competitive binding assays to discover and characterize other chemical agents useful as cholesterol absorption inhibitors. New compounds of the present invention are also highly efficacious inhibitors of cholesterol absorption.

Use of azetidinone compounds

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Old Bridge, NJ, United States of America

Maureen Laverty