Muscarinic antagonists

US6498168B2 · kind B2 · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Derek Lowe · Scotch Plains, US
• Wei K. Chang · Livingston, US
• Joseph A. Kozlowski · Princeton, US
• Joel G. Berger · Cedar Grove, US
• Robert McQuade · Scotch Plains, US
• Allen Barnett · Pine Brook, US
• Margaret H. Sherlock · Bloomfield, US
• Wing C. Tom · Cedar Grove, US
• Sundeep Dugar · Bound Brook, US
• Lian-Yong Chen · Edison, US
• John W. Clader · Cranford, US
• Samuel Chackalamannil · Califon, US
• Wang Yuguang · New Brunswick, US
• Stuart W. McCombie · Caldwell, US
• Jayaram R. Tagat · Westfield, US
• Susan F. Vice · Mountainside, US
• Wayne Vaccaro · Yardley, US
• Michael J. Green · Skillman, US
• Margaret E. Browne · Bloomfield, US
• Theodros Asberom · West Orange, US

Key dates

• Filing date: Jul 11, 2001
• Grant date: Dec 24, 2002
• Expiry date: Jul 11, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R1, R2, R3, R4, R21, R27, R28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.