Muscarinic antagonists

US6288068A · kind A · 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
• Javaram 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: Jan 12, 2000
• Grant date: Sep 11, 2001
• Expiry date: Jan 12, 2020

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) ##STR1## PA1 wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alheimer'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.