Muscarinic antagonists

US6043255A · 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
• Yuguang Wang · Shanghai, CN
• 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
• Craig D. Boyle · Readington, US

Key dates

• Filing date: Mar 10, 1999
• Grant date: Mar 28, 2000
• Expiry date: Mar 10, 2019

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## 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 Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.