Inventors:
Derek Lowe - Scotch Plains NJ
Wei Chang - Livingston NJ
Joseph Kozlowski - Princeton NJ
Joel G. Berger - Cedar Grove NJ
Robert McQuade - Scotch Plains NJ
Allen Barnett - Pine Brook NJ
Margaret Sherlock - Bloomfield NJ
Wing Tom - Cedar Grove NJ
Sundeep Dugar - Bridgewater NJ
John W. Clader - Cranford NJ
Samuel Chackalamannil - East Brunswick NJ
Wang Yuguang - North Brunswick NJ
Stuart W. McCombie - Caldwell NJ
Jayaram R. Tagat - Westfield NJ
Susan F. Vice - Mountainside NJ
Wayne Vaccaro - Yardley PA
Michael J. Green - Skillman NJ
Margaret E. Browne - Bloomfield NJ
Theodros Asberom - West Orange NJ
Assignee:
Schering Corporation - Kenilworth NJ
International Classification:
C07D29508
C07D30781
C07D33358
A61K 31495
Abstract:
Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds of formula I ##STR1## wherein one of Y and Z is N and the other is N, CH, or C-alkyl; X is --O--, --SO. sub. 0-2 --, amino, substituted amino, --CO--, --CH. sub. 2 --, mono or di-substituted methylene, --CS--, --CONR. sup. 20 --, --NR. sup. 20 --SO. sub. 2 --, --NR. sup. 20 CO--, --SO. sub. 2 NR. sup. 20 --, --CH. dbd. CH--, --C. tbd. C-- or --NHC(O)NH--; R is optionally substituted phenyl, aryl or cycloalkyl, or other substituents as defined in the specification; R. sup. 1 and R. sup. 21 are H, CN or optionally substituted alkyl, or other substituents as defined in the specification; R. sup. 2 is optionally substituted cycloalkyl or piperidyl, or other substituents as defined in the specification; and R. sup. 3, R. sup. 4, R. sup. 5, R. sup. 20, R. sup. 27 and R. sup. 28 are as defined in the specification; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease; pharmaceutical compositions and methods of preparation are also disclosed, as well as synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.
