Heterocyclic derivatives of di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula I (including all isomers, salts and solvates) wherein wherein one of Y and Z is âNâ and the other is âNâ or âCHâ; X is âOâ, âSâ, âSOâ, âSO â or âCH â; Q is R is alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R , R and R are H or alkyl; R is alkyl, cyclolalkyl or R is H, alkyl, âC(O)alkyl, arylcarbonyl, âSO alkyl, aryl-sulfonyl âC(O)Oalkyl, aryloxycarbonyl, âC(O)NH-alkyl or aryl-aminocarbonyl, wherein the aryl portion is optionally substituted; R is H or alkyl; and R is H, alkyl, hydroxyalkyl or alkoxyalkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimers disease. Pharmaceutical compositions and methods of treatment are also disclosed.
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:
C07D40102
US Classification:
514316, 546186, 546187, 546188, 546189
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, R , R , R , R , R , R , R , X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimers 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.
Compounds For The Treatment Of Inflammatory Disorders
Zhaoning Zhu - Plainsboro NJ, US Robert Mazzola - Clinton NJ, US Zhuyan Guo - Scotch Plains NJ, US Brian J. Lavey - Chatham NJ, US Lisa Sinning - New Providence NJ, US Joseph Kozlowski - Princeton NJ, US Brian McKittrick - New Vernon NJ, US Neng-Yang Shih - North Caldwell NJ, US
Assignee:
Schering Corporation - Kenilworth NJ
International Classification:
A61K 314709 C07D21514
US Classification:
514311, 514314, 546175
Abstract:
This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-α or combinations thereof.
Compounds For The Treatment Of Inflammatory Disorders
Zhaoning Zhu - Plainsboro NJ, US Robert Mazzola - Clinton NJ, US Zhuyan Guo - Scotch Plains NJ, US Brian J. Lavey - Chatham NJ, US Lisa Sinning - New Providence NJ, US Joseph Kozlowski - Princeton NJ, US Brian McKittrick - New Vernon NJ, US Neng-Yang Shih - North Caldwell NJ, US
Assignee:
Schering Corporation - Kenilworth NJ
International Classification:
A61K 31/165 A61K 31/18 A61K 31/21 A61K 31/27
US Classification:
514624, 514601, 514513, 514484
Abstract:
This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-α or combinations thereof.
Joseph A. Kozlowski - Princeton NJ, US Neng-Yang Shih - North Caldwell NJ, US Brian J. Lavey - Chatham NJ, US Razia K. Rizvi - Bloomfield NJ, US Bandarpalle B. Shankar - Branchburg NJ, US James M. Spitler - Westfield NJ, US Ling Tong - Warren NJ, US Ronald L. Wolin - San Diego CA, US Michael K. Wong - North Brunswick NJ, US
Joseph A. Kozlowski - Princeton NJ, US Neng-Yang Shih - North Caldwell NJ, US Brian J. Lavey - Chatham NJ, US Razia K. Rizvi - Bloomfield NJ, US Bandarpalle B. Shankar - Branchburg NJ, US James M. Spitler - Westfield NJ, US Ling Tong - Warren NJ, US Ronald L. Wolin - San Diego CA, US Michael K. Wong - North Brunswick NJ, US
Brian J. Lavey - New Providence NJ, US Joseph A. Kozlowski - Princeton NJ, US Guowei Zhou - Livingston NJ, US Ling Tong - Warren NJ, US Wensheng Yu - Edison NJ, US Michael K. C. Wong - North Brunswick NJ, US Bandarpalle B. Shankar - Branchburg NJ, US Neng-Yang Shih - Lexington MA, US M. Arshad Siddiqui - Newton MA, US Kristin E. Rosner - Watertown MA, US Chaoyang Dai - Acton MA, US Janeta Popovici-Muller - Waltham MA, US Vinay M. Girijavallabhan - Watertown MA, US Dansu Li - Watertown MA, US Razia Rizvi - Bloomfield NJ, US Lei Chen - Roselle Park NJ, US De-Yi Yang - Morris Plains NJ, US Robert Feltz - Parsippany NJ, US Seong Heon Kim - Livingston NJ, US
Dr. Kozlowski graduated from the Midwestern University/ Chicago College of Osteopathic Medicine in 1976. He works in Lansing, MI and specializes in Family Medicine. Dr. Kozlowski is affiliated with Mclaren Orthopedic Hospital.
Swaney High School Mcnabb IL 1983-1988, Dekalb County Special Education Association Dekalb IL 1985-1988
Community:
Eleanor Hewitt, Dulcy Hartkopf, Lee Burr, Marion Kuhne, Robert Judd, Richard Jensen, Nancy Boyle, Margie Kocher, Cindy Hutton, Gary Songer, Allan Turner, Darlene Powell