Schering Corporation

Endo Laboratories, Inc.

Other

Schering Corportion

Joel G Berger

Wei K Chang

John W Clader

Joseph A Kozlowski

Wayne D Vaccaro

Theodros Asberom

Sundeep Dugar

Samuel Chackalamannil

Michael J Green

Stuart W McCombie

Margaret H Sherlock

Wing C Tom

Susan F Vice

Derek B Lowe

Allen Barnett

Robert D McQuade

Lian-Yong Chen

Margaret E Browne

Elijah H Gold

Jayaram R Tagat

Wang Yuguang

Craig D Boyle

Guowei Zhou

Yuguang Wang

Marjorie Peters

Ronald J Doll

David J Blythin

Jonathan A Pachter

Pirouz Tahbaz

Arthur J Elliott

Thomas Fevig

Konstaninos S Petrakis

Javaram R Tagat

Edward O'Connor

Bonnie Canner

Muscarinic antagonists

Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates)

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.

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 or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.

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.

Synthesis of .alpha.-substituted-aryl ethylamines

A magnetic domino set is disclosed comprising a set of dominoes magnetically attracted to a playing surface which, when folded, also serves as an attractive carrying case for the dominoes.

Magnetic domino set

A compound of formula I ##STR1## wherein X, V, W, Y, Z, R, a, b, c, and d are as described herein. These compounds are useful in the treatment of tumors, allergies, bronchoconstriction and CNS diseases and conditions.

Hydro-ethano-indeno-pyridines

Disclosed herein are compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein Ar, R, X, and Y are as described herein are described. The compounds are useful for treating psychoses and depression and for providing analgesia. Compositions containing the compounds and methods for producing the compounds are also disclosed.

Indolyl-, pyrrolyl- and pyrazolyl substituted benzazepines

Bicyclic amides as inhibitors of acyl-coenzyme A: cholesterol acyl

Bridged benzazepines

4,5-bridged-2,3,4,5-tetrahydro-1H-3-benzazepine-7-ols and derivatives

Disclosed are fused benzazepine compounds, pharmaceutical compositions including such compounds, methods of using such compounds, for example, in the treatment of psychoses and/or depression, and intermediates useful in the preparation of such compounds.

Fused benzazepines

Disclosed herein are novel compounds of formula II ##STR1## and pharmaceutically acceptable salts thereof, wherein: Q represents H, halo or --OSO.sub.2 R' wherein R' is CH.sub.3, CF.sub.3, phenyl or tolyl;

Substituted benzazepines useful as intermediates for producing

Growing community of inventors

Cedar Grove, NJ, United States of America

Joel G Berger