Schering Corporation

Margaret H Sherlock

Wing C Tom

Joseph A Kozlowski

Sundeep Dugar

Samuel Chackalamannil

Michael J Green

John W Clader

Stuart W McCombie

Wayne D Vaccaro

Joel G Berger

Wei K Chang

Theodros Asberom

Susan F Vice

Derek B Lowe

Allen Barnett

Robert D McQuade

Lian-Yong Chen

Margaret E Browne

Jayaram R Tagat

Joseph Mayer

Wang Yuguang

Craig D Boyle

Yuguang Wang

James F Long

Pauline C Ting

Daniel M Solomon

James J Kaminski

Loretta A Bober

Jay S Fine

Michael J Grace

Heide Roebke

Javaram R Tagat

Nathan Sperber

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.

Compounds of formula ##STR1## or pharmaceutically acceptable salts thereof, wherein E, Q, T, U, V, L, Z, X, W, M, Y and Y' are as set forth herein, are described. These compounds are useful as agents in the treatment of allergy, inflammation, autoimmune diseases, B-cell lymphomas, tumors, and the after effects of bone marrow transplantation.

Naphthyridines which affect IL-4 and G-CSF

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.

Heterobicyclic compounds having antiinflammatory activity

Certain substituted 1,8-naphthyridines and 1,5,8-azanaphthyridines are useful for treating allergic reactions in mammals. Certain of the compounds may also be utilized to treat chronic obstructive lung diseases in mammals. Methods for preparing the compounds and methods for their use are also described.

Method for treating allergic reactions and compositions therefore

Substituted 1,8-naphthyridinones are anti-allergic, anti-inflammatory and cytoprotective agents. Methods for their preparation and use are disclosed.

Substituted 1,8-naphthyridinones, useful as anti-allergic agents

1-Mercaptoalkyl-substituted-2-imidazolidinones having anti-inflammatory activity are disclosed. Methods for their preparation and use are described.

Anti-inflammatory 1-mercaptoalkyl-substituted-2-imidazolidinone

Certain substitute 1,8-naphthyridines and 1,5,8-azanaphthyridines are useful in treating and preventing ulcers in mammals. Methods for preparing the compounds and methods for their use are also described.

Composition containing 1-phenyl-1,8-naphthridin-2(1H)-ones and a

1-Phenyl-1,8-naphthridin-2(1H)-ones

There are disclosed certain alkali metal, alkaline earth metal, amine and amino acid salts of 3-(n-butyl)-4-hydroxy-1-phenyl-1,8-naphthyridine-2(1H)-one which, unlike the parent compound, are useful for orally treating chronic obstructive lung diseases such as asthma, bronchitis and the like.

Salts of 3(n-butyl)-4-hydroxy-1-phenyl-1,8-naphthyridine-2(1H)-one and

This invention relates to 1-amino naphthyridines prepared by a base-catalyzed condensation while in an aprotic solvent. In this condensation an o-alkyl aryl nitrile may be reacted either with the same or different o-alkyl aryl nitrile or with another nitrile. The 1-amino naphthyridines are useful as antifungal and antibacterial agents.

Process for preparing 1-aminonaphthyridines

Growing community of inventors

Bloomfield, NJ, United States of America

Margaret H Sherlock