Schering Aktiengesellschaft

Berlex Laboratories, Inc.

Thomas K Morgan, Jr

Ronald A Wohl

William C Lumma, Jr

Julius Diamond

Klaus Nickisch

Randall E Lis

Gary Bruce Phillips

Paul W Erhardt

Yuo-Ling Chou

John W Lampe

Alfred A Hagedorn, Iii

Jay R Wiggins

Lumma, Jr, William C

Novel imidazolybenzoyl substituted heterocycles and their use as cardiovascular agents most especially as Class III antiarrhythmic agents is described. Pharmaceutical formulations containing such compounds are also discussed.

Imidazolylbenzoyl substituted heterocycles

This invention relates to novel 2-substituted-1(4)-aryl piperazines and to a process for their preparation. The compounds of this invention have been found to have cardiovascular, primarily antiarrhythmic effects and are of the following general formula I ##STR1## wherein R is hydrogen, lower alkyl or benzyl; and R.sub.1 and R.sub.2 are the same or independently hydrogen, lower alkyl, lower alkoxy or halogen;

2-substituted-1(4)-aryl piperazines and the process for their preparation

Novel derivatized alkanolamines of the following structural formula ##STR1## are described as useful cardiovascular agents. Most especially described is their usefulness as cardiovascular agents exhibiting an antiarrhythmic effect. Said antiarrhythmic effect is of a combination Class II/Class III variety. Pharmaceutical formulations containing such compounds are also described.

Derivatized alkanolamines as cardiovascular agents

N-(aminoalkyl)-substituted(N or C alkyl)-aryl-4-(methylsylfonylamino)benzamides of the formula ##STR1## wherein R is C.sub.1 -C.sub.4 straight chain alkyl, one of R.sub.1, R.sub.2 and R.sub.3 is a phenyl or naphthyl group and the others are hydrogen, --NR.sub.4 R.sub.5 is a secondary or teritary amino group, X and X.sub.1 are hydrogen or alkyl and n is 0 or 1, are useful as antiarrhythmic agents in the treatment of cardiac arrhythmias especially as combination Class I/Class III agents.

N-(aminoalkyl)-substituted(N or C

This invention relates to a process for the preparation of substituted sulfonamidobenzamides which compounds are known antiarrhythmic agents and to the novel N-acylaziridine employed therein.

1-[4-[(methyl-sulfonyl)amino]benzoyl]aziridine

Novel substituted 4-[1H-imidazol-1-yl]benzamides and their use in the treatment of cardiac arrthythmias especially as Class III or combination Class I/III antiarrhythmic agents is described. Pharmaceutical formulations containing such compounds are also disclosed.

Substituted 4-(1H-imidazol-1-yl)benzamides as antiarrhythmic agents

The imidazolium salts described are useful as antiarrhythmic agents. A method of treating arrhythmia by increasing the refractoriness of cardiac tissue is provided as well as pharmaceutical formulations containing such imidazolium salts.

Antiarrhythmic imidazoles

Antiarrhythmic imidazoliums

Novel quinuclidines, their acid addition, quaternary ammonium and inner salts are described. Also provided is the method of using these compounds as antiarrhythmic agents and pharmaceutical formulations containing such compounds.

Quinuclidines and quinuclidinium salts as antiarrhythmic agents

The imidazolium salts described are useful as antiarrhythmic agents. A method of treating arrhythmia by increasing the refractoriness of cardiac tissue is provided as well as pharmaceutical formulations containing such imidazolium salts. The compounds are described by the following formula: ##STR1##

Novel 1,2-disubstituted imidazol(in)es are described herein. The compounds are generally produced by reacting a haloacylanilide with an excess of 2-substituted-imidazol(in)e. The compounds are antiarrhythmic agents.

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Morris Plains, NJ, United States of America

Thomas K Morgan, Jr