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US 4,544,654 AGranted
Substituted sulfonamidobenzamides, antiarrhythmic agents and compositions thereof
AssigneeSchering Corporation
InventorsDavid D. Davey, William C. Lumma, Jr., Ronald A. Wohl
Life of this patent
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Abstract
Novel substituted sulfonamidobenzamides are described as useful antiarrhythmic agents. Their use in the treatment of cardiac arrhythmias, especially re-entrant arrhythmias, via the prolongation of the action potential of cardiac tissue is provided. Pharmaceutical formulations containing such compounds are also disclosed.
Claims28
A compound according to the formula:
- ##STR7## wherein R=lower alkyl, cycloalkyl, cycloalkyl(lower)alkyl, benzyl, or benzyl substituted by halogen, loweralkyl, loweralkoxy, or lower alkyl substituted by hydroxy, lower alkoxy, carbamoyl, N-loweralkylcarbamoyl, N,N-diloweralkylcarbamoyl and sulfamoyl;
- X,X.sub.1 =hydrogen and halogen;
- R.sub.1 =hydrogen, loweralkyl, unsaturated loweralkyl, loweralkoxyloweralkyl, or collectively with R.sub.2 is an alkylene chain forming an azetidine, pyrrolidine, piperidine, or hexahydroazepine ring, or collectively with R.sub.3 is a bond or an alkylene chain forming an azetidine, pyrrolidine, piperidine or a hexahydroazepine ring, or collectively with R.sub.5 may produce a piperazine or a hexahydro-1,4-diazepine ring system;
- R.sub.2 =hydrogen, loweralkyl or collectively with R.sub.3 is a bond or an alkylene chain to form a saturated carbocyclic ring of from 4 to 8 ring carbon atoms.
- R.sub.3,R.sub.4 =hydrogen, loweralkyl or collectively is an alkylene chain forming a saturated carbocyclic ring of from 4 to 6 ring carbon atoms;
- R.sub.5,R.sub.6 =unsaturated loweralkyl, C.sub.1 -C.sub.12 straight or branched chain alkyl, C.sub.3 -C.sub.6 cycloalkyl, cycloalkyl(lower)alkyl, or when taken together form a saturated heterocyclic ring of from 4 to 8 ring members which may be substituted by one or more methyl groups or optionally contains a --O--, or ##STR8## linkage wherein p is the integer 0, 1 or 2;
- R.sub.6 =loweralkyl substituted by phenyl which may be substituted by up to 3 substituents selected from hydroxy or methoxy groups;
- n=0, 1, 2;
- and the pharmaceutically acceptable salts thereof;
- with the proviso that:
- (a) when any of R.sub.1, R.sub.5 or R.sub.6 is unsaturated loweralkyl, the unsaturation cannot be alpha to the nitrogen atom.
8 more elements
Dependencies are inferred from the claim text.