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Summary
Novelty: Novel aryl-fused and hetaryl-fused 2,4-diazepines, benzodiazocines and benzodiazepines are said to possess anti-arrhythmic activity. Some novel intermediates which are used in the preparation of the inventive compounds are also disclosed.
Biology: Anti-arrhythmic activity was demonstrated using electrophysiological techniques in guinea pigs. In an assay to assess the dose which causes a 20% increase in the effective refrectory period (ERP). The most active compounds had ED20 values of 0.01 to 0.05 mg/kg.
Chemistry: (R)-(+)-4,5-Dihydro-4-methyl-1-phenyl-3-(2-phenylethyl)-1H-2,4-benzodiazepine is one of eleven specifically claimed compounds.
Structure: 