Benzodiazepine derivatives

C - Chemistry – Metallurgy – 07 – D

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260/240.3

C07D 243/24 (2006.01)

Patent

CA 1114373

ABSTRACT This invention provides benzodiazepine derivatives of the general formula Image I , wherein R1 represents a lower alkyl group, R2 represents a hydrogen atom or a lower alkyl group, R3 represents a halogen atom and R4 represents a hydrogen or halogen atom and either R5 represents a hydrogen atom or a lower alkyl group and R6 represents a lower alkyl, lower hydroxyalkyl or lower acyloxyalkyl group or R5 represents a hydrogen atom and R6 represents an aryl or lower aralkyl group or R5 and R6 together with the nitrogen atom to which they are attached represent a group of the formula Image or an N-methylpiperazine, thiazolidine, morpholine or thiomorpholine group, -2- and pharmaceutically acceptable acid addition salts thereof, which can be manufactured starting from partly novel intermediates. These compounds and salts possess aldo- sterone-antagonistic properties and are accordingly suitable for the control or prevention of heart failure, of hepatic ascites, of primary aldosteronism and of idiopathic hypertension. Some of these compounds and salts also inhibit the intestinal resorption of cholesterol and are accordingly suitable for the prevention or control of atherosclerosis.

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