7-Isocyanato-1,4-benzodiazepin-2-ones

Details 7-Isocyanato-1,4-benzodiazepin-2-ones 7-Isocyanato-1,4-benzodiazepin-2-ones

1980-09-11

1981-10-13

Bond, Robert T.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

C07D24324

Patent

active

042947588

ABSTRACT:
This invention provides benzodiazepine derivatives of the general formula ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a hydrogen atom or a lower alkyl group, R.sup.3 represents a halogen atom and R.sup.4 represents a hydrogen or halogen atom and either R.sup.5 represents a hydrogen atom or a lower alkyl group and R.sup.6 represents a lower alkyl, lower hydroxyalkyl or lower acyloxyalkyl group or R.sup.5 represents a hydrogen atom and R.sup.6 represents an aryl or lower aralkyl group or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached represent a 3-membered to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula ##STR2## in which R.sup.7 represents a hydrogen atom or a lower alkyl group, and pharmaceutically acceptable acid addition salts thereof, which possess aldosterone-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 according suitable for the prevention or control of atherosclerosis. Also provided are a process for the manufacture of the above end products and novel intermediates therefor.

REFERENCES:
Aroher and Sternbach, "The Chemistry of Benzodiazepines", (Chemical Reviews), vol. 68, No. 6, Dec. 1968.

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