Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing
Patent
1980-09-11
1981-07-28
Waltz, Thomas A.
Organic compounds -- part of the class 532-570 series
Organic compounds
Amino nitrogen containing
260239E, 2603264, 26032643, 544 59, 544164, 544390, 548200, 560251, 564 50, C07C12719
Patent
active
042811880
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 >N--R.sup.7 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:
patent: 3329701 (1967-07-01), Saucy et al.
patent: 3910911 (1975-10-01), Ishizumi et al.
patent: 4141895 (1979-02-01), Middleton
Fischli Albert E.
Szente Andre
Hoffman Frank P.
Hoffmann-La Roche Inc.
Leon Bernard S.
Saxe Jon S.
Waltz Thomas A.
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