Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal
Patent
1981-07-16
1982-04-27
Bond, Robert T.
Chemistry of carbon compounds
Miscellaneous organic carbon compounds
C-metal
424244, C07D24324
Patent
active
043270263
ABSTRACT:
There is presented benzodiazepine derivatives of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is lower alkyl, R.sup.2 and R.sup.3 each are hydrogen or lower alkyl, R.sup.4 is the group ##STR3## R.sup.5 is hydrogen or halogen, R.sup.8 is hydrogen or lower alkyl, R.sup.9 is lower alkyl or lower alkoxyalkyl, R.sup.10 is lower alkyl, R.sup.11 is hydrogen, lower alkyl or lower hydroxyalkyl, R.sup.12 is hydrogen or lower alkyl and R.sup.14 is lower alkyl or aryl, and either R.sup.6 is hydrogen or lower alkyl and R.sup.7 is lower alkyl or lower hydroxyalkyl or R.sup.6 and R.sup.7 together with the nitrogen atom are a 3- 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.13, in which R.sup.13 is hydrogen or lower alkyl, and either R.sup.6 ' is hydrogen or lower alkyl and R.sup.7 ' is lower alkyl or R.sup.6 ' and R.sup.7 ' together with the nitrogen atom are a 3- 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.13 ', in which R.sup.13 ' is lower alkyl, with the proviso that R.sup.4 is the group R.sup.6 ' R.sup.7 ' N--CO--NH--CH(R.sup.8)-- when A is the group (c),
and pharmaceutically acceptable acid addition salts thereof.
The compounds exhibit aldosterone-antagonistic properties and are suitable for the control or prevention of heart failure, hepatic ascites, primary aldosteronism and idiopathic hypertension.
REFERENCES:
patent: 4294758 (1981-10-01), Fischli et al.
Branca Quirico
Fischli Albert E.
Szente Andre
Bond Robert T.
Hoffman Frank P.
Hoffmann-La Roche Inc.
Leon Bernard S.
Saxe Jon S.
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