The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Apr. 27, 1982

Filed:

Jul. 16, 1981
Applicant:
Inventors:

Quirico Branca, Basel, CH;

Albert E Fischli, Riehen, CH;

Andre' Szente, Riehen, CH;

Assignee:

Hoffmann-La Roche Inc., Nutley, NJ (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07D / ;
U.S. Cl.
CPC ...
2602 / ; 424244 ;
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.


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