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US 4,361,511 AGranted
Benzodiazepine derivatives
AssigneeHoffmann-La Roche Inc.
InventorsQuirico Branca, Albert E. Fischli, Andre Szente
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AssigneeHoffmann-La Roche Inc.
InventorsQuirico Branca, Albert E. Fischli, Andre Szente
Estimating the term…
There are presented compounds of the formula ##STR1## wherein R.sup.1 is a lower alkyl group, R.sup.2 is a hydrogen atom or a lower alkyl group, R.sup.3 is a hydrogen or halogen atom, R.sup.4 is a hydrogen atom or a group of the formula R.sup.5 --CO--,R.sup.6 R.sup.7 N--O--, ##STR2## A is a lower alkylene group, X is an oxygen or sulphur atom or a group of the formula >N--.sup.8 , R.sup.5 is a lower alkyl or lower haloalkyl group, R.sup.6 is a hydrogen atom or a lower alkyl group, R.sup.7 is a lower alkyl group and R.sup.8 is a hydrogen atom or a lower alkyl or lower hydroxyalkyl group, and their pharmaceutically acceptable acid addition salts. The compounds have aldosterone-antagonistic properties and are accordingly suitable for the control or prevention of heart failure, hepatic ascites, primary aldosteronism and idiopathic hypertension.
A compound of the formula ##STR40## wherein R.sup.1 is a lower alkyl group, R.sup.2 is a hydrogen atom or a lower alkyl group, R.sup.3 is a hydrogen or halogen atom, R.sup.4 is a hydrogen atom or a group of the formula R.sup.5 -CO-, R.sup.6 R.sup.7 N-CO-, ##STR41## A is a lower alkylene group, X is an oxygen or sulphur atom or a group of the formula >N-R.sup.8, R.sup.5 is a lower alkyl or lower haloalkyl group, R.sup.6 is a hydrogen atom or a lower alkyl group, R.sup.7 is a lower alkyl group and R.sup.8 is a hydrogen atom or a lower alkyl or lower hydroxyalkyl group, and their pharmaceutically acceptable acid addition salts.
The compound:
The compound:
The compound:
A compound selected from the group consisting of
A compound of the formula ##STR43## wherein R.sup.41 is a protecting group of the group consisting of tertbutoxycarbonyl, benzoyloxycarbonyl, benzyl, tetrahydropyranyl, 2methoxy-2-propyl, methoxymethyl, .beta.-methoxyethoxymethyl, tertbutyl and acetyl or a group of the formula ##STR44## U is an oxygen or sulphur atom or a group of the formula >N-R.sup.83, R.sup.62 is a protecting group of the group consisting of tertbutoxycarbonyl, benzoyloxycarbonyl, benzyl, tetrahydropyranyl, 2-methoxy-2-propyl, methoxymethyl, .beta.-methoxyethoxymethyl, tertbutyl and acetyl, R.sup.72 is a lower alkyl group, R.sup.82 is a protecting group of the group consisting of tertbutoxycarbonyl, benzoyloxycarbonyl, benzyl, tetrahydropyranyl, 2-methoxy-2-propyl, methoxymethyl, .beta.-methoxyethoxymethyl, tertbutyl and acetyl or a group of the formula -A-O-V, R.sup.83 is a hydrogen atom, a lower alkyl group, a lower hydroxyalkyl group, a protecting group of the group consisting of tertbutoxycarbonyl, benzoyloxycarbonyl, benzyl, tetrahydropyranyl, 2-methoxy-2-propyl, methoxymethyl, .beta.-methoxyethoxymethyl, tertbutyl and acetyl or a group of the formula -A-O-V and R.sup.9 and V each are a protecting group of the group consisting of tertbutoxycarbonyl, benzoyloxycarbonyl, benzyl, tetrahydropyranyl, 2-methoxy-2-propyl, methoxymethyl, .beta.-methoxyethoxymethyl, tertbutyl and acetyl wherein R.sup.1 is a lower alkyl group, R.sup.2 is a hydrogen atom or a lower alkyl group, R.sup.3 is a hydrogen or halogen atom and A is a lower alkylene group.
A compound of the formula ##STR45## wherein R.sup.42 is a group of the formula ##STR46## L is a leaving group selected from the group consisting of tosyloxy or alkylsulphonyloxy, R.sup.1 is a lower alkyl group, R.sup.2 is a hydrogen atom or a lower alkyl group, R.sup.3 is a hydrogen or a halogen atom and A is a lower alkylene group.
A compound of the formula ##STR47## wherein R.sup.1 is a lower alkyl group, R.sup.2 is a hydrogen atom or a lower alkyl group, R.sup.3 is a hydrogen or halogen atom, A is a lower alkylene group and L represents a leaving group selected from the group consisting of tosyloxy or alkylsulphonyloxy.
Dependencies are inferred from the claim text.