Diazepine derivatives and their use
AssigneeHoffmann-La Roche Inc.
InventorsWalter Hunkeler, Emilio Kyburz
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Abstract
There is presented imidazodiazepines of the formula ##STR1## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is a pyridine ring, X is an oxygen or sulphur atom, R.sup.1 is hydrogen, halogen, lower alkyl, lower alkoxymethyl or the group--COOR.sup.3 and R.sup.2 and R.sup.3 each are lower alkyl, and their pharmaceutically acceptable acid addition salts. The compounds are useful in the antagonization of the central-depressant, muscle relaxant, ataxic, blood pressure-lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity, for example as antidotes in the case of intoxications with 1,4-benzodiazepines which have tranquillizing activity. Also presented are methods to produce such imidazodiazepines.
Claims12
A compound of the formula ##STR15## wherein A together with the two carbon atoms denoted as .alpha. and .beta. is a pyridine ring, X is an oxygen or sulphur atom, R.sup.1 is hydrogen, halogen, lower alkyl, lower alkoxymethyl or a group of the formula --COOR.sup.3 and R.sup.2 and R.sup.3 each are lower alkyl, and pharmaceutically acceptable acid addition salts thereof.
The compound:
- t-Butyl 5,6-dihydro-5-methyl-6-oxo-4H-imidazo-[1,5-a]pyrido[3,4-f][1,4]diazepine-3 -carboxylate.
The compound:
- Ethyl 5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a]-pyrido[3,4-f][1,4]diazepine-3 -carboxylate.
A compound selected from the group consisting of t-Butyl, 5,6-dihydro-5-methyl-6-oxo-4H-imidazo-[1,5-a]pyrido[2,3-f][1,4]diazepine-3 -carboxylate, ethyl 5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a]pyrido[2,3-f]-[1,4]diazepine-3 -carboxylate, 3-chloro-4,5-dihydro-5-methyl-6H-imidazo[1,5-a]pyrido[2,3-f][1,4]diazepin- 6-one and t-butyl 5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a]-pyrido[3,2-f][1,4]diazepine-3 -carboxylate.
A method of antagonizing, in a patient, the central-depressant, muscle relaxant, ataxic, blood pressure lowering and respiratory-depressant properties of 1,4-benzodiazepines which have tranquillizing activity which comprises daily administration to said patient of from about 0.2 mg to about 500 mg of a compound of the formula ##STR17## wherein A together with the two carbon atoms denoted as .alpha. and .beta. signifies a pyridine ring, X signifies an oxygen or sulphur atom, R.sup.1 signifies hydrogen, halogen, lower alkyl, lower alkoxymethyl or the group --COOR.sup.3 and R.sup.2 and R.sup.3 each signify lower alkyl and the pharmaceutically acceptable acid additional salts thereof.
Dependencies are inferred from the claim text.