The novel imidazodiazepine derivatives of the general formula <IMG> I wherein A together with the two carbon atoms denoted by a and .beta. signifies one of the groups <IMG> (a) <IMG> (b) and <IMG> (c), R1 signifies a partially unsaturated lower hydrocarbon group which is optionally substituted by hydroxy, oxo, aryl of the group -OR, -SR or -OCOR or a lower alkyl group which is substituted by aryl or the group -OR', -SR' or -OCOR', R and R' each signify aryl or a saturated or partially unsaturated C1-18-hydro-carbon group which is optionally substituted by aryl or lower alkoxy, R2 signifies hydrogen and R3 signifies lower alkyl or R2 and R3 together signify dimethylene or trimethylene and R4 and R5 each signify hydrogen, halogen, trifluoromethyl, cyano, nitro or lower alkyl, the group -OR' having a significance different from lower alkoxy and the compounds of formula I having the (S)- or (R,S)-configuration with reference to the carbon atom denoted by .gamma. when R2 and R3 together signify dimethylene or trimethylene, can be used in the control or prevention of convulsions, anxiety states, stress conditions, excitation states and sleep disorders and/or in the partial or complete selective antagonism of some or all activities which 1,4-benzodiazepines having tranquillizing activity or other substances display via the central benzodiazepine receptors.
IMIDAZODIAZEPINE DERIVATIVES