The novel imidazodiazepine derivatives of the formula <IMG> I wherein A together with the two carbon atoms denoted by .alpha. and .beta. signifies one of the groups <IMG> <IMG> and <IMG> (a) (b) (c) R1 signifies one of the groups -CH=CH-R6 and -C?C-R6, (d) (e) R2 signifies hydrogen and R3 signifies lower alkyl or R2 and R3 together signify dimethylene or trimethylene, R4 and R5 each signify hydrogen, halogen. trifluoromethyl or lower alkyl and R6 signifies hydrogen, halogen, acyl or a saturated lower hydrocarbon group which is optionally mono- or disubstituted by hydroxy, lower alkoxy. (C3-C7)- -cycloalkyl or oxo, whereby the compounds of formula I have the (S)- or (R,S)-configuration with reference to the carbon atom denoted by .gamma. when R2 and R3 together signify dimethylene or trimethylene and whereby the double bond present in group (d) has the E- and/or Z-configuration when R6 is different from hydrogen. possess valuable pharmacodynamic properties. They have as a common characteristic a pronounced affinity to the central benzodiazepine receptors and have either pronounced anxiolytic, anticonvulsant, muscle relaxant and sedative-hypnotic properties and/or they partially or completely selectively antagonize some or all activities which 1,4-benzodiazepines having tranquillizing activity or other substances display via the central benzodiazepine receptors.
IMIDAZODIAZEPINE DERIVATIVES