Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1989-08-22
1991-06-04
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540498, C07D48708, C07D49514, A61K 3155
Patent
active
050214110
ABSTRACT:
Imidazodiazepine derivatives of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. represent one of the following groups ##STR2## R.sup.1 is a partially unsaturated lower hydrocarbon group which is optionally substituted with hydroxy, oxo, aryl or the group --OR, --SR or --OCOR or a lower alkyl group which is substituted with aryl or the group --OR', --SR' or --OCOR'. R and R' each represents aryl or a saturated or partially unsaturated C.sub.1-18 -hydrocarbon group which is optionally substituted with aryl or lower alkoxy, R.sup.2 is hydrogen and R.sup.3 is lower alkyl or R.sup.2 and R.sup.3 together represent dimethylene or trimethylene and R.sup.4 and R.sup.5 each is hydrogen, halogen, trifluoromethyl, cyano, nitro or lower alkyl, the group --OR' being 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 R.sup.2 and R.sup.3 together represent dimethylene or trimethylene, can be used in the control or prevention of convulsions, anxiety states, stress conditions, excitation states and sleep disorders, or in the partial or complete selective antagonism of some or all activities which 1,4-benzodiazepines having tranquillizing activity or other substances exhibit via the central benzodiazepine receptors.
REFERENCES:
patent: 4316839 (1982-02-01), Gerecke et al.
patent: 4346030 (1982-08-01), Gerecke
patent: 4616010 (1986-10-01), Hunkeler et al.
patent: 4775671 (1988-10-01), Hunkeler et al.
patent: 4803920 (1989-09-01), Hunkeler
Hunkeler Walter
Kyburz Emilio
Meier Marc
Gerstl Robert
Gould George M.
Hoffmann-La Roche Inc.
Johnston George W.
Kass Alan P.
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