Imidazodiazepines

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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540498, 540503, 540495, 540506, 540511, 540504, A61K 3155, C07D48714, C07D48704, C07D49514

Patent

active

047756713

ABSTRACT:
There is presented compounds of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. signifies one of the groups ##STR2## and the dotted line signifies the double bond present in cases (1), (2) and (4) and wherein R.sup.1 signifies a 5- or 6-membered aromatic heterocyclic group or the group --C(R.sup.6).dbd.NOR.sup.7 (B), R.sup.2 signifies hydrogen and R.sup.3 signifies hydrogen or lower alkyl or R.sup.2 and R.sup.3 together signify dimethylene, trimethylene or propenylene, R.sup.4 and R.sup.5 each signify hydrogen, halogen, trifluoromethyl, cyano, nitro, amino or lower alkyl, R.sup.6 signifies hydrogen or lower alkyl and R.sup.7 signifies lower alkyl, the compound 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 signify dimethylene, trimethylene or propenylene, and pharmaceutically acceptable acid addition salts thereof have a pronounced affinity to the central benzodiazepine receptors and have anxiolytic, anticonvulsant, muscle relaxant and sedative-hypnotic properties.

REFERENCES:
patent: 4031079 (1977-06-01), Mohrbacher et al.
patent: 4316839 (1982-02-01), Gereke et al.
patent: 4352815 (1982-10-01), Hunkeler et al.
patent: 4352816 (1982-10-01), Hunkeler et al.
patent: 4352817 (1982-10-01), Hunkeler et al.
patent: 4352818 (1982-10-01), Hunkeler et al.
patent: 4353827 (1982-10-01), Hunkeler et al.
patent: 4359420 (1982-06-01), Gereke et al.
patent: 4362732 (1982-12-01), Hunkeler et al.
patent: 4435403 (1984-03-01), Braestrup et al.
patent: 4489003 (1984-12-01), Hunkeler et al.
patent: 4507313 (1985-03-01), Braestrup et al.
patent: 4622320 (1986-11-01), Watjen et al.
patent: 4622321 (1986-11-01), Watjen et al.
R. F. Squires and C. Braestrup "Benzodiazepine Receptors in Rat Brain", Nature, vol. 266, pp. 732-734, (1977).
Chang et al., "Benzodiazepine Receptors: Labeling in Intact Animals With .sup.3 H Fluritrazepam", European Journal of Pharmacology, vol. 48, pp. 213-218, (1978).

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