Imidazobenzodiazepines

Details Imidazobenzodiazepines Imidazobenzodiazepines

1983-07-14

1984-12-18

Bond, Robert T.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

2602393T, 424256, 424273R, C07D47114, C07D47122, C07D51322, A61K 3155

Patent

active

044890036

ABSTRACT:
There are described novel pharmaceutically active substances which have a pronounced affinity to the central benzodiazepine receptors and which have only a low toxicity.
These active substances, namely imidazobenzodiazepines of the formula ##STR1## wherein A is lower alkylene, n is zero or 1, R.sup.1 is lower alkynyl, lower alkenyl, aryl, (C.sub.3-8)-cycloalkyl optionally substituted by lower alkyl or (C.sub.5-8)-cycloalkenyl optionally substituted by lower alkyl, or a 5- or 6-membered saturated or unsaturated heterocycle which contains an oxygen or sulphur atom as a ring member and which is optionally substituted by lower alkyl, R.sup.4 and R.sup.5 each are hydrogen, halogen, trifluoromethyl, cyano, nitro, amino or lower alkyl and either R.sup.2 is hydrogen and R.sup.3 is lower alkyl or R.sup.2 and R.sup.3 together are dimethylene, trimethylene or propenylene, the compounds of formula I in which R.sup.2 and R.sup.3 together are dimethylene, trimethylene or propenylene having the (S) or (R,S) configuration with reference to the carbon atom denoted by .gamma.,
and their pharmaceutically acceptable acid addition salts, can be used as medicaments in the form of pharmaceutical preparations, especially in the control of convulsions and anxiety states and/or in the partial or complete antagonization of some or all activities which 1,4-benzodiazepines having tranquillizing activity or other substances display via the central benzodiazepine receptors.

REFERENCES:
patent: 4316839 (1982-02-01), Gerecke 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: 4353827 (1982-10-01), Hunkeler et al.

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