C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/239.4
C07D 487/04 (2006.01) C07D 209/38 (2006.01) C07D 265/26 (2006.01) C07D 487/14 (2006.01)
Patent
CA 1202969
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 general formula Image I wherein A signifies lower alkylene, n signifies zero or 1, R1 signifies lower alkynyl, lower alkenyl, aryl, (C3-8)- -cycloalkyl optionally substituted by lower alkyl or (C5-8)-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, R4 and R5 each represent hydrogen, halogen, trifluoromethyl, cyano, nitro, amino or lower alkyl and either R2 signifies hydrogen and R3 signifies lower alkyl or R2 and R3 together signify dimethylane, trimethylene or propenylene, the compounds of formula I in which R2 and R3 together signify di- methylene, trimethylene or propenylene having the (S) or (R,S) configuration with reference to the carbon atom denoted by Y, 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 antagoniz- ation of some or all activities which 1,4-benzodiazepines having tranquillizing activity or other substances display via the central benzodiazepine receptors.
431129
Hunkeler Walter
Kyburz Emilio
Gowling Lafleur Henderson Llp
Hoffmann-La Roche Limited
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