Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1987-11-18
1988-10-04
Bond, Robert T.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
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.
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Hunkeler Walter
Kyburz Emilio
Bond Robert T.
Hoffmann-La Roche Inc.
Isgro William G.
Leon Bernard S.
Saxe Jon S.
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