Tricyclic pyridone derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546 80, C07D51304, A61K 3138

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active

052583872

ABSTRACT:
The novel pyridone derivatives of the formula ##STR1## wherein Ra is hydrogen or halogen, Rb is --OR.sup.1 or --NR.sup.2 R.sup.3 ; R.sup.1 is an unsubstituted lower alkyl or a lower alkyl substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)amino, di(lower alkyl)carbamoyl or lower alkoxycarbonylamino; R.sup.2 is hydrogen or a lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)-amino, di(lower alkyl)carbamoyl or lower alkoxycarbonyl-amino; and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 taken together with the nitrogen atom to which they are attached is a 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl or 1-piperazinyl which is unsubstituted or mono- or disubstituted by lower alkyl, hydroxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl or phenyl; B and the carbon atom denoted by a taken together is a group of the formula >C.sub..alpha. --S--CH.dbd.CH-- or >C.sub..alpha. --CR.sup.4 .dbd.CH--CH.dbd.CH-- and R.sup.4 is hydrogen, fluorine or chlorine,
can be used for the control or prevention of illnesses. In particular, they have muscle relaxant, sedative-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.

REFERENCES:
patent: 4885297 (1989-08-01), Fischer et al.
CA 88; 169 907 d, p. 570, 1978.

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