Quinoline derivatives, their preparation and therapeutic composi

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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546156, C07D21516, A61K 3147

Patent

active

049141104

ABSTRACT:
The invention relates to new quinoline derivatives of the formula: ##STR1## wherein R stands for C.sub.2 H.sub.5, C.sub.2 H.sub.4 F, CH.sub.2 -O-CH.sub.2 -CH.sub.2 OH, ##STR2## to a process for their preparation comprising reacting, for 12-24 hours, at 70.degree.-95.degree. C., in dimethylformamide, the 1,4-dihydro- 3-ethoxycarbonyl- 6,8- difluoro-4-oxo-quinoline with an excess of RX (2-5 mol of RX for one mol of quinoline), in the presence of K.sub.2 CO.sub.3 and subsequently hydrolysing the obtained 3-ester by HCl under reflux conditions and to pharmaceutical compositions comprising at least one 1,4-dihydro- 3-carboxy- 6,8-difluoro- 1-R-4-oxo-quinoline derivative in admixture with a pharmaceutically acceptable diluent or carrier.

REFERENCES:
patent: 4146625 (1979-03-01), Lee
patent: 4264604 (1981-04-01), Sturm
patent: 4327101 (1982-04-01), Mushika et al.

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