Analgesic and anti-inflammatory 4-OH quinoline carboxylic acid d

Details Analgesic and anti-inflammatory 4-OH quinoline carboxylic acid d Analgesic and anti-inflammatory 4-OH quinoline carboxylic acid d

1988-04-20

1991-01-29

Rivers, Diana

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514256, 544322, 546156, A61K 3147, C07D41714, C07D40114, C07D41314

Patent

active

049887084

ABSTRACT:
A compound selected from the group consisting of optical isomers and racemates of 4-hydroxy-3-quinoline carboxylates of the formula ##STR1## wherein X is in the 5-, 6-, 7- or 8-position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --SCF.sub.3, and OCF.sub.3, R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.2 is selected from the group consisting of thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl and tetrazolyl, all optionally substituted with alkyl of 1 to 4 carbon atoms and phenyl and phenyl substituted with at least one member of the group consisting of --OH, alkyl and alkoxy of 1 to 4 carbon atoms, --CF.sub.3, --NO.sub.2 and halogen, A is ##STR2## in which R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms and aryl, R.sub.5 is heteroaryl f 3 to 14 carbon atoms optionally substituted with alkyl of 1 to 4 carbon atoms and their non-toxic, pharmaceutically acceptable salts with acids or bases having analgesic and anti-inflammatory activity.

REFERENCES:
patent: 4486438 (1984-12-01), Clemence et al.
patent: 4735951 (1988-05-01), Cleence et al.
patent: 4845105 (1989-07-01), Clemence et al.

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