method for the preparation of quinoline carboxylic acid - 3 - new derivatives, process conditions of pharmaceutical preparations alone in this, and thus formed the preparations.

摘要

Novel quinoline-3-carboxamides of the formula IMAGE I wherein R1 is in the 5,6,7 or 8-position and is selected from the group consisting of hydrogen, halogen, -CF3, -OCF3, -SCF3, straight chain alkyl of 1 to 4 carbon atoms, branched alkyl of 3 to 5 carbon atoms and alkoxy of 1 to 4 carbon atoms, R2 is selected from the group consisting of hydrogen and methyl, R3 is selected from the group consisting of thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl and imidazolyl and R4 is selected from the group consisting of hydrogen, hydroxyl, alkyl of 1 to 4 carbon atoms, phenyl and benzyl with the proviso that when R1 is in the 7 or 8-position and is halogen, -CH3, -OCF3 or -SCF3 and R4 is hydrogen, R3 is not thiazolyl, pyridinyl or oxazolyl and the non-toxic, pharmaceutically acceptable acid addition salts when R3 is imidazolyl or 4,5-dihydrothiazolyl having analgesic activity and their preparation and novel intermediates therefore.