1-Oxo-6-substituted pyrimido [1,2-a]quinoline-2-carboxylic acids and derivatives thereof and their use as antiallergy agents

The method of treating bronchial asthma in a mammalian subject requiring such treatment which comprises administering to said subject an anti-bronchial effective amount of a compound having the formula ##STR12## wherein each of the benzenoid substituents R.sub.1, R.sub.2 and R.sub.3 is selected from the group consisting of hydrogen, alkoxy having from 1 to 5 carbon atoms, carboalkoxy having from 1 to 5 carbon atoms in the alkoxy group, fluoro, chloro, bromo, methylthio, methylsulfinyl and alkyl having from 1 to 5 carbon atoms;

• with the proviso that no more than two of R.sub.1, R.sub.2 and R.sub.3 are bulky branched chain alkyl or branched chain alkoxy groups and when two of said R.sub.1, R.sub.2 and R.sub.3 are bulky groups they are located on non-adjacent positions;
• R.sub.2 and R.sub.3 when taken together are selected from the group consisting of 1,3-butadienyl and alkylenedioxy of 1 to 2 carbon atoms;
• R.sub.4 is selected from the group consisting of chloro, bromo and OR.sub.4 ' wherein OR.sub.4 ' is selected from the group consisting of alkoxy having from 1 to 5 carbon atoms, alkenyloxy of 3 to 4 carbon atoms and alkynyloxy of 3 to 4 carbon atoms;
• R.sub.5 is selected from the group consisting of hydroxy, alkoxy having from 1 to 5 carbon atoms and hydroxy substituted alkoxy having from 2 to 5 carbon atoms;
• and the pharmaceutically-acceptable cationic salts of those compounds wherein R.sub.5 is hydroxy.

A pharmaceutical composition useful in treating bronchial asthma in a mammalian subject requiring such treatment which comprises a pharmaceutically-acceptable carrier and a compound of the formula ##STR13## wherein each of the benzenoid substituents R.sub.1, R.sub.2 and R.sub.3 is selected from the group consisting of hydrogen, alkoxy having from 1 to 5 carbon atoms, carboalkoxy having from 1 to 5 carbon atoms in the alkoxy group, fluoro, chloro, bromo, methylthio, methylsulfinyl and alkyl having from 1 to 5 carbon atoms;

• with the proviso that no more than two of R.sub.1, R.sub.2 and R.sub.3 are bulky branched chain alkyl or branched chain alkoxy groups, and when two of said R.sub.1, R.sub.2 and R.sub.3 are bulky groups they are located on nonadjacent positions;
• R.sub.2 and R.sub.3 when taken together are selected from the group consisting of 1,3-butanediol and alkylenedioxy of 1 to 2 carbon atoms;
• R.sub.5 is selected from the group consisting of hydroxy, alkoxy having from 1 to 5 carbon atoms;
• and hydroxy substituted alkoxy having from 2 to 5 carbon atoms;
• R.sub.4 is selected from the group consisting of chloro, bromo and OR.sub.4 ' wherein OR.sub.4 ' is selected from the group consisting of alkoxy having from 1 to 5 carbon atoms, alkenyloxy of 3 to 4 carbon atoms and alkynyloxy of 3 to 4 carbon atoms;
• and the pharmaceutically-acceptable cationic salts of those compounds wherein R.sub.5 is hydroxy.