1-Oxo-6-substituted pyrimido [1,2-a]quinoline-2-carboxylic acids

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...

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260251A, 2602564F, A61K 31505, C07D47104

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active

040667669

ABSTRACT:
A novel series of 1-oxo-1H-6-substitutedpyrimido[1,2-a]quinoline-2-carboxylic acids of the formula ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3 is hydrogen, alkyl having from 1 to 5 carbon atoms, alkoxy having from 1 to 5 carbon atoms, carboalkoxy having from 1 to 5 carbon atoms in the alkoxy group, fluoro, chloro, bromo, methylthio or methylsulfinyl; with the proviso that no more than two of R.sub.1, R.sub.2 and R.sub.3 are bulky groups; i.e., branched-chain alkyl or branched-chain alkoxy, 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.4 is selected from the group consisting of chloro and 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 hydroxy, alkoxy having from 1 to 5 carbon atoms and hydroxy substituted alkoxy having from 2 to 5 carbon atoms; R.sub.2 and R.sub.3 when taken together are 1,3-butadienyl or alkylenedioxy of one to two carbon atoms; and the pharmaceutically-acceptable cationic salts of those compounds wherein R.sub.5 is hydroxy; compositions thereof; and their use as antiallergy agents.

REFERENCES:
patent: 3743733 (1973-07-01), Houlihan
patent: 4014881 (1977-03-01), Kadin et al.
patent: 4017625 (1977-04-01), Kadin
Gupta et al., Indian J. Chem., vol. 9, No. 3, 201-206 (1971).
Richardson et al., J. Med. Chem. 15, 1203-1206 (1972).

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