| 摘要 |
<p>1500666 Pyrimido[1,2-a]quinoline - derived amides PFIZER Inc 14 July 1976 [1 Aug 1975] 29181/76 Heading C2C The invention comprises compounds of formula and their pharmaceutically acceptable cationic salts, wherein R 1 and R 2 are each H, Cl, F or C 1-5 alkyl or alkoxy, or R 1 -R 2 is methylenedioxy or ethylenedioxy, and R 3 is Cl, Br or C 1-5 alkoxy. In examples, the amide link is formed from 5-aminotetrazole and the analogous pyrimidoquinolinecarboxylic acid; the latter is made by hydrolysing the ethyl ester, which is in turn prepared by cyclizing a correspondingly substituted ethyl 2-quinolylaminomethylenemalonate. Additionally, the product in which R 3 is halogen may be converted to one in which R 3 is alkoxy, by reaction with an alkanol. Therapeutic compositions having antiallergy activity comprise compounds of the above formula, and may contain additional active agents such as theophylline or sympathomimetic amines.</p> |
