Substituted naphthyridinones, processes for their preparations and therapeutical applications.

摘要

Compounds of formula

wherein
X is sulfur, oxygen or imino;
n is an integer of from 2 to 6 such that the length of the carbon chain connecting the two nitrogen atoms is not less than 2;
R1, R2, R3, R4 and R5 are independently hydrogen, loweralkyl, loweralkoxy, amino, haloloweralkyl, or phenyl; or any two adjacent substituents may be joined to form a benzo substituent;
R6 and R7 are independently hydrogen, phenyl-loweralkyl, N-loweralkylcarbamoyl, N-loweralkylthiocarbamoyl; or R6 and R7 may be joined to form a morpholino ring or R6 and R7 may be an alkylene linkage of 4 or 5 carbon atoms to form a pyrrolidine or piperidine group which may be substituted with loweralkyl, oxo or benzo substituents; and the broken line in the 3,4 position of the naphthyridine molecule indicates that the bond may be either a single or a double bond; and the acid addition and quaternary ammonium salts thereof, provided that when n is 2, R3, R5, R6 and R7 are all methyl groups X, is oxygen and the 3,4-position is unsaturated at least one of R1, R2 or R4 is other than hydrogen are disclosed.
These compounds inhibit gastric secretions in the gastro-intestinal tract.