2-Heterocyclyl oxy-alkyl-4(1H)-pyrimidone derivs. - useful as inhibitors of gastric acid secretion, antiinflammatory agents etc.

摘要

2-Heterocyclyloxyalkyl- 4(1H)-pyrimidone derivs. of formula (I) and their salts are new. (R1 is H, 1-10C alkyl, 2-5C alkenyl, 2-5C alkynyl, Ph, cycloalkylmethyl, opt. substd. aralkyl or A-NR3R4; A is 1-5C alkylene; R3 and R4 are 1-5C alkyl; or NR3R4 is piperidino or pyrrolidino; R2 is H, 1-5C alkyl or CF3; Y is 5-dimethylamino-2-furyl, m-(N-piperidinomethyl)phenyl or a heterocyclic gp. of formula (II); R is H or 1-5C alkyl; B is O or S; m is 0-3; and n is 1-3). Intermediates of formulae (II) and (III) are new (sic.). (R5 is 1-5C alkyl). (I) are inhibitors of gastric acid secretion, anti-inflammatory agents and agents for treating cardiovascular and stomach diseases. (I; R1 is 4-9C alkyl) have a cytoprotective action as well as histamine H2-receptor blocking activity. Dose is 0.1-0.8 g daily in 1-4 doses. Specifically claimed are 8 cpds. (I), including 5-(p-t-butyl-benzyl)-2- 2-(((2- ((diaminomethylene) amino)-4-thiazolyl) methyl)thio)ethyl)-6-methyl-4(1H)-pyrimidone and the corresp. 5-n-butyl and 5-n-pentyl cpds.