NEW MATERIAL:Amidine derivatives of formula I (R is H, alkyl, hydroxyl; m and n are 1W3; Y is O or S; R1 is alkyl, halogenoalkyl, hydroxyl, amino, hydroxyamino, mono or dialkylamino, arylamino, aralkylamino, aryl; R2 is H, alkyl, hydroxyl) and their acid adducts.
EXAMPLE: N-Sulfamoyl-3-(2-guanidinothiazol-4-yl methylthio)propionamidine.
USE: Inhibitor of acid secretion in a stomach: this activity does not originate from the anticholinergic activity and some of these compounds have the activity originated from antagonic activity against histamine H2 receptors.
PREPARATION: The reaction between a compound of formula II (R' is alkyl) and an amine of the formula: H2N-R'2 or between a compound of formula III and an amine of the formula: H2N-SO2R1 affords the compound of formula I.
YANAGISAWA ISAO
ISHII YOSHIO
TSUKAMOTO SHINICHI
ITOU TOKUKI
ISOMURA YASUO
TAKEDA MASAAKI