AMIDINES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.

摘要

Amidine phosphonate compounds have the structure in which Het is a 5- or 6- membered unsaturated nitrogen heterocycle, Z is sulphur or methylene, n is 2 or 3, R<1> is hydrogen, lower alkyl or Het-CH2Z(CH2)n2-, p is 0 or 1, R<2> is hydrogen or lower alkyl, or R<1> and R<2> together form a (CH2)2 or (CH2)3 group, R<3> is lower alkyl, aryl or aryl-(lower alkyl), and R<4> is hydrogen when p is 0 and hydrogen, lower alkyl, aryl or aryl (lower alkyl) when p is 1. Those compounds where R<4> is other than hydrogen are intermediates for the preparation of the compounds where R<4> is hydrogen, which have histamine H2-antagonist activity and are the active ingredients of pharmaceutical compositions. The compounds are prepared by primary amine coupling reactions, phosphonylation and hydrolysis.