3,5-Disubstituted-1,2,4-triazole compounds, processes for their preparation and pharmaceutical compositions containing them.

摘要

The invention provides compounds of the general formula (I) <CHEM> and physiologically acceptable salt, hydrates and bio-precursors thereof in which R1 represents hydrogen, C1-10 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, heteroaralkyl, trifluoroalkyl or C1-10 alkyl substituted by hydroxy, alkoxy or dialkylamino; or C1-6 alkyl substituted by cycloalkyl; R1 represnets hydrogen or a C1-4 alkyl group; or R1 and R2 may together with the nitrogen atom to which they are attached form a 5-10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or substituted by one or more C1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom, selected from oxygen or sulphur; Alk represents a straight or branched C1-6 alkylene chain; Q represents a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1- and 3-positions or 1- and 4-positions; X represents oxygen, sulphur or a methylene group; n represents zero, 1 or 2; m represents 2, 3 or 4 with the proviso that n + m is at least 3; R3 represents alkenyl, alkoxy or alkyl substituted by hydroxy, acyloxy, alkoxy, amino, alkylamino, dialkylamino, aryl, heteroaryl or C@ alkylsulphonyl; or R3 represents COR4 or CR4=NOH where R4 represents hydrogen or C1-4 alkyl. The compounds show pharmacological activity as selective histamine H2-antagonists.