76956-53-1Relevant academic research and scientific papers
TRIAZOLE ACYLAMINES, PHARMACEUTICAL COMPOSITIONS THEREOF AND METHOD OF USE THEREOF
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, (2008/06/13)
The invention relates to compounds of the general formula (I) STR1 and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR 1 and R 2, which may be the same of different, each represent hydrogen, C 1 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino alkylamino dialkylamino or cycloalkyl or R 1 and R 2 may together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C 1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom which is oxygen or sulphur; Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms,Q represents a furan or thiophene ring in which incorporation into the rest of the molecule is through bonds at the 2-and 5-positions, the furan ring optionally bearing a further substituent R 6 adjacent to the group R 1 R 2 N-Alk, or Q represents a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1-and 3-or 1-and 4-positions; R 6 represents halogen or C 1-4 alkyl which may be substituted by hydroxy or C 1-4 alkoxy;x represents--CH 2--,--O--,--S--or STR2 where R 5 represents hydrogen or methyl; n represents zero, 1 or 2;m represents 2, 3 or 4;R 3 represents hydrogen, alkyl, alkenyl, aralkyl, hydroxyalkyl with at least two carbon atoms, alkoxyalkyl, or aryl, andR 4 represents hydrogen, alkyl, alkenyl or aralkyl and R 7 represents the group COR 8 where R 8 represents hydrogen, alkyl, aryl, aralkyl, alkoxy, heteroaryl or monocyclic heteroarylalkyl or R 7 represents the group SO 2 R 9 where R 9 represents alkyl or aryl, or R. sub.7 represents the group STR3 where Y is oxygen or sulphur and R. sub.10 represents hydrogen, alkyl, cycloalkyl, aryl or aralkyl. The compounds of formula (I) show pharmacological activity as selective histamine H 2-antagonists.
