| abstract |
1496787 Heteroalkylthioalkyl amidine derivatives SMITH KLINE & FRENCH LABORATORIES Ltd 10 March 1975 [12 March 1974] 10869/74 Heading C2C Novel compounds of Formula I wherein R 1 represents a grouping of the structure shown in Formula II wherein Het is an imidazole, pyridine, thiazole, isothiazole, thiadiazole, isoxazole or triazole ring which is optionally substituted by lower alkyl, hydroxyl, halogen or amino; n is 2 or 3; R 2 is lower alkyl, phenyl optionally substituted by hydroxy or mercapto, SR 4 or, when R 3 is other than hydrogen, NHR 5 ; R 3 is hydrogen, lower alkyl or R 1 ; R 4 and R 5 which may be the same or different are lower alkyl; and R 3 may be linked with R 4 or R 5 to form a thiazole or imidazoline ring; or a pharmaceutically acceptable acid adition salt thereof are prepared by usual methods for amidine and guanidine synthesis. Ethyl 4 - hydroxybenzimidate is prepared from 4-cyanophenol. Pharmaceutical compositions in conventional forms for oral or parenteral administration and having histamine H 2 -receptor blocking activity comprise an above novel compound and a carrier or diluent.n[GB1496787A] |