PURPOSE: To provide biphenylmethylimidazole derivatives excellent in angiotensin II antagonism and useful as an antihypertensive drug and a medicine for improving heart diseases.
CONSTITUTION: Compounds of formula I [R1 is alkyl or alkenyl; R2 and R3 are R1, H, cycloalkyl, aralkyl or aryl.; R4 is H, alkyl, alkanoyl, alkenoyl, alkoxycarbonyl, O- or S-containing 5- or 6-membered heterocyclic group, etc.; R5 is (protected)carboxy or CONR8R9 (R8 and R9 are H, alkyl or form alkylene in combination of both); R6 is H, alkyl or alkoxy; R7 is (protected)carboxy or tetrazol-5-yl] or salts thereof, e.g. 2-butyl-2-[(2'-carboxybiphenyl-4-yl)methyl]4- hydroxymethyl-5-imidazole-5-carboxylic acid. The above-mentioned compound can be obtained by reacting a compound of formula II with a compound of formula III in the presence of a base and, as necessary, e.g. removing a protecting group.
FUJIMOTO KOICHI
AMAMIYA YOSHIYA
SHIMOJI YASUO
KANEZAKI TAKUO
KOIKE HIROYUKI
SADA TOSHIO
