| abstract |
PURPOSE: To provide the novel imidazole derivatives which have an antagonistic activity to angiotensin II, receptors and the useful for treatment of the arterial hypertension, cardiac failure, renal failure, etc. n CONSTITUTION: This compd. is expressed by formula I [A may be oxidized by the residue of a group consisting of a 3, 4 or 5-membered monocyclic group or 6 to 12-memberd condensed ring and may contain ≥1 pieces of complex atoms of N or S; R is 1 to 6C alkyl, alkenyl, etc., may be substd.; R 1 to R 4 are each H, halogen, hydroxyl, etc., or 1 to 6C alkyl, alkenyl, etc., may be substd.; R 5 is CH 2 ; Y is formula II (Y 1 is unsubstd. phenyl; Y 2 is free carboxy which may be subjected to salt formation in a zero position, etc.; B is CO-NH, etc.)]. The compd. of the formula I is obtd. by bringing the compd. of formula III (X is 0, etc.; R 15 is OH, etc.; R' is the same as R) into reaction with the compd. of formula IV (R' 1 to R' 4 are the same as R 1 to R 4 ) to obtain the compd. of formula V and bringing the compd. of formula VI (Hal is halogen) into reaction with the resultant compd. 4-[(2-Butyl-1H-benzimidazol-1-yl) methyl]benzoic acid is exemplified. n COPYRIGHT: (C)1992,JPO |