1-Benzyl-benzimidazole cpds. as angiotensin II antagonists - for treating hypertonia, coronary insufficiency, angina, gastrointestinal and bladder disorders etc.

摘要

Substd. 1-benzylimidazole derivs. of formula (I), their mixts. of positional isomers, and their addn. salts with (in)organic acids or bases are new, where A = CO, NHCO or CONH; R1 = opt. branched 3-5C alkyl or alkenyl; R2 and R3 = each H if R4 = 2-sulphophenyl or 2-phosphonooxyphenyl in which one OH gp. is opt. replaced with 1-3C alkoxy; or R2 = H if R3 = alkoxycarbonylamino contg. 2-4C, 1-6C alkanoylamino or (5-7C cycloalkyl) (1-3C)alkanoylamino, (these last 2 gps. opt. substd. on N alkyl), phthalimido which is opt. partially or completely hydrogenated on the benzene ring or R7-NR6-CO-NR5; or R1 = 1-3C alkyl in position 4 if R3 = OH opt. substd. with (5-7C cycloalkyl) (1-3C) alkyl or phenyl (1-3C)-alkyl; R4 = Ph (opt. substd. in position 2 with carboxy, benzyloxycarbonyl or alkoxycarbonyl contg. a total of 2-5C, or opt. mono- or di-substd. by Cl, Br, 1-3C alkyl or 1-3C alkoxy), pyridyl (substd. in the position ortho to A with carboxy, benzyloxycarbonyl or alkoxycarbonyl contg. a total of 2-5C), cyclohexyl (substd. in 2-position with carboxy, benzyloxycarbonyl or alkoxycarbonyl contg. a total of 2-5C), 2-sulphophenyl or 2-phosphonoxyphenyl in which the OH gp. is opt. replaced with 1-3C alkoxyl; R5 = H or 1-6C alkyl; R6 = H, 1-6C alkyl or 5-7C cycloalkyl; R7 = H or 1-6C alkyl; or R6 and R7 together with the N to which they are attached forms a linear 4-6C alkyleneimino gp.; or R5 and R6 together form 2-4C alkylene. USE/ADVANTAGE - (I) are angiontensin II antagonists and can be used to treat hypertomia, cardiac insufficiency, ischaemic peripheral circulatory disorders, or myocardial ischaemia (Angina).