PURPOSE: To provide substituted indoles and benzimidazole derivatives which inhibit angiotensin II activity and are useful as agents for treating and preventing hypertension, congestive heart failures, cardiac hypertrophy or the like.
CONSTITUTION: The compounds of formula I or their isomers expressed by formula II, for instance, 2-butyl-3-[[4-[2-(2H-tetrazol-5-yl)-1H-indol-1- yl]phenyl]methyl]-4(3H)-quinazolinone are provided. In the formula I, X is N, a CR'6; R1 is an alkyl, alkenyl, alkynyl, cycloalkyl, NR11R12, substitutable benzyl, OR15, SR15 or the like; R2 is a halogen, CN, OR15, SR15 or the like; R3 is CN, NO2, CONR11R12, (R15OCO)alkyl or the like; R4, R5 are each H, an alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocyclo or the like; R6, R'6 are each H, an alkyl, aryl, cycloalkyl, SO3H, PO3H, CO2R8 or the like; R7 is H, a CO2R8, SO3H, PO3H or the like; R8 is H, an alkyl, phenyl or the like; R11, R12 are each H, an alkyl, benzyl or the like; R15 is an alkyl, aryl, heterocyclo or the like.
KAANEIRU ESU ATOWARU
