Patent ID: 6242445
Filing Date: 2001-06-05
Classification: C07D

Abstract:
A benzimidazole derivative of the general formula (I): ##STR13##wherein A is --O-- or --NH--;R.sup.1 is an aliphatic hydrocarbon group having 1 to 8 carbon atoms, or an aliphatic hydrocarbon group having 1 to 8 carbon atoms which is substituted with one or more halogen atoms;R.sup.2 is --OH, --OR.sup.10, --NHR.sup.11, --NR.sup.12 R.sup.13, or --NH.sub.2, or a three- to seven-membered saturated cycloaliphatic amino group which may be optionally interrupted by one or more nitrogen, oxygen, or sulfur atoms, or a three- to seven-membered saturated cycloaliphatic hydrocarbon group containing at least one nitrogen atom in the ring which is substituted with one or more aliphatic hydrocarbon groups having 1 to 8 carbon atoms, or a three- to seven-membered saturated cycloaliphatic hydrocarbon group containing at least one nitrogen atom in the ring which is substituted with one or more aliphatic hydrocarbon groups having 1 to 8 carbon atoms which is substituted with one or more halogen atoms;R.sup.3 is --COOH, --COOR.sup.4, or --OH;R.sup.4 is an aliphatic hydrocarbon group having 1 to 8 carbon atoms, an aliphatic hydrocarbon group having 1 to 8 carbon atoms which is substituted with one or more halogen atoms, --(CH.sub.2).sub.m NR.sup.14 R.sup.15, --(CH.sub.2).sub.n R.sup.5, --(CH.sub.2).sub.p CH(NR.sup.16 R.sup.17)COOR.sup.18, --R'--COOR.sup.19, --CH(R.sup.20)OC(.dbd.O)R.sup.7, or --CH(R.sup.21)OC(.dbd.O)OR.sup.8 ;R.sup.5 is a three- to seven-membered saturated cycloaliphatic amino group which may be optionally interrupted by one or more nitrogen, oxygen, or sulfur atoms, or a three- to seven-membered saturated cycloaliphatic hydrocarbon group containing at least one nitrogen atom in the ring which is substituted with one or more aliphatic hydrocarbon groups having 1 to 8 carbon atoms, or a three- to seven-membered saturated cycloaliphatic hydrocarbon group containing at least one nitrogen atom in the ring which is substituted with one or more aliphatic hydrocarbon groups having 1 to 8 carbon atoms which is substituted with one or more halogen atoms, or a three- to seven-membered unsaturated heterocyclic group;R.sup.6 is a three- to seven-membered saturated cycloaliphatic hydrocarbon group containing at least one nitrogen atom in the ring which may be optionally substituted with one or more aliphatic hydrocarbon groups having 1 to 8 carbon atoms, or a three- to seven-membered saturated cycloaliphatic hydrocarbon group containing at least one nitrogen atom in the ring which may be optionally substituted with one or more aliphatic hydrocarbon groups having 1 to 8 carbon atoms which is substituted with one or more halogen atoms;R.sup.7 and R.sup.8 are --(CH.sub.2).sub.r R.sup.9 ;R.sup.9 is a hydrogen atom, an aliphatic hydrocarbon group having 1 to 8 carbon atoms, an aliphatic hydrocarbon group having 1 to 8 carbon atoms which is substituted with one or more halogen atoms, or --NR.sup.22 R.sup.23 ;R.sup.10, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.22, and R.sup.23 are independently an aliphatic hydrocarbon group having 1 to 8 carbon atoms, or an aliphatic hydrocarbon group having 1 to 8 carbon atoms which is substituted with one or more halogen atoms;R.sup.20 and R.sup.21 are a hydrogen atom, an aliphatic hydrocarbon group having 1 to 8 carbon atoms, or an aliphatic hydrocarbon group having 1 to 8 carbon atoms which is substituted with one or more halogen atoms; and m, n, p, and r are 0 or an integer of 1 to 6, or a salt thereof.