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    • 41. 发明授权
    • Benzimidazoles and pharmaceutical compositions containing them
    • 苯并咪唑和含有它们的药物组合物
    • US5565469A
    • 1996-10-15
    • US402744
    • 1995-03-13
    • Gerhard MihmNorbert HauelUwe RiesJacobus C. Antonius van MeelWolfgang WienenMichael Entzeroth
    • Gerhard MihmNorbert HauelUwe RiesJacobus C. Antonius van MeelWolfgang WienenMichael Entzeroth
    • C07D235/20A61K31/415A61K31/4184A61K31/425A61K31/435A61P9/00A61P9/10A61P9/12A61P43/00C07D235/18C07D235/26C07D235/28C07D403/04C07D403/14C07D413/04C07D413/14C07D417/04C07D417/14C07D471/04
    • C07D413/14C07D235/18C07D417/04C07D417/14C07D471/04
    • Angiotensin-II inhibiting benzimidazoles, useful for the treatment of hypertension. Exemplary compounds are:(a) 4'-[(2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl)-methyl]-2-(1,3-thiazolidin-2,4-dione-5-methylidinyl)-biphenyl,(b) 4'-[(2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl)-methyl]-2-sulpho-biphenyl,(c) 4'-[(2-ethyl-4-methyl-6-(5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl)-benzimidazol-1-yl)-methyl]-2-sulpho-biphenyl,(d) 4'-[(2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl)-methyl]-2-trifluoroacetylamino-biphenyl,(e) 4'-[(2-ethyl-4-methyl-6-(5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl)-benzimidazol-1-yl)-methyl]-2-trifluoroacetylamino-biphenyl,(f) 4'-[(2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl)-methyl]-2-(4-methoxy-benzylaminocarbonylaminosulphonyl)-biphenyl,(g) 4'-[(2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl)-methyl]-2-(cyclohexylamino-carbonylaminosulphonyl)-biphenyl,(h) 4'-[(2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazol-1-yl)-methyl]-2-(benzoylamino-sulphonyl)-biphenyl,(i) 4'-[(2-ethyl-4-methyl-6-(5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl)-benzimidazol-1-yl)-methyl]-2-(benzoylaminosulphfonyl)-biphenyl,(j) 4'-[(2-n-butyl-4-methyl-6-(propanesultam-1-yl)-benzimidazol-1-yl)-methyl]-2-(benzoylaminosulphonyl)-biphenyl and(k) 4'-[(2-ethyl-4-methyl-6-(5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl)-benzimidazol-1-yl)-methyl]-2-(cyclohexylaminocarbonylaminosulphonyl)-biphenyl.
    • 血管紧张素II抑制苯并咪唑,可用于治疗高血压。 示例性化合物是:(a)4' - [(2-正丙基-4-甲基-6-(1-甲基苯并咪唑-2-基) - 苯并咪唑-1-基) - 甲基] -2-(1,3 - 联苯并联,(b)4' - [(2-正丙基-4-甲基-6-(1-甲基苯并咪唑-2-基) - 苯并咪唑-1-基] (c)4' - [(2-乙基-4-甲基-6-(5,6,7,8-四氢 - 咪唑并[1,2-a]吡啶 -2-基) - 苯并咪唑-1-基) - 甲基] -2-磺基 - 联苯,(d)4' - [(2-正丙基-4-甲基-6-(1-甲基苯并咪唑-2-基) ) - 苯并咪唑-1-基) - 甲基] -2-三氟乙酰基氨基 - 联苯,(e)4' - [(2-乙基-4-甲基-6-(5,6,7,8-四氢 - 咪唑并[1 ,2-a]吡啶-2-基) - 苯并咪唑-1-基) - 甲基] -2-三氟乙酰基氨基 - 联苯,(f)4' - [(2-正丙基-4-甲基-6- - 甲基苯并咪唑-2-基) - 苯并咪唑-1-基) - 甲基] -2-(4-甲氧基 - 苄基氨基羰基氨基磺酰基) - 联苯,(g)4' - [(2-正丙基-4-甲基-6- (1-甲基苯并咪唑-2-基) - 苯并咪唑-1-基) - 甲基] -2-(环己基氨基 - 羰基氨基磺酰基) - 联苯,(h)4' - [(2-正丙基-4-甲基-6- (1-甲基苯并咪唑-2-基) - 苯并咪唑 (甲基)-2-(苯甲酰氨基磺酰基) - 联苯,(i)4' - [(2-乙基-4-甲基-6-(5,6,7,8-四氢 - 咪唑并[ [1,2-a]吡啶-2-基) - 苯并咪唑-1-基) - 甲基] -2-(苯甲酰氨基磺酰基) - 联苯,(j)4' - [(2-正丁基-4-甲基 - 6-(丙磺酰基-1-基) - 苯并咪唑-1-基) - 甲基] -2-(苯甲酰基氨基磺酰基) - 联苯和(k)4' - [(2-乙基-4-甲基-6- ,7,8-四氢 - 咪唑并[1,2-a]吡啶-2-基) - 苯并咪唑-1-基) - 甲基] -2-(环己基氨基羰基氨基磺酰基) - 联苯。