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    • 31. 发明授权
    • Benzimidazole derivatives, preparation and therapeutic use thereof
    • 苯并咪唑衍生物,其制备和治疗用途
    • US06794382B2
    • 2004-09-21
    • US10343467
    • 2003-01-30
    • Francis BarthDaniel BichonFrank BolkeniusViviane Van Dorsselaer
    • Francis BarthDaniel BichonFrank BolkeniusViviane Van Dorsselaer
    • C07D47106
    • C07D471/06C07D487/06
    • The invention relates to benzimidazole derivatives of general formula in which X represents a nitrogen atom or a carbon atom; and when X represents a nitrogen atom: R3 represents a hydrogen atom or a C1-C4 alkyl group, or does not exist, to give the compounds of formula (I) comprising a secondary or tertiary amine; R4 represents a hydrogen atom or a C1-C6 alkyl, C3-C7 cycloalkyl, optionally substituted C3-C7 heterocycloalkyl, —(CH2)p-heteroaryl, heteroaryl-carbonyl, phenylcarbonyl, (C1-C6)alkylcarbonyl, —(CH2)pCOOR, optionally substituted phenylsulphonyl or optionally substituted —(CH2)p-phenyl group, and, when X represents a carbon atom: R3 represents a hydrogen atom or a group —NR5R6, —N(R5)3+, —NHCOR7, —CONHR5, —COR7, —NHCONH2, —OH or —CH2OH, R4 represents a hydrogen atom or an optionally substituted —(CH2)p-phenyl, —(CH2)p-heteroaryl or —(CH2)tNR7R8 group. Preparation process and therapeutic application.
    • 本发明涉及X表示氮原子或碳原子的一般结构式的苯并咪唑衍生物,当X表示氮原子时:R 3表示氢原子或C 1 -C 4烷基,或不存在,得到 式(I)包括仲胺或叔胺; R 4表示氢原子或C 1 -C 6烷基,C 3 -C 7环烷基,任选取代的C 3 -C 7杂环烷基, - (CH 2)p - 杂芳基,杂芳基 - 羰基,苯基羰基,( C 1 -C 6)烷基羰基, - (CH 2)p COOR,任选取代的苯基磺酰基或任选取代的 - (CH 2)对苯基,并且当X表示碳原子时:R 3表示氢原子或-NR 5 R 6基,-N( R5)3 +,-NHCOR7,-CONHR5,-COR7,-NHCONH2,-OH或-CH2OH,R4表示氢原子或任选取代的 - (CH 2)p - 苯基, - (CH 2)p - - (CH2)tNR7R8组。制备方法和治疗应用。