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24 条记录 (耗时 0.024 秒)

    Benzimidazole derivatives, preparation and therapeutic use thereof
    13.
    发明授权
    Benzimidazole derivatives, preparation and therapeutic use thereof 失效
    苯并咪唑衍生物，其制备和治疗用途

    公开(公告)号：US06794382B2

    公开(公告)日：2004-09-21

    申请号：US10343467

    申请日：2003-01-30

    申请人： Francis Barth ,  Daniel Bichon ,  Frank Bolkenius ,  Viviane Van Dorsselaer

    发明人： Francis Barth ,  Daniel Bichon ,  Frank Bolkenius ,  Viviane Van Dorsselaer

    IPC分类号： C07D47106

    CPC分类号： C07D471/06 ,  C07D487/06

    摘要： 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.

    摘要翻译： 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。

    Preparation of fluorinated methyl aminoalkanoic acids and novel process intermediates
    20.
    发明授权
    Preparation of fluorinated methyl aminoalkanoic acids and novel process intermediates 失效
    氟化甲基氨基链烷酸的制备和新工艺中间体

    公开(公告)号：US4353828A

    公开(公告)日：1982-10-12

    申请号：US170395

    申请日：1980-07-21

    申请人： Philippe Bey ,  Fritz Gerhart ,  Viviane Van Dorsselaer

    发明人： Philippe Bey ,  Fritz Gerhart ,  Viviane Van Dorsselaer

    IPC分类号： C07F3/02 ,  C07C87/26 ,  C07D209/48

    CPC分类号： C07F3/02 ,  Y02P20/55

    摘要： Fluorinated alkenylamines of the Formula V ##STR1## wherein n represents 0, 1, 2 or 3; R.sub.1 represents hydrogen or C.sub.1 -C.sub.10 alkyl and Y represents (a), when n represents O, CH.sub.2 F, (b), when n represents 1, CH.sub.2 F or CHF.sub.2, or (c) when n represents 2 or 3, CH.sub.2 F, CHF.sub.2 or CF.sub.3 are novel process intermediates. They are obtained by hydrolysis and subsequent reduction of the corresponding alkenyl fluorinated methyl ketimine magnesium halides, which are novel compounds resulting from reaction of the corresponding alkenyl magnesium halides with the corresponding fluorinated acetonitriles. The fluorinated alkenylamines of Formula V are oxidized while the amino group is protected to provide, after removal of the amine protecting group, the corresponding fluorinated methyl aminoalkanoic acids which are useful pharmacological or anti-bacterial agents.

    摘要翻译： 式V的氟化烯基胺其中n表示0,1,2或3; R1表示氢或C1-C10烷基，Y表示（a），当n表示O，CH2F，（b）时，当n表示1时，CH2F或CHF2，或（c）当n表示2或3时，CH2F，CHF2或 CF3是新型工艺中间体。 它们通过水解和随后还原相应的烯基氟代甲基酮亚胺卤化镁得到，其是由相应的烯基卤化镁与相应的氟化乙腈反应得到的新化合物。 式V的氟化链烯基胺被氧化，同时保护氨基以除去胺保护基之后提供相应的氟化甲基氨基链烷酸，其是有用的药理学或抗菌剂。