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    Benzimidazole derivative compounds and method of making
    5.
    发明授权
    Benzimidazole derivative compounds and method of making 失效
    苯并咪唑衍生物及其制备方法

    公开(公告)号：US4950677A

    公开(公告)日：1990-08-21

    申请号：US222593

    申请日：1988-07-21

    申请人： Albert Fischli ,  Anna Krasso ,  Andre Szente

    发明人： Albert Fischli ,  Anna Krasso ,  Andre Szente

    IPC分类号： C07D401/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/044 ,  C07D495/04

    CPC分类号： C07D401/04

    摘要： A compound of the formula ##STR1## wherein R.sup.1 -R.sup.19 are as described in the specification. The present invention is concerned with benzimidazole derivatives, particularly benzimidazole-2-yl pyridinium compounds of formula I which are pharmaceutically useful in treating or preventing gastric and duodenal ulcers. The invention includes the compounds I, pharmaceutical compositions containing such compounds and the use of such compounds in therapeutic treatment or prevention of gastric and duodenal ulcers.

    摘要翻译： 其中R1-R19如说明书中所述的式（Ⅰ）化合物。 本发明涉及可用于治疗或预防胃和十二指肠溃疡的苯并咪唑衍生物，特别是式I的苯并咪唑-2-基吡啶鎓化合物。 本发明包括化合物I，含有这些化合物的药物组合物以及这些化合物在治疗性或预防胃和十二指肠溃疡中的用途。

    (Bezimidazol-2-yl)-pyridinium compounds
    7.
    发明授权
    (Bezimidazol-2-yl)-pyridinium compounds 失效

    公开(公告)号：US4766133A

    公开(公告)日：1988-08-23

    申请号：US893856

    申请日：1986-08-06

    申请人： Albert Fischli ,  Anna Krasso ,  Andre Szente

    发明人： Albert Fischli ,  Anna Krasso ,  Andre Szente

    IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D473/38 ,  C07D491/04 ,  A61K31/44

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D473/38 ,  C07D491/04

    摘要： (Benzimidazol-2-yl)-pyridinium compounds of the formula ##STR1## wherein A is --SR.sup.9, --SO.sub.3.sup.- or --S--SO.sub.3.sup.- ; R.sup.1 and R.sup.3 each is hydrogen or (C.sub.1 -C.sub.7)-alkyl; R.sup.2 is hydrogen, (C.sub.1 -C.sub.7)-alkyl, (C.sub.1 -C.sub.7)-alkoxy or a negatively charged oxygen atom; R.sup.4 is hydrogen or a negative charge; R.sup.5, R.sup.6, R.sup.7 and R.sup.8 each is hydrogen, (C.sub.1 -C.sub.7)-alkyl, aryl, halogen, cyano, nitro, formyl, (C.sub.2 -C.sub.7)-alkanoyl, arylcarbonyl, carboxy, carboxy-(C.sub.1 -C.sub.7)-alkyl, (C.sub.1 -C.sub.7)-alkoxycarbonyl, aryloxycarbonyl, aryl-(C.sub.1 -C.sub.7)-alkoxycarbonyl, (C.sub.1 -C.sub.7)-alkoxycarbonyl-(C.sub.1 -C.sub.7)-alkyl, carbamoyl, mono- or di-(C.sub.1 -C.sub.7)-alkylcarbamoyl, pyrrolidinocarbonyl, piperidinocarbonyl, carbamoyl-(C.sub.1 -C.sub.7)-alkyl, mono- or di-(C.sub.1 -C.sub.7)-alkylcarbamoyl-(C.sub.1 -C.sub.7)-alkyl, pyrrolidinocarbonyl-(C.sub.1 -C.sub.7)-alkyl, piperdinocarbonyl-(C.sub.1 -C.sub.7)-alkyl, hydroxy, (C.sub.1 -C.sub.7)-alkoxy, (C.sub.2 -C.sub.7)-alkanoloxy, aryloxy, arylcarbonyloxy, (C.sub.1 -C.sub.7)-alkoxycarbonyloxy, aryl-(C.sub.1 -C.sub.7)-alkoxycarbonyloxy, aryloxycarbonyloxy, carbamoyloxy, mono- or di-(C.sub.1 -C.sub.7)-alkylcarbamoyloxy, pyrrolidinocarbonyloxy, piperidinocarbonyloxy, hydroxy-(C.sub.1 -C.sub.7)-alkyl, trifluoromethyl, di-(C.sub.1 -C.sub.7)-alkoxymethyl or (C.sub.2 -C.sub.3)-alkylenedioxymethyl or two of these substituents which are adjacent jointly and together with the carbon atoms to which they are attached are a 5-, 6- or 7-membered ring; and R.sup.9 is (C.sub.1 -C.sub.20)-alkyl, (C.sub.3 -C.sub.7)-cycloalkyl, (C.sub.3 -C.sub.7)-alkenylalkyl, (C.sub.3 -C.sub.7)-alkynylalkyl, substituted (C.sub.3 -C.sub.7)- alkenyl-alkyl, aryl, aryl-(C.sub.1 -C.sub.7)-alkyl, hydroxy- (C.sub.2 -C.sub.7)-alkyl, (C.sub.1 -C.sub.7)-alkoxy- (C.sub.2 -C.sub.7)-alkyl, (C.sub.1 -C.sub.7)-alkoxycarbonyl- (C.sub.1 -C.sub.7)-alkyl, carboxy-(C.sub.1 -C.sub.7)-alkyl, di-(C.sub.1 -C.sub.7)-alkoxycarbonyl-(C.sub.2 -C.sub.7)-alkyl, dicarboxy-(C.sub.2 -C.sub.7)-alkyl, carboxy-(C.sub.1 -C.sub.7)-alkylcarbamoyl-(C.sub.1 -C.sub.7)-alkyl, optionally N-substituted amino-(C.sub.2 -C.sub.7)-alkyl, optionally N-substituted amino-carboxy-(C.sub.2 -C.sub.7)-alkyl, optionally N-substituted amino-(C.sub.1 -C.sub.7)-alkoxycarbonyl-(C.sub.2 -C.sub.7)-alkyl, heteroaryl, heteroaryl-(C.sub.1 -C.sub.7)-alkyl or a residue derived from a cysteine-containing oligopeptide by elimination of the SH group;provided that when there is a net single positive charge there is an external anion, or a pharmaceutically acceptable acid addition salt thereof.