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    Vinylpyrrolidinon cephalosporin derivatives
    4.
    发明公开
    Vinylpyrrolidinon cephalosporin derivatives 失效
    Vinylpyrrolidinon头孢衍

    公开(公告)号：EP0841339A1

    公开(公告)日：1998-05-13

    申请号：EP97118780.2

    申请日：1997-10-29

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： Angehrn, Peter ,  Heinze-Krauss, Ingrid ,  Richter, Hans G.F.

    IPC分类号： C07D501/48 ,  C07D501/50 ,  C07D501/52 ,  C07D501/56 ,  A61K31/545

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： The present invention relates to cephalosporin derivatives of the general formula
    where

    R 1 is halogen, lower alkyl, phenyl, benzyl, styryl, naphthyl or heterocyclyl; the lower alkyl, phenyl, benzyl, styryl, naphthyl and heterocyclyl being optionally substituted by at least one of halogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkoxy, optionally substituted phenyl, amino, lower alkylamino, di-lower alkylamino, carboxy, lower alkylcarboxy, carbamoyl or lower alkylcarbamoyl;
    R 4 , R 5 independently are hydrogen, lower alkyl or phenyl;
    X is S, O, NH or CH 2 ;
    n is 0,1 or 2;
    m is 0 or 1;
    s is 0 or 1;
    R 2 is hydrogen, hydroxy, -CH 2 -CONHR 6 , lower alkyl-Q r , cycloalkyl-Q r , lower alkoxy, lower alkenyl, cycloalkenyl-Q r , lower alkynyl, aralkyl-Q r , aryl-Q r , aryloxy, aralkoxy, a heterocyclic ring or a heterocyclyl-Q r , the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl, aryl, aryloxy, aralkoxy and the heterocyclic ring may be substituted with at least one group selected from carboxy, amino, nitro, cyano, -SO 2 NHR 6 , optionally fluoro substituted lower alkyl, lower alkoxy, hydroxy, halogen, -CONR 6 R 7 , -CH 2 CONR 6 R 7 , -N(R 7 )COOR 8 , R 7 CO-, R 7 OCO-, R 7 COO-, -C(R 7 R 9 )CO 2 R 8 , -C(R 7 R 9 )CONR 7 R 10 , wherein

    R 6 is hydrogen, lower alkyl, cycloalkyl or aryl;
    R 7 and R 9 are independently hydrogen or lower alkyl;
    R 8 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group; and
    R 10 is hydrogen, ω-hydroxy-alkyl, phenyl, naphthyl or heterocyclyl, the phenyl, naphthyl or heterocyclyl being unsubstituted or substituted with at least one of the groups of optionally protected hydroxy, halogen, optionally substituted lower alkyl or ω-hydroxyalkyl, optionally substituted lower alkoxy and/or cyano, or R 7 and R 10 form together group of formula


    Q is -CHR-, -CO- or -SO 2 -;
    r is 0 or 1;
    R is hydrogen or lower alkyl; and
    R 3 is hydroxy, -O - , lower-alkoxy, or -OM and M represents an alkali metal;
    as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts, as wen as the preparation of such compounds, their use for the treatment of infectious diseases and pharmaceutical preparations containing such compounds.

    摘要翻译： 本发明涉及通式为CHEM的头孢菌素衍生物，其中R 1为卤素，低级烷基，苯基，苄基，苯乙烯基，萘基或杂环基; 羟基，任选取代的低级烷基，任选取代的低级烷氧基，任选取代的苯基，氨基，低级烷基氨基，二低级烷基氨基，羧基，低级烷基，低级烷基氨基， ，低级烷基羧基，氨基甲酰基或低级烷基氨基甲酰基; R 4，R 5独立地是氢，低级烷基或苯基; X是S，O，NH或CH 2; n为0,1或2; m为0或1; s为0或1; R 2是氢，羟基，-CH 2 -CONHR 6，低级烷基-Q，环烷基-Q，低级烷氧基，低级烯基，环烯基-Q，低级炔基，芳烷基-Q，芳基-Cr，芳氧基，芳烷氧基 ，杂环或杂环基-Q，低级烷基，环烷基，低级烷氧基，低级烯基，环烯基，低级炔基，芳烷基，芳基，芳氧基，芳烷氧基和杂环可以被至少一个选自羧基， 氨基，硝基，氰基，-SO 2 NHR 6，任选氟取代的低级烷基，低级烷氧基，羟基，卤素，-CONR 6 R 7，-CH 2 CONR 6 R 7， （R 7）COOR 8，R 7 CO-，R 7 OCO-，R 7 COO-，-C（R 7 R 9）CO 2 R 8，-C（R R 7 R 9）CONR 7 R 10，其中R 6是氢，低级烷基，环烷基或芳基; R 7和R 9独立地是氢或低级烷基; R 8是氢，低级烷基，低级烯基或羧酸保护基; R 10是氢，ω-羟基 - 烷基，苯基，萘基或杂环基，苯基，萘基或杂环基是未取代的或被至少一个任选被保护的羟基，卤素，任选取代的低级烷基或ω- - 羟烷基，任选取代的低级烷氧基和/或氰基，或R 7和R 10一起形成式CHEM的基团是-CHR-， - CO-或-SO 2 - ; r为0或1; R是氢或低级烷基; R 3为羟基，-O - ， - 低级烷氧基或-OM，M为碱金属; 以及其易水解的酯，所述化合物的药学上可接受的盐和式I化合物的水合物及其酯和盐，作为这些化合物的制备，其用于治疗感染性疾病的药物和含有 这样的化合物。