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    1-carba-(dethia)-cephalosporin derivatives
    2.
    发明授权
    1-carba-(dethia)-cephalosporin derivatives 失效
    1-卡巴（dethia） - 头孢菌素衍生物

    公开(公告)号：US5939410A

    公开(公告)日：1999-08-17

    申请号：US929248

    申请日：1997-09-10

    申请人： Peter Angehrn ,  Paul Hebeisen ,  Ingrid Heinze-Krauss ,  Malcolm Page

    发明人： Peter Angehrn ,  Paul Hebeisen ,  Ingrid Heinze-Krauss ,  Malcolm Page

    IPC分类号： C07D463/14 ,  A61K31/435 ,  A61K31/4353 ,  A61K31/445 ,  A61K31/4545 ,  A61P31/04 ,  C07D463/00

    CPC分类号： C07D463/22 ,  Y02P20/55

    摘要： Compounds of formula I whereinR.sup.1 is hydrogen, lower alkyl which is unsubstituted or substituted by fluoro, aralkyl, cycloalkyl, --COR.sup.4 or --C(R.sup.5 R.sup.6)CO.sub.2 R.sup.7 --C(R.sup.5 R.sup.6)CONHR.sup.7 ; where R.sup.5 and R.sup.6 are each independently hydrogen or lower alkyl, or R.sup.5 and R.sup.6 taken together form a cycloalkyl group; R.sup.4 is hydrogen or lower alkyl and R.sup.7 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group;R.sup.2 is hydrogen, hydroxy, lower alkyl-Q.sub.m, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl-Q.sub.m, aryl-Q.sub.m, aryloxy, aralkoxy, a heterocyclic ring or heterocyclyl lower alkyl, the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl, aryl, aryloxy, aralkoxy and the heterocyclic ring being unsubstituted or substituted with at least one group selected from carboxy, amino, nitro, cyano, lower alkyl which is unsubstituted or substituted by fluoro, lower alkoxy, hydroxy, halogen, --COR.sup.6, --C(R.sup.5 R.sup.6)CO.sub.2 R.sup.7, --C(R.sup.5 R.sup.6)CONR.sup.5 R.sup.8, --CONR.sup.5 R.sup.6, --N(R.sup.6)COOR.sup.10, R.sup.6 OCO-- or R.sup.6 COO-- where R.sup.5 and R.sup.6 are hydrogen or lower alkyl; R.sup.7 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group; R.sup.8 is hydrogen, lower alkyl or phenyl which is unsubstituted or substituted with at least one halogen, hydroxy, amino, lower alkyl, or lower alkoxy; R.sup.10 is lower alkyl, lower alkenyl or a carboxylic acid protecting group;Q is --CHR--, --CO-- or --SO.sub.2 --;R is hydrogen or lower alkyl;R.sup.3 is hydroxy, --O--, lower alkoxy, --OM and M represents an alkali metal;m is 0 or 1;n is 0, 1 or 2;x is CH or Nas well as readily hydrolysable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts are provided. These compounds have valuable antiinfective properties.

    摘要翻译： 式I化合物，其中R 1是氢，未被取代或被氟取代的低级烷基，芳烷基，环烷基，-COR 4或-C（R 5 R 6）CO 2 R 7 -C（R 5 R 6）CONHR 7; 其中R 5和R 6各自独立地为氢或低级烷基，或者R 5和R 6一起形成环烷基; R4是氢或低级烷基，R7是氢，低级烷基，低级烯基或羧酸保护基; R2是氢，羟基，低级烷基-Qm，环烷基，低级烷氧基，低级烯基，环烯基，低级炔基，芳烷基-Qm，芳基-Qm，芳氧基，芳烷氧基，杂环或杂环基低级烷基，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，杂环是未取代的或被至少一个选自羧基，氨基，硝基，氰基，未被取代或被氟取代的低级烷基 ，低级烷氧基，羟基，卤素，-COR6，-C（R5R6）CO2R7，-C（R5R6）CONR5R8，-CONR5R6，-N（R6）COOR10，R6OCO-或R6COO-，其中R5和R6是氢或低级烷基; R7是氢，低级烷基，低级烯基或羧酸保护基; R8是氢，低级烷基或未取代的或被至少一个卤素，羟基，氨基，低级烷基或低级烷氧基取代的苯基; R 10为低级烷基，低级烯基或羧酸保护基; Q是-CHR-，-CO-或-SO 2 - ; R是氢或低级烷基; R3是羟基，-O-，低级烷氧基，-OM，M代表碱金属; m为0或1; n为0,1或2; x是CH或N，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。 这些化合物具有有价值的抗感染性。

    Cephalosporin pyridinium derivatives
    4.
    发明授权
    Cephalosporin pyridinium derivatives 失效
    头孢菌素吡啶衍生物

    公开(公告)号：US5935950A

    公开(公告)日：1999-08-10

    申请号：US924626

    申请日：1997-09-05

    申请人： Peter Angehrn ,  Ingrid Heinze-Krauss ,  Malcolm Page ,  Urs Weiss

    发明人： Peter Angehrn ,  Ingrid Heinze-Krauss ,  Malcolm Page ,  Urs Weiss

    IPC分类号： C07D501/04 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/16 ,  C07D501/24 ,  C07D501/56

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： Compounds of formula I ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, cycloalkyl or acetyl;x is CH or N;n is 0, 1 or 2;m is 0 or 1;R.sup.2 is hydrogen, lower alkyl, .omega.-hydroxy alkyl, benzyl or lower alkyl-heterocyclyl, the benzyl and the heterocyclyl group being unsubstituted or substituted with at least one of the groups amino, cyano, carboxy, halogen, hydroxy, lower alkyl, lower alkoxy or --CONR.sub.2, where R is hydrogen or lower alkyl; or R.sup.2 is --CH.sub.2 CONR.sup.4 R.sup.5 ; whereinR.sup.4, R.sup.5 are each independently hydrogen, .omega.-hydroxy-alkyl, phenyl, benzyl, naphthyl or heterocyclyl, the phenyl, benzyl, naphthyl or heterocyclyl groups being unsubstituted or substituted with at least one of the groups optionally protected hydroxy, halogen, optionally substituted lower alkyl, optionally substituted lower alkoxy, .omega.-hydroxyalkyl or cyano; or R.sup.4 and R.sup.5 form together a group of formula ##STR2## with the proviso that when pyridinium ring A is pyridinium-4-yl, m is 1; as well as readily hydrolysable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts. These compounds are useful as parenteral antibiotics.

    摘要翻译： 其中R1是氢，低级烷基，环烷基或乙酰基的式Ⅰ化合物; x是CH或N; n为0,1或2; m为0或1; R2是氢，低级烷基，ω-羟基烷基，苄基或低级烷基 - 杂环基，苄基和杂环基是未取代的或被至少一个氨基，氰基，羧基，卤素，羟基，低级烷基，低级 烷氧基或-CONR2，其中R是氢或低级烷基; 或R 2为-CH 2 CONR 4 R 5; 其中R 4，R 5各自独立地为氢，ω-羟基 - 烷基，苯基，苄基，萘基或杂环基，苯基，苄基，萘基或杂环基为未取代的或被至少一个选自羟基，卤素， 取代的低级烷基，任选取代的低级烷氧基，ω-羟烷基或氰基; 或R 4和R 5一起形成式的基团，条件是当吡啶鎓环A为吡啶鎓-4-基时，m为1; 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。 这些化合物可用作胃肠外抗生素。