发明公开
- 专利标题： 1-Carba-(dethia)-Cephalosporin Derivatives
- 专利标题（中）： 1-Carba-（dethia） - 头孢菌素衍生物
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申请号： EP97116236.7申请日： 1997-09-18
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公开(公告)号： EP0831093A1公开(公告)日： 1998-03-25
- 发明人: Angehrn, Peter , Hebeisen, Paul , Heinze-Krauss, Ingrid , Page, Malcolm
- 申请人： F. HOFFMANN-LA ROCHE AG
- 申请人地址： 4070 Basel CH
- 专利权人： F. HOFFMANN-LA ROCHE AG
- 当前专利权人： F. HOFFMANN-LA ROCHE AG
- 当前专利权人地址： 4070 Basel CH
- 代理机构： Kjellsaa-Berger, Hanny, Dr.
- 优先权： EP96115210 19960923
- 主分类号： C07D463/00
- IPC分类号： C07D463/00 ; A61K31/545
摘要：
1-carba-(dethia)-cephalosporin derivatives of the general formula I
wherein
R 1 is hydrogen, optionally fluoro substituted lower alkyl, aralkyl, cycloalkyl, -COR 4 or -C(R 5 R 6 )CO 2 R 7 -C(R 5 R 6 )CONHR 7 ; where R 5 and R 6 are each independently hydrogen or lower alkyl, or R 5 and R 6 taken together form a cycloalkyl group; R 4 is hydrogen or lower alkyl and R 7 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group;
R 2 is hydrogen, hydroxy, lower alkyl-Q m , cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl-Q m , aryl-Q 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, optionally fluoro substituted lower alkyl, lower alkoxy, hydroxy, halogen, -COR 6 , -C(R 5 R 6 )CO 2 R 7 , -C(R 5 R 6 )CONR 5 R 8 , -CONR 5 R 6 , -N(R 6 )COOR 10 , R 6 OCO- or R 6 COO- where R 5 and R 6 are hydrogen or lower alkyl; R 7 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group; R 8 is hydrogen, lower alkyl or optionally substituted phenyl; R 10 is lower alkyl, lower alkenyl or a carboxylic acid protecting group;
Q is -CHR-, -CO- or -SO 2 -;
R is hydrogen or lower alkyl
R 3 is hydroxy, lower-alkoxy, or -O - , when R 2 has a positive charge, or -OM and M represents an alkali metal;
m is 0 or 1;
n is 0, 1 or 2;
X is CH or N
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.
wherein
R 1 is hydrogen, optionally fluoro substituted lower alkyl, aralkyl, cycloalkyl, -COR 4 or -C(R 5 R 6 )CO 2 R 7 -C(R 5 R 6 )CONHR 7 ; where R 5 and R 6 are each independently hydrogen or lower alkyl, or R 5 and R 6 taken together form a cycloalkyl group; R 4 is hydrogen or lower alkyl and R 7 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group;
R 2 is hydrogen, hydroxy, lower alkyl-Q m , cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl-Q m , aryl-Q 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, optionally fluoro substituted lower alkyl, lower alkoxy, hydroxy, halogen, -COR 6 , -C(R 5 R 6 )CO 2 R 7 , -C(R 5 R 6 )CONR 5 R 8 , -CONR 5 R 6 , -N(R 6 )COOR 10 , R 6 OCO- or R 6 COO- where R 5 and R 6 are hydrogen or lower alkyl; R 7 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group; R 8 is hydrogen, lower alkyl or optionally substituted phenyl; R 10 is lower alkyl, lower alkenyl or a carboxylic acid protecting group;
Q is -CHR-, -CO- or -SO 2 -;
R is hydrogen or lower alkyl
R 3 is hydroxy, lower-alkoxy, or -O - , when R 2 has a positive charge, or -OM and M represents an alkali metal;
m is 0 or 1;
n is 0, 1 or 2;
X is CH or N
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.
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