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1.发明公开Pyridinium-substituted (lactamylvinyl)cephalosporin derivatives, their preparation and their use as antibiotics 失效吡啶鎓取代物（乳酰基乙烯基） - 头孢菌素衍生物，deren Herstellung und deren Verwendung als Antibiotika
公开(公告)号：EP0838465A1
公开(公告)日：1998-04-29
申请号：EP97117810.8
申请日：1997-10-15
IPC分类号： C07D501/48 , A61K31/545
CPC分类号： C07D501/00
摘要： Cephalosporin pyridinium derivatives of the general formula I
wherein
R 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 2 is hydrogen, lower alkyl, ω-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 2 , R being hydrogen or lower alkyl; or R 2 is -CH 2 CONR 4 R 5 ; wherein
R 4 , R 5 are independently 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, optionally substituted lower alkoxy, ω-hydroxyalkyl and/or cyano; or R 4 and R 5 form together a group of formula
with the proviso that m is 1, when the pyridinium ring A is a pyridinium-4-yl;
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.摘要翻译： 通式I
的头孢菌素吡啶鎓衍生物，其中R 1是氢，低级烷基，环烷基或乙酰基; X是CH或N; n为0,1或2; m为0或1; R 2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，R为氢或低级烷基; 或R 2为-CH 2 CONR 4 R 5; 其中R 4，R 5独立地是氢，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，任选取代的低级烷氧基，ω-羟烷基和/或氰基; 或R 4和R 5一起形成式CHEM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。 -
公开(公告)号：EP0761673A1
公开(公告)日：1997-03-12
申请号：EP96113998.7
申请日：1996-09-02
发明人： Hebeisen, Paul , Stalder, Henri , Heinze-Krauss, Ingrid , Weiss, Urs , Richter, Hans , Yiannikouros, George Petros , Runtz, Valeri
IPC分类号： C07D501/48 , A61K31/545
CPC分类号： C07D501/00
摘要： The present invention relates to cephalosporin derivatives of the general formula I
wherein
R 1 is a group selected from 2-, 3- and 4-hydroxyphenyl, 2- and 3-methoxyphenyl, 4-carboxyphenyl, 4-carbamoylphenyl, 3-trifluoromethylphenyl, 2- and 3-fluorophenyl, 3-nitrophenyl, 3-fluoro-4-hydroxyphenyl, 2-fluoro-4-hydroxyphenyl, 3-fluoro-2-hydroxyphenyl, 3-, 4-dihydroxyphenyl, benzyl, -CHR-phenyl, 3-hydroxybenzyl, 4-aminobenzyl, 2-, 3- and 4-fluorobenzyl, 2-, 3- and 4-methoxybenzyl, 4-nitrobenzyl, 4-carboxybenzyl, 4-trifluoromethylbenzyl, 1-naphthyl and 2-naphthyl, all hydroxy, amino, carboxy and carbamoyl substituents optionally being substituted, or is pyridinyl mono-substituted with halogen, pyrimidyl, pyrazinyl di-substituted with lower alkyl, pyridazinyl mono-substituted with halogen, piperidinyl in which the amino group may be substituted by an acyl group, thiadiazolyl, oxo-tetrahydrofuranyl, thiophenyl mono-substituted with lower alkoxycarbonyl or carbamoyl, tetrazolyl-lower alkyl, tetrahydrofuranyl-lower alkyl, thiophenyl-lower alkyl or benzimidazolyl-lower alkyl; and
R is carboxy or esterified carboxy;
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 well as the their use and the process for manufacturing such compounds.摘要翻译： 本发明涉及通式I
的头孢菌素衍生物，其中R 1是选自2-，3-和4-羟基苯基，2-和3-甲氧基苯基，4-羧基苯基，4-氨基甲酰基苯基， 3-三氟甲基苯基，2-和3-氟苯基，3-硝基苯基，3-氟-4-羟基苯基，2-氟-4-羟基苯基，3-氟-2-羟基苯基，3-，4-二羟基苯基，苄基，-CHR 2-苯基，3-羟基苄基，4-氨基苄基，2-，3-和4-氟苄基，2-，3-和4-甲氧基苄基，4-硝基苄基，4-羧基苄基，4-三氟甲基苄基，1-萘基和2-萘基 ，任选被取代的全部羟基，氨基，羧基和氨基甲酰基取代基，或被卤素单取代的吡啶基，嘧啶基，被低级烷基二取代的吡嗪基，被卤素单取代的哒嗪基，其中氨基可以被 酰基，噻二唑基，氧代 - 四氢呋喃基，被低级烷氧基羰基或氨基甲酰基单取代的噻吩基，四唑基 - 低级 四氢呋喃基 - 低级烷基，噻吩基 - 低级烷基或苯并咪唑基 - 低级烷基; 且R为羧基或酯化羧基; 易于水解的酯，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，以及它们的用途和制备这些化合物的方法。 -
公开(公告)号：EP0849269A1
公开(公告)日：1998-06-24
申请号：EP97121833.4
申请日：1997-12-11
IPC分类号： C07D501/34 , A61K31/545
CPC分类号： C07D417/12 , C07D501/00 , C07F9/5726 , C07F9/65583 , Y02P20/55
摘要： The present invention relates to cephalosporin derivatives of the general formula
wherein
X is CH or N;
R 1 is hydrogen or cyclopentyl;
R 2 is a group of formula
R 3 is hydrogen, an alkalimetal ion or a tertiary ammonium group;
R 4 is hydrogen, an amino protecting group, pyrrolidin-2-ylmethyl, azetidin-3-ylmethyl, iminomethyl, 1-carbamimidoyl;
R 5 is hydrogen, dialkylcarbamoyl, ω-hydroxyalkyl, ω-aminoalkyl, pyridinium-1-ylmethyl, 1-hydroxy-3-aminomethyl-propyl or (hydroxy)-(pyrrolidin-2-yl)methyl;
R 6 is hydrogen, trifluoromethyl or hydroxy; and
R 7 is alkyl, ω-hydroxy-alkyl, cycloalkyl, 3-pyrrolidinyl, 3-azetidinyl, iminomethyl or 1-carbamimidoyl;
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;
the invention is further concerned with the manufacture of compounds of formula I; with their use as pharmaceutically active substances,
particularly for the treatment and prophylaxis of infectious diseases, and with pharmaceutical preparations containing a compound of formula I for the treatment and prophylaxis of infectious diseases.摘要翻译： 本发明涉及通式
的头孢菌素衍生物，其中X为CH或N; R 1是氢或环戊基; R 2是式CH的基团R 3是氢，碱金属离子或叔铵基团; R 4是氢，氨基保护基，吡咯烷-2-基甲基，氮杂环丁烷-3-基甲基，亚氨基甲基，1-甲脒基; R 5是氢，二烷基氨基甲酰基，ω-羟基烷基，ω-氨基烷基，吡啶鎓-1-基甲基，1-羟基-3-氨基甲基 - 丙基或（羟基） - （吡咯烷-2-基）甲基; R 6是氢，三氟甲基或羟基; 和R 7是烷基，ω-羟基 - 烷基，环烷基，3-吡咯烷基，3-氮杂环丁烷基，亚氨基甲基或1-咔咔脒基; 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; 本发明还涉及式I化合物的制备; 其用作药物活性物质，特别是用于治疗和预防感染性疾病，以及含有式I化合物的药物制剂用于治疗和预防感染性疾病。 -
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
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。
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公开(公告)号：EP0831093A1
公开(公告)日：1998-03-25
申请号：EP97116236.7
申请日：1997-09-18
IPC分类号： C07D463/00 , A61K31/545
CPC分类号： C07D463/22 , Y02P20/55
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.摘要翻译： 其中R 1为氢，任选氟取代的低碳烷基，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的通式I的1-碳 - （dethia） - 头孢菌素衍生物; 其中R5和R6各自独立地为氢或低级烷基，或者R5和R6一起形成环烷基; R4是氢或低级烷基，R7是氢，低级烷基，低级链烯基或羧酸保护基; R2为氢，羟基，低级烷基-Qm，环烷基，低级烷氧基，低级链烯基，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， 低级链烯基，环烯基，低级炔基，芳烷基，芳基，芳氧基，芳烷氧基和杂环未被取代或被选自羧基，氨基，硝基，氰基，任选氟取代的低碳烷基，低碳烷氧基， 羟基，卤素，-COR6，-C（R5R6）CO2R7，-C（R5R6）CONR5R8，-CONR5R6，-N（R6）COOR10，R6OCO-或R6COO-，其中R5和R6为氢或低级烷基; R7是氢，低级烷基，低级链烯基或羧酸保护基; R8是氢，低级烷基或任选取代的苯基; R10是低级烷基，低级链烯基或羧酸保护基; Q是-CHR - ， - CO-或-SO2-; 当R2具有正电荷时，R是氢或低级烷基，R3是羟基，低级烷氧基或-O-，或者-OM和M表示碱金属; m是0或1; n是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化合物的水合物以及它们的酯和盐。
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