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    Cephalosporin pyridinium derivatives
    2.
    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。

    Derivatives of 3-pyrrolidylidene-2-one-cephalsporines
    3.
    发明授权
    Derivatives of 3-pyrrolidylidene-2-one-cephalsporines 失效
    3-吡咯烷亚基-2-单头孢菌素的衍生物

    公开(公告)号：US5925632A

    公开(公告)日：1999-07-20

    申请号：US875563

    申请日：1997-07-25

    申请人： Ingrid Heinze-Krauss ,  Hans Richter

    发明人： Ingrid Heinze-Krauss ,  Hans Richter

    IPC分类号： C07D501/04 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/06 ,  C07D501/48 ,  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, aralkyl, cycloalkyl, R.sup.3 CO-- or --C(R.sup.4 R.sup.5)CO.sub.2 R.sup.6 ; where R.sup.4 and R.sup.5 are each independently hydrogen or lower alkyl, or R.sup.4 and R.sup.5 taken together with the carbon atom to which they are attached form a cycloalkyl group; R.sup.3 is hydrogen or lower alkyl and R.sup.6 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group;R.sup.2 is isobutyl, 2,2-dimethyl-propyl or cyclohexyl-methyl;n is 0, 1 or 2;X is CH or N;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 are disclosed. These compounds have valuable antibacterial activity.

    摘要翻译： PCT No.PCT / EP96 / 00667 Sec。 371日期1997年7月25日 102（e）日期1997年7月25日PCT提交1996年2月16日PCT公布。 公开号WO96 / 26943 日期：1996年9月6日，式（I）化合物，其中R1为氢，低级烷基，芳烷基，环烷基，R3CO-或-C（R4R5）CO2R6; 其中R 4和R 5各自独立地为氢或低级烷基，或者R 4和R 5与它们所连接的碳原子一起形成环烷基; R3是氢或低级烷基，R6是氢，低级烷基，低级烯基或羧酸保护基; R2是异丁基，2,2-二甲基 - 丙基或环己基 - 甲基; 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化合物及其酯和盐的水合物被公开。 这些化合物具有有价值的抗菌活性。

    Propenyl cephalosporin derivatives and process for the manufacture thereof
    5.
    发明授权
    Propenyl cephalosporin derivatives and process for the manufacture thereof 失效
    丙烯基头孢菌素衍生物及其制备方法

    公开(公告)号：US06583133B1

    公开(公告)日：2003-06-24

    申请号：US09337908

    申请日：1999-06-22

    申请人： Peter Angehrn ,  Erwin Götschi ,  Ingrid Heinze-Krauss ,  Hans G. F. Richter

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

    IPC分类号： C07D50124

    CPC分类号： C07D501/00

    摘要： Disclosed are cephalosporin derivatives of the general formula wherein R is an organic residue with a molecular weight not exceeding 400 bonded to the adjacent sulphur atom via carbon and consisting of carbon, hydrogen, and optional oxygen, sulfur, nitrogen and/or halogen atoms; R1 is hydrogen, lower alkyl or phenyl; and A is a secondary, tertiary or quaternary nitrogen atom bound directly to the propenyl group and being substituted by an organic residue with a molecular weight not exceeding 400 and consisting of carbon, hydrogen, and optional oxygen, sulfur, nitrogen and/or halogen atoms, 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.

    摘要翻译： 公开了通式化合物的头孢菌素衍生物R是分子量不超过400的有机残基，其通过碳与相邻的硫原子键合，并由碳，氢和任选的氧，硫，氮和/或卤素原子组成; R1是氢，低级烷基或苯基; A是与丙烯基直接键合并被分子量不超过400的有机残基取代的仲，叔或季氮原子，由碳，氢和任选的氧，硫，氮和/或卤素原子组成 ，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。

    Vinylpyrrolidinone cephalosporin derivatives
    6.
    发明授权
    Vinylpyrrolidinone cephalosporin derivatives 失效

    公开(公告)号：US06294668B1

    公开(公告)日：2001-09-25

    申请号：US08964640

    申请日：1997-11-05

    申请人： Peter Angehrn ,  Ingrid Heinze-Krauss ,  Hans G. F. Richter

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

    IPC分类号： C07D50124

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： The present invention relates to cephalosporin derivatives of the general formula where R1 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; R4, R5 independently are hydrogen, lower alkyl or phenyl; X is S, O, NH or CH2; n is 0,1 or 2; m is 0 or 1; s is 0 or 1; R2 is hydrogen, hydroxy, —CH2—CONHR6, lower alkyl-Qr, cycloalkyl-Qr, lower alkoxy, lower alkenyl, cycloalkenyl-Qr, lower alkynyl, aralkyl-Qr, aryl-Qr, aryloxy, aralkoxy, a heterocyclic ring or a heterocyclyl-Qr, 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, —SO2NHR6, optionally fluoro substituted lower alkyl, lower alkoxy, hydroxy, halogen, —CONR6R7, —CH2CONR6R7, —N(R7)COOR8, R7CO—, R7OCO—, R7COO —, —C(R7R9)CO2R8, —C(R7R9)CONR7R10, wherein R6 is hydrogen, lower alkyl, cycloalkyl or aryl; R7 and R9 are independently hydrogen or lower alkyl; R8 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group; and R10 is hydrogen, &ohgr;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 &ohgr;-hydroxyalkyl, optionally substituted lower alkoxy and/or cyano, or R7 and R10 form together group of formula Q is —CHR—, —CO— or —SO2—; r is 0 or 1; R is hydrogen or lower alkyl; and R3 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 well as the preparation of such compounds, their use for the treatment of infectious diseases and pharmaceutical preparations containing such compounds.

    1-carba-(dethia)-cephalosporin derivatives
    8.
    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。