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    Cephalosporins
    1.
    发明授权
    Cephalosporins 失效
    CEPHALOSPORINS

    公开(公告)号：US5075298A

    公开(公告)日：1991-12-24

    申请号：US265252

    申请日：1988-10-31

    申请人： Jozsef Aszodi ,  Alain Bonnet ,  Jean-Francois Chantot

    发明人： Jozsef Aszodi ,  Alain Bonnet ,  Jean-Francois Chantot

    IPC分类号： C07D519/06 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/04 ,  C07D501/22 ,  C07D501/24 ,  C07D519/00

    CPC分类号： C07D519/00

    摘要： A compound selected from the group consisting of a syn isomer of a compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl and alkynyl of 2 to 6 carbon atoms and cycloalkyl of 3 to 6 carbon atoms, all optionally substituted with at least one member of the group consisting of optionally esterified or salified carboxy, alkoxy carbonyl, carbamoyl, dimethylcarbamoyl, amino, alkylamino, dialkylamino, halogen, alkoxy and alkylthio of 1 to 4 carbon atoms, aryl, heterocyclic aryl, arylthio and heterocyclic arylthio optionally substituted by alkyl of 1 to 4 carbon atoms, R.sub.1 is selected from the group consisting of ##STR2## and A is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, magnesium, --NH.sub.4 and an organic amine or A is selected from the group consisting of the residue of an easily cleavable ester group or --COOA is --COO-- and the wavy line indicates --CH.sub.2 --R.sub.1 is in the E or Z position and their non-toxic, pharmaceutically acceptable acid addition salts having good antibacterial activity.

    摘要翻译： 选自下式的化合物的顺式异构体的化合物其中R选自氢，1至6个碳原子的烷基，2至6个碳原子的烯基和炔基，以及 具有3至6个碳原子的环烷基，全部由至少一个由任意酯化或成盐的羧基，烷氧基羰基，氨基甲酰基，二甲基氨基甲酰基，氨基，烷基氨基，二烷基氨基，卤素，烷氧基和1至4个碳的烷硫基任意取代 原子，芳基，杂环芳基，芳硫基和任选被1至4个碳原子的烷基取代的杂环芳硫基，R 1选自下列组成的组，A选自氢，碱金属， 碱土金属，镁，-NH 4和有机胺或A选自易裂解酯基团的残基或-COOA为-COO-，波浪线表示-CH2-R1位于E或 Z 位置及其无毒，药学上可接受的酸加成盐具有良好的抗菌活性。

    Cephalosporins
    9.
    发明授权
    Cephalosporins 失效
    头孢菌素

    公开(公告)号：US06313305B1

    公开(公告)日：2001-11-06

    申请号：US08900366

    申请日：1997-07-21

    申请人： Jozsef Aszodi ,  Jean-Francois Chantot ,  Patrick Fauveau ,  Solange Gouin d'Ambrieres ,  Daniel Humbert ,  Christophe Dini

    发明人： Jozsef Aszodi ,  Jean-Francois Chantot ,  Patrick Fauveau ,  Solange Gouin d'Ambrieres ,  Daniel Humbert ,  Christophe Dini

    IPC分类号： C07D28508

    CPC分类号： C07D501/00 ,  C07C45/63 ,  C07C45/673 ,  C07C45/71 ,  C07C47/565 ,  C07C47/575 ,  C07C59/64 ,  C07C69/734 ,  C07C205/44 ,  C07C239/20 ,  C07C255/56 ,  C07C255/57 ,  Y02P20/55

    摘要： A compound having the formula selected from the group consisting of wherein either R3p and R4p are identical and selected from the group consisting of —OH, protected —OH and acyloxy of 1 to 8 carbon atoms, R2p is selected from the group consisting of —CN, —F, Br and I and R1p and R5p are hydrogen or R5p is —F and R1p and R2p are hydrogen or R1p and R2p are F and R5p is hydrogen, or R4p and R5p are identical and selected from the group consisting of —OH, protected —OH and acyloxy of 1 to 8 carbon atoms, R3p is selected from the group consisting of F and —CN and R1p and R2p are hydrogen, R8 is hydrogen or an amine protective group and R10 is the remainder in which the hydroxy or amino are protected wherein R′1 is selected from the group consisting of alkyl of 1 to 4 carbon atoms, —CN, carboxy and alkoxy carbonyl of 1 to 4 carbon atoms.

    摘要翻译： 具有选自R3p和R4p中的式的化合物是相同的，并且选自-OH，被保护的-OH和1至8个碳原子的酰氧基，R2p选自-CN， -F，Br和I，R1p和R5p是氢或R5p是-F，R1p和R2p是氢或R1p，R2p是F，R5p是氢，或R4p和R5p是相同的，选自-OH， 保护的-OH和1至8个碳原子的酰氧基，R3p选自F和-CN，R1p和R2p是氢，R8是氢或胺保护基，R10是其中羟基或氨基 被保护，其中R'1选自1至4个碳原子的烷基，-CN，羧基和1至4个碳原子的烷氧基羰基。

    Cephalosporins
    10.
    发明授权
    Cephalosporins 失效
    头孢菌素

    公开(公告)号：US5936083A

    公开(公告)日：1999-08-10

    申请号：US625910

    申请日：1996-04-01

    申请人： Jozsef Aszodi ,  Jean-Francois Chantot ,  Solange Gouin D'Ambrieres

    发明人： Jozsef Aszodi ,  Jean-Francois Chantot ,  Solange Gouin D'Ambrieres

    IPC分类号： C07D501/00 ,  C07D501/22 ,  C07D501/24 ,  C07D501/56

    CPC分类号： C07D501/00

    摘要： A compound selected from the group consisting of a syn isomer of a compound of the formula ##STR1## in the R or S form or in the form of an R, S mixture wherein R us selected from the group consisting of ##STR2## R and R' are individually selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, CO.sub.2 --Q, ##STR3## CH.sub.2 --SQ, Q and Q' are individually hydrogen or alkyl of 1 to 4 carbon atoms, P, P' and P" are individually alkyl of 1 to 4 carbon atoms optionally substituted by one of the substituents R and R' the dotted line indicating that P and P' can optionally form with the nitrogen atom to which they are linked a heterocycle with 5 or 6 links, R.sub.b and R.sub.c are individually selected from the group consisting of an equivalent of an alkali metal, an alkaline earth metal, magnesium, ammonium and an amine organic base or A and A' are the remainder of an easily cleavable ester group or CO.sub.2 A is CO.sub.2 --and the wavy line indicates that CH.sub.2 R.sub.1 is in the E or Z position and their non-toxic, pharmaceutically acceptable acid addition salts having anti-bacterial activity.

    摘要翻译： 选自R或S形式的式的化合物的顺式异构体或R，S混合物形式的化合物，其中R us选自R和R'的化合物分别选自 由氢，1-4个碳原子的烷基，1-4个碳原子的烷氧基，卤素，CO2-Q，CH2-SQ，Q和Q'分别是氢或1-4个碳原子的烷基，P， P'和P“分别是1至4个碳原子的烷基，任选被一个取代基R和R'取代，虚线表示P和P'可以任选地与它们连接的氮原子一起形成杂环与 5或6链，Rb和Rc分别选自碱金属，碱土金属，镁，铵和胺有机碱的当量，A和A'是易裂解酯基的剩余部分 或CO 2 A是CO 2 - 而波浪线表示CH 2 R 1在E或Z位置a 它们具有抗菌活性的无毒的，药学上可接受的酸加成盐。