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33 条记录 (耗时 0.026 秒)

    Cephalosporin derivatives
    2.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号：US4520193A

    公开(公告)日：1985-05-28

    申请号：US322961

    申请日：1981-11-19

    申请人： Christian Berger ,  Daniel Farge ,  Claude Moutonnier ,  Gerard Wolff

    发明人： Christian Berger ,  Daniel Farge ,  Claude Moutonnier ,  Gerard Wolff

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/20 ,  C07D501/24 ,  C07D501/38

    CPC分类号： C07D501/24

    摘要： The invention provides new cephalosporin derivatives of the general formula, ##STR1## which are in the form of a bicyclooct-2-ene or bicyclooct-3-ene, in which formula R.sub.1 is a radical of the general formula ##STR2## [in which R.sub.5 is hydrogen, alkyl, vinyl, cyanomethyl, protected carboxyalkyl or a protective radical and R.sub.6 is a protective radical] or an amino-protecting radical, R.sub.2 is an acid-protecting radical and R.degree. represents various organic radicals, or alternatively R.sub.1 is an amino-protecting radical or various acyl radicals, R.sub.2 is a protective radical and R.degree. represents various organic radicals, and R.sub.3 and R.sub.4 are alkyl radicals optionally substituted by alkoxy or dialkylamino, or phenyl radicals, or --NR.sub.3 R.sub.4 forms a heterocyclic ring. These products are intermediates for the synthesis of cephalosporins having antibacterial activity.

    摘要翻译： 本发明提供了通式为（IMA）（I）的新型头孢菌素衍生物，其为双环-2-烯或双环辛-3-烯的形式，其中式R1为通式为“IMAGE” （II）[其中R5为氢，烷基，乙烯基，氰基甲基，被保护的羧基烷基或保护基，R6为保护基]或氨基保护基，R2为酸保护基，R DEG为各种有机基团 或者R 1为氨基保护基或各种酰基，R 2为保护基，R≠表示各种有机基团，R 3和R 4为任选被烷氧基或二烷基氨基取代的烷基或苯基或-NR 3 R 4形式 杂环。 这些产品是合成具有抗菌活性的头孢菌素的中间体。

    Thiazolo(3,2-C)benzoxazine derivatives
    3.
    发明授权
    Thiazolo(3,2-C)benzoxazine derivatives 失效
    噻唑（3,2-C）苯并恶嗪衍生物

    公开(公告)号：US4291032A

    公开(公告)日：1981-09-22

    申请号：US192988

    申请日：1980-10-02

    申请人： Christian Berger ,  Daniel Farge ,  Claude Moutonnier ,  Gerard Wolff

    发明人： Christian Berger ,  Daniel Farge ,  Claude Moutonnier ,  Gerard Wolff

    IPC分类号： A61K31/4188 ,  A61K31/535 ,  A61K31/5365 ,  A61P25/04 ,  A61P29/00 ,  C07D513/04

    CPC分类号： C07D513/04

    摘要： New thiazolo[3,2-c]-1,3-benzoxazine derivatives of the general formula (I), in which X is oxygen or sulfur, R.sub.1 and R.sub.2, which are identical or different, are hydrogen or halogen atoms or alkyl, alkoxy, alkylthio or trifluoromethyl radicals, in the 7-, 8-, 9- or 10-position, and R.sub.3 is a hydrogen atom or a carboxyl radical, their salts, if appropriate, their preparation and the medicaments in which they are present.These new derivatives are particularly useful as analgesic agents. ##STR1##

    摘要翻译： 其中X是氧或硫的通式（I）的新的噻唑并[3,2-c] -1,3-苯并恶嗪衍生物，相同或不同的R 1和R 2是氢或卤素原子或烷基， 烷氧基，烷硫基或三氟甲基，在7-，8-，9-或10-位，R3是氢原子或羧基，它们的盐，如果合适，它们的制备和它们存在的药物。 这些新衍生物作为止痛剂特别有用。 （一）

    Cephalosporin derivatives, and compositions containing them
    5.
    发明授权
    Cephalosporin derivatives, and compositions containing them 失效
    头孢菌素衍生物和含有它们的组合物

    公开(公告)号：US4034088A

    公开(公告)日：1977-07-05

    申请号：US573110

    申请日：1975-04-30

    申请人： Christian Berger ,  Daniel Farge ,  Georges Gros ,  Mayer Naoum Messer ,  Claude Moutonnier

    发明人： Christian Berger ,  Daniel Farge ,  Georges Gros ,  Mayer Naoum Messer ,  Claude Moutonnier

    IPC分类号： C07D501/06 ,  A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  C07D20060101 ,  C07D501/04 ,  C07D501/16 ,  C07D501/20 ,  C07D501/22 ,  C07D501/24 ,  C07D501/26 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46 ,  C07D501/60

    CPC分类号： C07D501/20

    摘要： New cephalosporin derivatives of the general formula: ##STR1## in which R represents a straight or branched chain C.sub.1-4 alkyl radical, or a phenyl (straight or branched chain C.sub.1-4 alkyl) radical, n is 0, 1 or 2, and either R.sub.1 is a pyridinio ion and R.sub.2 is a carboxylato ion, or R.sub.1 represents a hydrogen atom, or an acetoxy, (5-methyl-1,3,4-thiadiazol-2-yl)-thio or (1-methyl-1,2,3,4-tetrazol-5-yl)-thio radical and R.sub.2 represents a carboxy radical or a radical of the formula; ##STR2## in which the radical: ##STR3## is a radical which can be removed easily by enzymatic means and in which R.sub.3 represents a hydrogen atom or a straight or branched chain C.sub.1-4 alkyl radical, a phenyl radical or a phenyl (C.sub.1-2 alkyl) radical and R.sub.4 represents a straight or branched chain C.sub.1-4 alkyl radical, a straight or branched chain C.sub.1-4 alkoxy radical, a cyclohexyl radical, a phenyl radical or a phenyl (C.sub.1-2 alkyl) radical;With the proviso that when R is an alkyl radical and either R.sub.1 is a hydrogen atom or an acetoxy radical and R.sub.2 is a carboxy radical or R.sub.1 is a pyridinio ion and R.sub.2 is a carboxylato ion, n is 1 or 2, and metal salts thereof and addition salts thereof with nitrogen-containing bases are new compounds; they possess valuable antibacterial properties, showing activity against both Gram-positive and Gram-negative bacteria.

    摘要翻译： 新的头孢菌素衍生物，其通式为：其中R表示直链或支链C 1-4烷基或苯基（直链或支链C 1-4烷基）基团，n为0,1或2，以及 R1是吡啶鎓离子，R2是羧基离子，或R1代表氢原子，或乙酰氧基，（5-甲基-1,3,4-噻二唑-2-基） - 硫代或（1-甲基-1 ，2,3,4-四唑-5-基） - 硫基，R 2表示下式的羧基或基团： ，其中基团：是可以通过酶学方法容易地除去的基团，其中R 3表示氢原子或直链或支链C 1-4烷基，苯基或苯基（C 1 -2烷基）基，R 4表示直链或支链C 1-4烷基，直链或支链C 1-4烷氧基，环己基，苯基或苯基（C 1-2烷基）基; 当R为烷基且R 1为氢原子或乙酰氧基且R 2为羧基或R 1为吡啶并且R 2为羧基离子时，n为1或2，其金属盐为 其与含氮碱的加成盐是新化合物; 它们具有有价值的抗菌性能，显示出对革兰氏阳性菌和革兰氏阴性菌的活性。

    Cephalosporin derivatives, their preparation and compositions containing them
    6.
    发明授权
    Cephalosporin derivatives, their preparation and compositions containing them 失效
    头孢菌素衍生物，它们的制备和含有它们的组合物

    公开(公告)号：US4508717A

    公开(公告)日：1985-04-02

    申请号：US522359

    申请日：1983-08-11

    申请人： Christian Berger ,  Daniel Farge ,  Claude Moutonnier ,  Jean-Francois Peyronel ,  Bernard Plau

    发明人： Christian Berger ,  Daniel Farge ,  Claude Moutonnier ,  Jean-Francois Peyronel ,  Bernard Plau

    IPC分类号： C07D501/20 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/24 ,  C07D501/36

    CPC分类号： C07D501/00

    摘要： Cephalosporin derivatives of the formula: ##STR1## in which A is a single bond or a radical --CH.sub.2 --, --NH-- or --NHCO--, attached to the 3-position or 4-position of the pyridinio radical, R is a methyl, carboxymethyl, carbamoylmethyl, benzyl or allyl radical, R.sub.a, R.sub.b and R.sub.c are hydrogen atoms, or alternatively R.sub.a is carboxyl and R.sub.b and R.sub.c, which are identical or different, are hydrogen atoms or alkyl radicals, or together form an alkylene radical, and n equals 0 or 1, in their syn form, and also their addition salts with acids, metal salts and addition salts with nitrogen-containing bases are antibacterial agents having a broad spectrum of activity.

    摘要翻译： 下式的头孢菌素衍生物：其中A是单键或者连接到吡啶基的3-位或4-位的基团-CH 2 - ， - NH-或-NHCO-，R 是甲基，羧甲基，氨基甲酰基甲基，苄基或烯丙基，Ra，Rb和Rc是氢原子，或者Ra是羧基，Rb和Rc相同或不同，是氢原子或烷基，或一起形成亚烷基 自由基，n等于0或1，并且它们与酸，金属盐和与含氮碱的加成盐的加成盐也是具有广谱活性的抗菌剂。

    Cephalosporin derivatives
    9.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号：US4034090A

    公开(公告)日：1977-07-05

    申请号：US592096

    申请日：1975-06-30

    申请人： Christian Berger ,  Daniel Farge ,  Georges Gros ,  Mayer Naoum Messer ,  Claude Moutonnier

    发明人： Christian Berger ,  Daniel Farge ,  Georges Gros ,  Mayer Naoum Messer ,  Claude Moutonnier

    IPC分类号： C07D501/06 ,  A61K31/546 ,  C07D257/04 ,  C07D285/12 ,  C07D285/125 ,  C07D285/13 ,  C07D501/20 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46 ,  A61K31/545

    CPC分类号： C07D257/04 ,  C07C329/00 ,  C07D285/125 ,  C07D285/13 ,  C07D501/20

    摘要： New cephalosporin derivatives of the formula: ##STR1## in which either (a) R.sub.1 is hydrogen, acetoxy, azido or heterocyclylthio or heterocyclylcarbonylthio which is (1,3,4-thiadiazol-2-yl)-thio which is unsubstituted or substituted by straight or branched chain C.sub.1-4 alkyl or alkoxy, straight or branched chain C.sub.1-4 alkylthio, straight or branched chain C.sub.1-4 alkylsulphonyl, amino or acetylamino; (1,2,3,4-tetrazol-5-yl)-thio which is unsubstituted or substituted in the 1-position by straight or branched chain C.sub.1-4 alkyl, hydroxy straight or branched chain C.sub.1-4 alkyl, phenyl or hydroxyphenyl, or in the 2-position by straight or branched chain C.sub.1-4 alkyl or hydroxy straight or branched chain C.sub.1-4 alkyl; (1,2,4-triazol-3-yl)-thio, (4-methyl-1,3-thiazol-2-yl)-thio, (3-methyl-1,2,4-thiadiazol-5-yl)-thio or (1,2,3-thiadiazol-4-yl)-carbonylthio, and R.sub.2 is carboxy or a radical of the formula: ##STR2## in which the radical: ##STR3## is a radical which can be easily removed enzymatically, and in which R.sub.3 is hydrogen or straight or branched chain C.sub.1-4 alkyl and R.sub.4 is straight or branched chain C.sub.1-4 alkyl or cyclohexyl; or (b) R.sub.1 is a pyridinio ion and R.sub.2 is a carboxylato ion, and pharmaceutically acceptable non-toxic metal salts thereof and addition salts thereof with nitrogen containing bases possess valuable anti-bacterial properties, showing activity against both Gram-positive and Gram-negative bacteria.

    摘要翻译： 下式的新型头孢菌素衍生物：其中（a）R 1是氢，乙酰氧基，叠氮基或杂环基硫基或杂环基羰基硫基，其是未取代的（1,3,4-噻二唑-2-基） - 硫基 直链或支链C 1-4烷基或烷氧基，直链或支链C 1-4烷硫基，直链或支链C 1-4烷基磺酰基，氨基或乙酰氨基; （1,2,3,4-四唑-5-基） - 硫基，其未被取代或在1-位被直链或支链C 1-4烷基取代，羟基直链或支链C 1-4烷基，苯基或羟基苯基 或2-位的直链或支链C 1-4烷基或羟基直链或支链C 1-4烷基; （1,2,4-三唑-3-基） - 硫代，（4-甲基-1,3-噻唑-2-基） - 硫代，（3-甲基-1,2,4-噻二唑-5-基） ） - 硫代或（1,2,3-噻二唑-4-基） - 羰基硫基，并且R 2是羧基或下式的基团：其中基团：（III）是 其可以容易地被酶除去，其中R 3是氢或直链或支链C 1-4烷基，R 4是直链或支链C 1-4烷基或环己基; 或（b）R 1是吡啶鎓离子，R 2是羧基离子，其药学上可接受的无毒金属盐和其与含氮碱基的加成盐具有有价值的抗菌性质，显示出对革兰氏阳性和革兰氏阴性菌的活性， 阴性细菌。

    1,4-Dithiin (and oxathiin)-yl cephalosporin derivatives, and compositions containing them
    10.
    发明授权
    1,4-Dithiin (and oxathiin)-yl cephalosporin derivatives, and compositions containing them 失效
    1,4-二硫辛（和氧硫辛酸） - 基头孢菌素衍生物和含有它们的组合物

    公开(公告)号：US4029781A

    公开(公告)日：1977-06-14

    申请号：US617066

    申请日：1975-09-26

    申请人： Christian Berger ,  Daniel Farge ,  Georges Gros ,  Mayer Naoum Messer ,  Claude Moutonnier

    发明人： Christian Berger ,  Daniel Farge ,  Georges Gros ,  Mayer Naoum Messer ,  Claude Moutonnier

    IPC分类号： C07D501/22 ,  A61K31/546 ,  C03C17/28 ,  C07D501/06 ,  C07D501/20 ,  C07D501/34 ,  A61K31/54

    CPC分类号： C07D501/20 ,  C03C17/28 ,  Y02P20/55

    摘要： New cephalosporin compounds of the formula: ##STR1## in which A is oxygen or sulphur, R.sub.1 is hydrogen or acetoxy and R.sub.2 is carboxy or a radical of the formula: ##STR2## in which the radical ##STR3## is a radical which can be easily removed enzymatically, and in which R.sub.3 is hydrogen or straight or branched chain C.sub.1-4 alkyl and R.sub.4 is straight or branched chain C.sub.1-4, alkyl or cyclohexyl, together with its diastereoisomeric forms and mixtures thereof, its acid addition salts and, where appropriate, its pharmaceutically acceptable non-toxic metal salts and addition salts with nitrogen-containing bases other than ammonia, exhibit valuable anti-bacterial properties, in particular against Gram-positive and Gram-negative bacteria.

    摘要翻译： 下式的新型头孢菌素化合物：其中A是氧或硫，R1是氢或乙酰氧基，R2是羧基或下式的基团：其中基团（I） （III）是可以容易地酶促去除的基团，其中R3是氢或直链或支链C1-4烷基，R4是直链或支链C1-4，烷基或环己基，以及它们的非对映异构形式和混合物 其酸加成盐，并且在适当的情况下，其药学上可接受的无毒金属盐和与氨以外的含氮碱的加成盐显示出有价值的抗菌性质，特别是抗革兰氏阳性和革兰氏阴性菌。