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    Cephalosporins
    1.
    发明授权
    Cephalosporins 失效
    头孢菌素

    公开(公告)号：US4200746A

    公开(公告)日：1980-04-29

    申请号：US888242

    申请日：1978-03-20

    申请人： Martin C. Cook ,  Gordon I. Gregory ,  Janice Bradshaw

    发明人： Martin C. Cook ,  Gordon I. Gregory ,  Janice Bradshaw

    IPC分类号： C07D501/20 ,  C07D501/46

    CPC分类号： C07D501/46

    摘要： Cephalosporin antibiotics in which the 7.beta.-acylamido group has the formula ##STR1## (where R.sup.1 is furyl or thienyl and R.sup.2 is C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, furylmethyl or thienylmethyl) and in which the 3-position substituent is a pyridiniummethyl group wherein the pyridine ring is optionally substituted by carbamoyl, carboxy, carboxymethyl, sulpho or methyl exhibit high antibacterial activity against a broad range of gram-positive and gram-negative organisms, coupled with particularly high stability to .beta.-lactamases produced by various gram-negative organisms and good stability in vivo, particularly to esterases.

    摘要翻译： 头孢菌素抗生素，其中7β-酰胺基具有式（IMAGE）（其中R 1为呋喃基或噻吩并且R 2为C 1-4烷基，C 3-7环烷基，呋喃基甲基或噻吩基甲基），其中3位取代基为 吡啶甲基，其中吡啶环任选被氨基甲酰基，羧基，羧甲基，磺基或甲基取代，对广泛的革兰氏阳性和革兰氏阴性生物表现出高抗菌活性，加上由各种克产生的β-内酰胺酶具有特别高的稳定性 - 阴性生物体和良好的体内稳定性，特别是酯酶。

    3-Acetoxymethyl cephalosporins having at position-7 a carboxy substituted .alpha.-etherified hydroxyiminoarylacetamido group
    2.
    发明授权
    3-Acetoxymethyl cephalosporins having at position-7 a carboxy substituted .alpha.-etherified hydroxyiminoarylacetamido group 失效
    在7位具有羧基取代的{60-羟基亚氨基芳基乙酰氨基的3-乙酰氧基甲基头孢菌素

    公开(公告)号：US4144393A

    公开(公告)日：1979-03-13

    申请号：US668245

    申请日：1976-03-18

    申请人： Janice Bradshaw ,  Martin C. Cook ,  Gordon I. Gregory

    发明人： Janice Bradshaw ,  Martin C. Cook ,  Gordon I. Gregory

    IPC分类号： C07D307/54 ,  C07D333/24 ,  C07D501/20 ,  C07D501/34 ,  A61K31/545

    CPC分类号： C07D307/54 ,  C07D333/24

    摘要： 3-Acetoxymethyl cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure ##STR1## where R is thienyl, furyl or phenyl; R.sup.a is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl or phenyl, and R.sup.b is hydrogen, carboxy, C.sub.2 -C.sub.5 carbalkoxy or any of the groups designated for R.sup.a, or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; exhibit broad spectrum antibiotic activity characterized by particularly high activity against gram negative microorganisms, including those which produce .beta.-lactamases. The compounds, which are syn isomers or exist as mixtures of syn and anti isomers containing at least 90% of the syn isomer, have particularly high in vitro activity against strains of Escherichia coli. Haemophilus influenzae and Proteus organisms; and also shown unusually high activity against Pseudomonas organisms.

    摘要翻译： 3-乙酰氧基甲基头孢菌素抗生素，其中7β-酰胺基具有结构

    Cephalosporins having a 7-(carboxy substituted .alpha.-etherified oximinoarylacetamido) group
    3.
    发明授权
    Cephalosporins having a 7-(carboxy substituted .alpha.-etherified oximinoarylacetamido) group 失效
    头孢菌素具有7-（羧基取代的{60-乙酰肟基芳基乙酰胺基）基团

    公开(公告)号：US4060686A

    公开(公告)日：1977-11-29

    申请号：US668246

    申请日：1976-03-18

    申请人： Janice Bradshaw ,  Martin Christopher Cook ,  Gordon Ian Gregory

    发明人： Janice Bradshaw ,  Martin Christopher Cook ,  Gordon Ian Gregory

    IPC分类号： C07D307/54 ,  C07D333/24 ,  C07D501/26 ,  C07D501/32 ,  C07D501/34

    CPC分类号： C07D307/54 ,  C07D333/24

    摘要： 3-Carbamoyloxymethyl and 3-N-methylcarbamoyloxymethyl cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure ##STR1## where R is thienyl, furyl or phenyl; R.sup.a is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl or phenyl, and R.sup.b is hydrogen, carboxy, C.sub.2 -C.sub.5 carbalkoxy or any of the groups designated for R.sup.a, or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; exhibit broad spectrum antibiotic activity charcterized by particularly high activity against gram negative microorganisms, including those which produce .beta.-lactamases. The compounds, which are syn isomers or exist as mixtures of syn and anti isomers containing at least 90% of the syn isomer, have particularly high in vitro activity against strains of Escherichia coli, Haemophilus influenzae and Proteus organisms; and also shown unusually high activity against Pseudomonas organisms.

    摘要翻译： 3-羧甲酰氧基甲基和3-N-甲基氨基甲酰氧甲基头孢菌素抗生素，其中7β-酰胺基具有结构