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11 条记录 (耗时 0.016 秒)

    Cephalosporin derivatives, and their application as antibiotics
    1.
    发明授权
    Cephalosporin derivatives, and their application as antibiotics 失效
    头孢菌素衍生物及其作为抗生素的应用

    公开(公告)号：US4950661A

    公开(公告)日：1990-08-21

    申请号：US188073

    申请日：1988-04-28

    申请人： Dominique Olliero ,  Ali Salhi

    发明人： Dominique Olliero ,  Ali Salhi

    IPC分类号： C07D501/20 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46 ,  C07D501/56

    CPC分类号： C07D501/36 ,  C07D501/34 ,  Y02P20/55

    摘要： The present invention relates to derivatives of the cephalosporin family, of formula: ##STR1## in which: X is an oxygen atom or a sulfur atomn is zero, 1 or 2.R.sub.1, R.sub.2 and R.sub.3 each designate, a hydrogen atom or else R.sub.1 and R.sub.2 designate a hydrogen atom or a methyl group, and R.sub.3 designates a carboxyl or cyclopropyl group, or elseR.sub.1 and R.sub.2 taken together with the carbon atom to which they are linked form a cyclobutyl or cyclopentyl group and R.sub.3 is a carboxyl group.B is the residue of a primary or secondary amine;their preparation process and application in therapeutics.

    摘要翻译： 本发明涉及头孢菌素家族的衍生物，其结构如下：其中：X是氧原子或硫原子，n是0,1或2.R 1，R 2和R 3各自表示氢 或者R 1和R 2表示氢原子或甲基，R 3表示羧基或环丙基，或者R 1和R 2与它们所连接的碳原子一起形成环丁基或环戊基，R 3为 羧基。 B是伯胺或仲胺的残基; 其制备方法和在治疗中的应用。

    Antibiotic compounds derived from cephalosporins, process for their production and pharmaceutical compositions
    2.
    发明授权
    Antibiotic compounds derived from cephalosporins, process for their production and pharmaceutical compositions 失效
    来自头孢菌素的抗生素化合物，其制备方法和药物组合物

    公开(公告)号：US4656166A

    公开(公告)日：1987-04-07

    申请号：US612896

    申请日：1984-05-22

    申请人： Ali Salhi ,  Dominique Olliero

    发明人： Ali Salhi ,  Dominique Olliero

    IPC分类号： A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/24 ,  C07D501/26 ,  C07D501/34 ,  C07D501/36 ,  C07D501/46 ,  C07D501/54 ,  C07D501/56 ,  C07D501/60

    CPC分类号： C07D501/36 ,  C07D501/34

    摘要： The compounds according to the invention correspond to the formula: ##STR1## in which: The COOA group at the 4 position is an acid radical, or an alkaline or alkaline-earth salt, or an amino acid or amine salt, for example triethylamine or ethanolamines, or an easily hydrolyzable or metabolically labile and pharmaceutically acceptable ester radical.X denotes an oxygen atom or a sulfur atomn is zero or 1R.sub.1 and R.sub.2 each denote independently hydrogen or a lower alkyl group, preferably a methyl group, orR.sub.1 and R.sub.2 taken together with the carbon atom to which they are linked form a cyclobutyl or cyclopentyl nucleus.B is the residue of a primary or secondary amine.

    摘要翻译： 根据本发明的化合物对应于下式：其中：4位的COOA基团是酸基或碱金属或碱土金属盐或氨基酸或胺盐，用于 例如三乙胺或乙醇胺，或易水解或代谢不稳定和药学上可接受的酯基。 X表示氧原子或硫原子，n为0或1，R 1和R 2各自独立地表示氢或低级烷基，优选甲基，或者R 1和R 2与它们所连接的碳原子一起形成环丁基 或环戊基核。 B是伯胺或仲胺的残基。

    Aromatic acid intermediates
    3.
    发明授权
    Aromatic acid intermediates 失效
    芳香酸中间体

    公开(公告)号：US5250725A

    公开(公告)日：1993-10-05

    申请号：US754037

    申请日：1991-09-03

    申请人： Dominique Olliero ,  Bernard Labeeuw ,  Gilles Roche ,  Ali Salhi

    发明人： Dominique Olliero ,  Bernard Labeeuw ,  Gilles Roche ,  Ali Salhi

    IPC分类号： C07C311/32 ,  C07D501/34 ,  C07C311/17

    CPC分类号： C07D501/34 ,  C07C311/32

    摘要： The present invention relates to novel cephalosporin derivatives with improved pharmacokinetics, corresponding to the formula: ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3 represent a hydrogen atom, or R.sub.1 and R.sub.2 represent a hydrogen atom or a methyl group and R.sub.3 represents a carboxyl group, or ##STR2## form a cyclobutyl group and R.sub.3 represents a carboxyl group; and A and B are different and occupy the meta and para positions of the benzene ring, one representing a hydroxyl group and the other being selected from the groups ##STR3## and --NH--SO.sub.2 --Alk--NH.sub.2 in which Alk denotes a C.sub.2 -C.sub.4 lower alkylene group and also to the pharmaceutically acceptable salts and esters of the said derivatives.It further relates to a process for the preparation of such cephalosporins and to pharmaceutical compositions in which they are present.

    摘要翻译： 本发明涉及具有改善的药代动力学的新型头孢菌素衍生物，其对应于下式：其中：R 1，R 2和R 3表示氢原子，或R 1和R 2表示氢原子或甲基 并且R 3表示羧基，或形成环丁基，R 3表示羧基; 并且A和B不同，占据苯环的间位和对位，一个表示羟基，另一个选自下组：其中R 1，R 2，R 2， Alk表示C2-C4低级亚烷基，也表示所述衍生物的药学上可接受的盐和酯。 本发明还涉及一种制备这种头孢菌素的方法及其存在的药物组合物。

    Cephalosporin derivatives and pharmaceutical compositions in which they are present
    4.
    发明授权
    Cephalosporin derivatives and pharmaceutical compositions in which they are present 失效
    CEPHALOSPORIN衍生物及其现有的药物组合物

    公开(公告)号：US5079241A

    公开(公告)日：1992-01-07

    申请号：US420270

    申请日：1989-10-13

    申请人： Dominique Olliero ,  Bernard Labeeuw ,  Gilles Roche ,  Ali Salhi

    发明人： Dominique Olliero ,  Bernard Labeeuw ,  Gilles Roche ,  Ali Salhi

    IPC分类号： C07C311/08 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07C303/38 ,  C07C311/32 ,  C07C311/46 ,  C07D501/04 ,  C07D501/34

    CPC分类号： C07D501/34 ,  C07C311/32

    摘要： The present invention relates to novel cephalosporin derivatives with improved pharmacokinetics, corresponding to the formula: ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3 represent a hydrogen atom, or R.sub.1 and R.sub.2 represent a hydrogen atom or a methyl group and R.sub.3 represents a carboxyl group, or ##STR2## form a cyclobutyl group and R.sub.3 represents a carboxyl group; and A and B are different and occupy the meta and para positions of the benzene ring, one representing a hydroxyl group and the other being selected from the groups ##STR3## and --NH--SO.sub.2 --Alk--NH.sub.2 in which Alk denotes a C.sub.2 -C.sub.4 lower alkylene group and also to the pharmaceutically acceptable salts and esters of the said derivatives.It further relates to a process for the preparation of such cephalosporins and to pharmaceutical compositions in which they are present.

    摘要翻译： 本发明涉及具有改善的药代动力学的新型头孢菌素衍生物，其对应于下式：其中：R 1，R 2和R 3表示氢原子，或R 1和R 2表示氢原子或甲基 并且R 3表示羧基，或形成环丁基，R 3表示羧基; A和B不同，占据苯环的间位和对位，一个表示羟基，另一个选自基团，其中Alk表示 C2-C4低级亚烷基，以及所述衍生物的药学上可接受的盐和酯。 本发明还涉及一种制备这种头孢菌素的方法及其存在的药物组合物。

    Derivatives of pyridinium thiomethyl cephalosporins
    9.
    发明授权
    Derivatives of pyridinium thiomethyl cephalosporins 失效
    吡啶硫代甲基头孢菌素的衍生物

    公开(公告)号：US4593022A

    公开(公告)日：1986-06-03

    申请号：US441757

    申请日：1982-11-15

    申请人： Bernard Labeeuw ,  Ali Salhi

    发明人： Bernard Labeeuw ,  Ali Salhi

    IPC分类号： C07D501/06 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D213/70 ,  C07D501/36 ,  C21C5/34 ,  C21C5/48 ,  C07D501/38

    CPC分类号： C07D213/70

    摘要： The present invention relates to cephalosporins of general formula: ##STR1## in which: R.sub.1 is H or CH.sub.3, R.sub.2 is CH.sub.3, or R.sub.1 and R.sub.2 taken together form a 1,3-propylene group,R.sub.3 is lower alkyl, alkenyl, alkynyl or CH.sub.2 COO alkyl,R.sub.4 is H or OH, the S being bonded to the pyridine ring in 2 or 4 position,A is H or cation or ester or hemiacetal which is easily hydrolyzable,and X is a derivative of a mineral or organic acid.The invention also relates to a process for preparing these new cephalosporins and to the drugs containing said cephalosporins.

    摘要翻译： 本发明涉及以下通式的头孢菌素：其中：R 1为H或CH 3，R 2为CH 3，或R 1和R 2一起形成1,3-亚丙基，R 3为低级烷基，烯基，炔基或 CH2COO烷基，R4为H或OH，S与吡啶环键合在2或4位，A为H或阳离子或酯或半缩醛，易水解，X为矿物或有机酸的衍生物。 本发明还涉及制备这些新型头孢菌素和含有头孢菌素的药物的方法。