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    Cephalosporin derivatives, and compositions containing them
    2.
    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
    3.
    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
    4.
    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。

    7H-Indolizino [5,6,7-IJ]isoquinoline derivatives
    6.
    发明授权
    7H-Indolizino [5,6,7-IJ]isoquinoline derivatives 失效
    7H-Indolizino {8,5,6,7-I] {9异喹啉衍生物

    公开(公告)号：US3946019A

    公开(公告)日：1976-03-23

    申请号：US491642

    申请日：1974-07-25

    申请人： Daniel Farge ,  Yves le Goff ,  Mayer Naoum Messer ,  Gilbert Poiget

    发明人： Daniel Farge ,  Yves le Goff ,  Mayer Naoum Messer ,  Gilbert Poiget

    IPC分类号： A23K1/16 ,  C07D471/16 ,  C07D471/18

    CPC分类号： C07D471/16

    摘要： Compounds of the formula: ##SPC1##Wherein R represents hydrogen, halogen or alkoxy of 1 to 4 carbon atoms, and R.sub.1 represents hydrogen, alkyl of 1 to 4 carbon atoms substituted by (i) carboxy, (ii) alkoxycarbonyl in which the alkoxy moiety contains 1 to 7 carbon atoms, or (iii) carbamoyl, or R.sub.1 represents phenylalkyl in which the alkyl moiety contains 1 to 4 carbon atoms and is substituted by (i) carboxy, (ii) alkoxycarbonyl in which the alkoxy moiety contains 1 to 4 carbon atoms, or (iii) carbamoyl, or R.sub.1 represents alkanoyl of 1 to 4 carbon atoms or benzoyl, are new compounds possessing chemotherapeutic properties and are particularly active as antibilharzial, anthelmintic and antimicrobial agents.

    摘要翻译： 下式的化合物：

    Naphthyridine derivatives
    7.
    发明授权
    Naphthyridine derivatives 失效
    萘啶衍生物

    公开(公告)号：US4016274A

    公开(公告)日：1977-04-05

    申请号：US623359

    申请日：1975-10-17

    申请人： Claude Cotrel ,  Cornel Crisan ,  Claude Jeanmart ,  Mayer Naoum Messer

    发明人： Claude Cotrel ,  Cornel Crisan ,  Claude Jeanmart ,  Mayer Naoum Messer

    IPC分类号： C07D519/00 ,  C07D401/14

    CPC分类号： C07D519/00

    摘要： Compounds of the formula: ##STR1## wherein one of the symbols =X-- represents =N-- and the other three each represent a group ##STR2## in which Y represents hydrogen, halogen, alkyl, alkoxy, cyano or nitro, at least two of the symbols representing hydrogen, Z represents hydrogen, halogen, alkyl, alkoxy, trifluoromethyl or nitro, and (i) n represents zero and R represents hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl or phenyl, or (ii) n represents 1 and R represents alkyl, hydroxyalkyl or phenyl, are new compounds possessing pharmacological properties; they are particularly active as tranquilizers and anti-convulsant agents.

    摘要翻译： 其中符号之一= X表示= N-，其余三个表示其中Y表示氢，卤素，烷基，烷氧基，氰基或硝基的基团，至少两个 表示氢的符号，Z表示氢，卤素，烷基，烷氧基，三氟甲基或硝基，（i）n表示0，R表示氢，烷基，烯基，炔基，羟烷基或苯基，或（ii）n表示1和 R代表烷基，羟基烷基或苯基，是具有药理学性质的新化合物; 它们作为镇静剂和抗惊厥药物是特别活跃的。

    Isoindolin-1-one derivatives
    8.
    发明授权
    Isoindolin-1-one derivatives 失效
    ISOINDOLIN-1-ONE衍生物

    公开(公告)号：US3987174A

    公开(公告)日：1976-10-19

    申请号：US527031

    申请日：1974-11-25

    申请人： Claude Cotrel ,  Claude Jeanmart ,  Mayer Naoum Messer

    发明人： Claude Cotrel ,  Claude Jeanmart ,  Mayer Naoum Messer

    IPC分类号： C07D209/48 ,  A61K31/44 ,  C07D401/04

    CPC分类号： C07D209/48

    摘要： Isoindolin-1-one derivatives substituted on the nitrogen atom in the 2-position by an unsubstituted or substituted phenyl radical or a heterocyclic radical having aromatic characteristics, substituted in the 3-position by a 3-amino(or substituted amino)-2-hydroxy-propoxy group, and optionally substituted in the 5-and/or 6-positions by one or two alkoxy radicals or optionally substituted in the 5- and 6-positions by a methylenedioxy radical, possess pharmacodynamic properties, and are especially useful as anti-arrhythmic agents.

    Process for the preparation of ampicillin
    9.
    发明授权
    Process for the preparation of ampicillin 失效
    氨苄青霉素的制备方法

    公开(公告)号：US3978078A

    公开(公告)日：1976-08-31

    申请号：US557095

    申请日：1975-03-10

    申请人： Jean Bouchaudon ,  Pierre Le Roy ,  Mayer Naoum Messer

    发明人： Jean Bouchaudon ,  Pierre Le Roy ,  Mayer Naoum Messer

    IPC分类号： C07D499/68 ,  C07D499/80

    CPC分类号： C07D499/68 ,  C07D499/80

    摘要： Ampicillin is prepared by reacting an inorganic or organic base with a new penicillin G derivative of the formula: ##EQU1## (wherein R.sub.1 represents a group protecting the carboxy radical and R.sub.2 represents a strong electron-attracting group, e.g. a halogenoethyl group) to open the imidazolidine ring and give an intermediate product of the formula: ##EQU2## and removing by methods known per se the groups --R.sub.1 and R.sub.2 O--CS-- which protect the carboxy radical and amine functions respectively.

    摘要翻译： 氨苄青霉素通过使无机或有机碱与新的下式的青霉素G衍生物反应制备：OHS | ANGLE CH3 C6H5-CH2-C --- N ---- CH-CHC ANGLE |||| CH3 R2O-CS -NC = OO = CN --- CH-COOR1 ANGLE CH | C6H5（其中R1表示保护羧基的基团，R2表示强电子吸引基团，例如卤代乙基），以打开咪唑烷环，得到中间体 下式的产物：S ANGLE CH3 R2O-CS-NH-CH-CONH-CH-CHC ANGLE ||| CH3 C6H5O = CN --- CH-COOR1，通过本身已知的方法除去基团-R1和R2O -CS-分别保护羧基和胺官能团。