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13 条记录 (耗时 0.026 秒)

    6-Acylamino-penam-3-carboxylic and 7-acylamino-3-cephem-4-carboxylic acids
    2.
    发明授权
    6-Acylamino-penam-3-carboxylic and 7-acylamino-3-cephem-4-carboxylic acids 失效
    6-酰基氨基 - penam-3-羧酸和7-酰基氨基-3-头孢烯-4-羧酸

    公开(公告)号：US4015000A

    公开(公告)日：1977-03-29

    申请号：US398512

    申请日：1973-09-18

    申请人： Karoly Kocsis ,  Bruno Fechtig ,  Hans Bickel

    发明人： Karoly Kocsis ,  Bruno Fechtig ,  Hans Bickel

    IPC分类号： C07D499/00 ,  C07D499/44 ,  C07D499/64 ,  C07D499/76 ,  C07D501/20 ,  C07D501/22 ,  C07D501/24 ,  C07D501/26

    CPC分类号： C07D499/00

    摘要： 6-Acylamino-penam-3-carboxylic acids and 7-acylamino-3-cephem-4-carboxylic acids in which the acyl group has the formula ##STR1## IN WHICH R.sub.1 is hydrogen, R.sub.2 is optionally substituted phenyl, thienyl or furyl or R.sub.1 and R.sub.2 together are optionally substituted cycloalkyl, n and m independently of one another represent 0 or 1 and B represents an optionally substituted 2,6-dioxo- or 2,6-dithioxo-1,2,3,6-tetrahydro-pyrimidyl, 2-thioxo-6-oxo-1,2,3,6-tetrahydropyrimidyl, 2,6-dihydroxy- or 2,6-dimercapto-pyrimidyl, 2-mercapto-6-hydroxy-pyrimidyl, 2,6-diaminopyrimidyl, 2-amino-6-hydroxy-pyrimidyl or 2,6-dihalogenopyrimidyl radical, these radicals being bonded in the 4- or 5-position.

    摘要翻译： 6-酰基氨基 - penam-3-羧酸和7-酰基氨基-3-头孢烯-4-羧酸，其中酰基具有下式R1是氢，R2是任选取代的苯基，噻吩基或呋喃基或 R 1和R 2一起为任选取代的环烷基，n和m彼此独立地表示0或1，B表示任选取代的2,6-二氧代 - 或2,6-二硫代-1,2,3,6-四氢 - 嘧啶基 2-硫代-6-氧代-1,2,3,6-四氢嘧啶基，2,6-二羟基 - 或2,6-二巯基嘧啶基，2-巯基-6-羟基 - 嘧啶基，2,6-二氨基嘧啶基， 2-氨基-6-羟基 - 嘧啶基或2,6-二卤代嘧啶基，这些基团键合在4-或5-位上。

    Cephalosporin compounds with terminal aminocarboxylic acid groupings and anti-bacterial use thereof
    4.
    发明授权
    Cephalosporin compounds with terminal aminocarboxylic acid groupings and anti-bacterial use thereof 失效
    具有末端氨基羧酸基团的头孢菌素化合物及其抗菌用途

    公开(公告)号：US4374134A

    公开(公告)日：1983-02-15

    申请号：US120591

    申请日：1980-02-11

    申请人： Karoly Kocsis ,  Peter Schneider ,  Bruno Fechtig ,  Riccardo Scartazzini

    发明人： Karoly Kocsis ,  Peter Schneider ,  Bruno Fechtig ,  Riccardo Scartazzini

    IPC分类号： C07D311/74 ,  A61K31/352 ,  C07D311/22 ,  C07D311/30 ,  C07D311/94 ,  C07D501/20 ,  C07D501/38 ,  A61K31/575

    CPC分类号： C07D311/22 ,  C07D311/30 ,  C07D311/94 ,  Y10S514/826 ,  Y10S514/861

    摘要： Acylamido-3-cephem-4-carboxylic acid compounds of the formula ##STR1## in which the index n represents an integer of from 1 to 4,the index m represents 0 or 1,X represents oxygen, sulphur or an --NH-- group,W represents a --CO--, --CO--NHSO.sub.2 -- or --SO.sub.2 NH--CO-- group, orX-W together represent a --CO-- or --CO--NHSO.sub.2 -- group,A represents optionally substituted phenylene, thienylene or furylene,Y represents hydrogen, hydroxyl, formyloxy, amino or sulpho optionally present in salt form, andZ represents hydrogen, orY andZ together represent an oxo group or an .dbd.N--O--R.sup.o group in which R.sup.o represents hydrogen or optionally substituted lower alkyl,R.sub.1 represents hydrogen, lower alkyl, lower alkoxy, halogen or a group of the formula --CH.sub.2 --R.sub.2 in which R.sub.2 is a free, esterified or etherified hydroxy or mercapto group or a quaternary ammonium group, andR.sub.3 represents hydrogen or methoxy,wherein the carboxyl groups are optionally esterified in a form that can be split under physiological conditions, and the salts thereof, are obtained by liberating the functional group(s) in a starting compound of the formula I in which at least one of the functional groups present is protected.The compounds are effective in vitro and in vivo against gram-positive and gram-negative bacteria and cocci.

    摘要翻译： 酰亚胺基-3-头孢烯-4-羧酸化合物，其中指数n表示1至4的整数，指数m表示0或1，X表示氧，硫 或-NH-基团，W表示-CO-，-CO-NHSO2-或-SO2NH-CO-基团，或XW一起表示-CO-或-CO-NHSO2-基团，A表示任选取代的亚苯基，亚噻吩基 或芳基，Y表示氢，羟基，甲酰氧基，任选以盐形式存在的氨基或磺基，Z表示氢，或Y和Z一起表示氧代基或= NO-Ro基，其中Ro表示氢或任选取代的较低级 烷基，R 1表示氢，低级烷基，低级烷氧基，卤素或式-CH 2 -R 2的基团，其中R 2是游离的，酯化的或醚化的羟基或巯基或季铵基团，R 3表示氢或甲氧基， 其中羧基任选地以可在生理条件下分裂的形式酯化 s及其盐是通过释放其中存在至少一个官能团被保护的式I起始化合物中的官能团而获得的。 这些化合物在体外和体内对革兰氏阳性和革兰氏阴性细菌和球菌有效。

    7.alpha. Ureido cephem-4-carboxylic acid derivatives
    5.
    发明授权
    7.alpha. Ureido cephem-4-carboxylic acid derivatives 失效
    7 {60 {0脲基头孢烯-4-羧酸衍生物

    公开(公告)号：US4115566A

    公开(公告)日：1978-09-19

    申请号：US642505

    申请日：1975-12-19

    申请人： Karoly Kocsis ,  Bruno Fechtig ,  Hans Bickel

    发明人： Karoly Kocsis ,  Bruno Fechtig ,  Hans Bickel

    IPC分类号： C07D307/52 ,  C07D307/68 ,  C07D333/38 ,  C07D499/00 ,  C07D501/20 ,  A61K31/545 ,  C07D501/28

    CPC分类号： C07D333/38 ,  C07D307/52 ,  C07D307/68 ,  C07D499/00

    摘要： 6-Acylamino-penam-3-carboxylic acids and 7-acylamino-3-cephem-4-carboxylic acids in which the acyl group has the formula ##STR1## in which R.sub.1 is hydrogen, R.sub.2 is optionally substituted phenyl, thienyl or furyl, or R.sub.1 and R.sub.2 together are optionally substituted cycloalkyl, and B is a radical which is bonded via a sulphur atom or is bonded to oxygen or sulphur with the interposition of an optionally substituted CH.sub.2 -group.

    摘要翻译： 6-酰基氨基 - 青霉烯-3-羧酸和其中酰基具有式“IMAGE”的7-酰基氨基-3-头孢烯-4-羧酸，其中R 1是氢，R 2是任选取代的苯基，噻吩基或呋喃基， 或者R 1和R 2一起是任选取代的环烷基，B是通过硫原子键合或与氧或硫键合的基团，并插入任选取代的CH 2 - 基团。

    Compounds with terminal aminocarboxylic acid grouping
    6.
    发明授权
    Compounds with terminal aminocarboxylic acid grouping 失效
    具有末端氨基羧酸分子的化合物

    公开(公告)号：US4467101A

    公开(公告)日：1984-08-21

    申请号：US420534

    申请日：1982-09-20

    申请人： Karoly Kocsis ,  Peter Schneider ,  Bruno Fechtig ,  Riccardo Scartazzini

    发明人： Karoly Kocsis ,  Peter Schneider ,  Bruno Fechtig ,  Riccardo Scartazzini

    IPC分类号： C07D499/06 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D307/34 ,  C07D307/52 ,  C07D307/54 ,  C07D333/04 ,  C07D333/24 ,  C07D501/00 ,  C07D501/20 ,  C07D501/32 ,  C07D501/34 ,  C07D501/57 ,  C07D501/59 ,  C07C143/52 ,  C07C147/13 ,  C07C153/00

    CPC分类号： C07D333/24 ,  C07D307/52 ,  C07D307/54

    摘要： Acylamido-3-cephem-4-carboxylic acid compounds of the formula ##STR1## in which the index n represents an integer of from 1 to 4,the index m represents 0 or 1,X represents oxygen, sulphur or an --NH-- group,W represents a --CO--, --CO--NHSO.sub.2 -- or --SO.sub.2 NH--CO-- group, orX-W together represent a --CO-- or --CO--NHSO.sub.2 -- group,A represents optionally substituted phenylene, thienylene or furylene,Y represents hydrogen, hydroxyl, formyloxy, amino or sulpho optionally present in salt form, andZ represents hydrogen, orY and Z together represent an oxo group or an .dbd.N--O--R.degree. group in which R.degree. represents hydrogen or optionally substituted lower alkyl,R.sub.1 represents hydrogen, lower alkyl, lower alkoxy, halogen or a group of the formula --CH.sub.2 --R.sub.2 in which R.sub.2 is a free, esterified or etherified hydroxy or mercapto group or a quaternary ammonium group, andR.sub.3 represents hydrogen or methoxy,wherein the carboxyl groups are optionally esterified in a form that can be split under physiological conditions, and the salts thereof, are obtained by liberating the functional group(s) in a starting compound of the formula I in which at least one of the functional groups present is protected.The compounds are effective in vitro and in vivo against gram-positive and gram-negative bacteria and cocci.

    摘要翻译： 酰亚胺基-3-头孢烯-4-羧酸化合物，其中指数n表示1至4的整数，指数m表示0或1，X表示氧，硫 或-NH-基团，W表示-CO-，-CO-NHSO2-或-SO2NH-CO-基团，或XW一起表示-CO-或-CO-NHSO2-基团，A表示任选取代的亚苯基，亚噻吩基 或呋喃基，Y表示氢，羟基，甲酰氧基，任选以盐形式存在的氨基或磺基，Z表示氢，或Y和Z一起表示氧代基或= NOROR基，其中R DEG表示氢或任选取代的低级 烷基，R 1表示氢，低级烷基，低级烷氧基，卤素或式-CH 2 -R 2的基团，其中R 2是游离的，酯化的或醚化的羟基或巯基或季铵基团，R 3表示氢或甲氧基， 其中羧基任选地以可在生理学上分裂的形式进行酯化 定义及其盐通过释放其中存在至少一个官能团被保护的式I起始化合物中的官能团而获得。 这些化合物在体外和体内对革兰氏阳性和革兰氏阴性细菌和球菌有效。

    Derivatives of penam-3-carboxylic acid and a pharmaceutical composition containing the same
    7.
    发明授权
    Derivatives of penam-3-carboxylic acid and a pharmaceutical composition containing the same 失效
    吡啶-3-羧酸的衍生物和含有它们的药物组合物

    公开(公告)号：US4202900A

    公开(公告)日：1980-05-13

    申请号：US900696

    申请日：1978-04-28

    申请人： Karoly Kocsis ,  Bruno Fechtig ,  Hans Bickel

    发明人： Karoly Kocsis ,  Bruno Fechtig ,  Hans Bickel

    IPC分类号： C07D499/00 ,  C07D499/64 ,  C07D499/74 ,  A61K31/43 ,  C07D499/68

    CPC分类号： C07D499/00

    摘要： 6-Acylamino-penam-3-carboxylic acids and 7-acylamino-3-cephem-4-carboxylic acids in which the acyl group has the formula ##STR1## in which R.sub.1 is hydrogen, R.sub.2 is optionally substituted phenyl, thienyl or furyl or R.sub.1 and R.sub.2 together are optionally substituted cycloalkyl, n and m independently of one another represent 0 or 1 and B represents an optionally substituted 2,6-dioxo- or 2,6-dithioxo-1,2,3,6-tetrahydro-pyrimidyl, 2-thioxo-6-oxo-1,2,3,6-tetrahydropyrimidyl, 2,6-dihydroxy- or 2,6-dimercapto-pyrimidyl, 2-mercapto-6-hydroxy-pyrimidyl, 2,6-diaminopyrimidyl, 2-amino-6-hydroxy-pyrimidyl or 2,6-dihalogenopyrimidyl radical, these radicals being bonded in the 4- or 5-position.

    摘要翻译： 6-酰基氨基 - penam-3-羧酸和其中酰基具有式“IMAGE”的7-酰基氨基-3-头孢烯-4-羧酸，其中R 1是氢，R 2是任选取代的苯基，噻吩基或呋喃基，或 R 1和R 2一起为任选取代的环烷基，n和m彼此独立地表示0或1，B表示任选取代的2,6-二氧代 - 或2,6-二硫代-1,2,3,6-四氢 - 嘧啶基 2-硫代-6-氧代-1,2,3,6-四氢嘧啶基，2,6-二羟基 - 或2,6-二巯基嘧啶基，2-巯基-6-羟基 - 嘧啶基，2,6-二氨基嘧啶基， 2-氨基-6-羟基 - 嘧啶基或2,6-二卤代嘧啶基，这些基团键合在4-或5-位上。

    Process for the manufacture of 3-methylene-cepham compounds
    8.
    发明授权
    Process for the manufacture of 3-methylene-cepham compounds 失效
    3-甲基苯酚化合物的制备方法

    公开(公告)号：US4013650A

    公开(公告)日：1977-03-22

    申请号：US425343

    申请日：1973-12-17

    申请人： Bruno Fechtig

    发明人： Bruno Fechtig

    IPC分类号： A61K31/545 ,  C07D501/04 ,  C07D501/14 ,  C07D501/22

    CPC分类号： C07D501/22 ,  Y02P20/55

    摘要： Compounds of the formula ##STR1## wherein R.sub.1.sup.a represents hydrogen or an amino protective group R.sub.1.sup.A and R.sub.1.sup.b represents hydrogen or an acyl group Ac, or R.sub.1.sup.a and R.sub.1.sup.b together represent a bivalent amino protective group, and R.sub.2 represents hydroxyl or a radical R.sub.2.sup.A which together with the carbonyl grouping --C(=O)-- forms a protected carboxyl group, as well as 1-oxides thereof, and salts of such compounds with salt-forming groups, are prepared from compounds of the formula ##STR2## wherein R.sub.1.sup.a and R.sub.1.sup.b have the above mentioned meaning, R denotes an acyloxy group, R.sub.2.sup.a has the meaning of R.sub.2 or R and R.sub.2.sup.o together denote an epoxy group, from a 1-oxide thereof or a salt of such a compound, by reduction with a metal which has a normal potential of -2.4 to -0.40 volt, or an amalgam thereof, at a pH of 1 to 8, in the presence of water.

    Saccharide derivatives and processes for their manufacture
    9.
    发明授权
    Saccharide derivatives and processes for their manufacture 失效
    糖衍生物及其制造方法

    公开(公告)号：US4873322A

    公开(公告)日：1989-10-10

    申请号：US3986

    申请日：1987-01-16

    申请人： Bruno Fechtig ,  Gerhard Baschang

    发明人： Bruno Fechtig ,  Gerhard Baschang

    IPC分类号： C07H3/08 ,  A61K31/70 ,  A61K31/7008 ,  A61K31/7028 ,  A61P31/12 ,  C07H5/04 ,  C07H5/10 ,  C07H15/04

    CPC分类号： C07H15/04

    摘要： Mono- and di-saccharidyl derivatives that are linked via a bridge member to a cephalin derivative, of the formula I, and processes for their manufacture are described. ##STR1## In the formula, R.sup.1 represents (a) aldohexosyl, (b) D-aldohexosyl that is glycosidically linked in the 4- or the 6-position to D-aldohexosyl, (c) aldopentosyl, (d) 6-deoxyaldohexosyl or (e) 2-acetylamino-2-deoxy-D-aldohexosyl, it being possible for free hydroxy groups present in the radicals mentioned under (a) to (e) above to be peracetylated, X represents oxygen or sulphur, Y represents alkylene having up to 10 carbon atoms in which from 1 to 3 non-terminal methylene groups may be replaced by oxygen, by carbonylimino or by carbonyloxy, R.sup.2 represents hydrogen, carboxy, lower alkoxycarbonyl, benzyloxycarbonyl or carbamoyl, R.sup.3 represents hydrogen and R.sup.4 represents a 1,2-dihydroxy-ethyl, 2-hydroxy-ethyl or hydroxymethyl group in which at least one hydroxy group is esterified by an unsubstituted aliphatic C.sub.10-24 -carboxylic acid and in which the other hydroxy group, if present, is free or esterified by an aliphatic C.sub.2-24 -carboxylic acid, or R.sup.3 and R.sup.4 each represents a hydroxymethyl group esterified by an unsubstituted aliphatic C.sub.10-24 -carboxylic acid. These compounds can be used as medicaments, for example for the prophylaxis and therapy of virus infections.

    摘要翻译： 描述了通过桥构件与式I的头孢氨酸衍生物连接的单糖和二糖基衍生物及其制备方法。 （I）在式中，R1表示（a）醛糖基，（b）在4-或6-位与D-二己糖基糖苷连接的D-二己糖基，（c）戊二糖基，（d）6 （e）2-乙酰氨基-2-脱氧-D-己二糖基，存在于上述（a）〜（e）所述的基团中的游离羟基可能被过乙酰化，X表示氧或硫，Y 表示具有至多10个碳原子的亚烷基，其中1至3个非末端亚甲基可被氧代替，羰基亚氨基或羰氧基表示，R2表示氢，羧基，低级烷氧基羰基，苄氧羰基或氨基甲酰基，R3表示氢，R4表示 其中至少一个羟基被未取代的脂族C 10-24羧酸酯化的1,2-二羟基 - 乙基，2-羟基 - 乙基或羟甲基，其中另一个羟基（如果存在）是游离的或 由脂肪族C 2-羧酸酯化，或者R 3和R 4各自表示羟基 庚基被未取代的脂族C 10-24羧酸酯化。 这些化合物可以用作药物，例如用于预防和治疗病毒感染。