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963 条记录 (耗时 0.029 秒)

    Antimicrobial cephem compounds
    41.
    发明授权
    Antimicrobial cephem compounds 失效
    抗微生物头孢烯化合物

    公开(公告)号：US4507293A

    公开(公告)日：1985-03-26

    申请号：US504428

    申请日：1983-06-15

    申请人： Takao Takaya ,  Hisashi Takasugi ,  Toshiyuki Chiba ,  Kiyoshi Tsuji

    发明人： Takao Takaya ,  Hisashi Takasugi ,  Toshiyuki Chiba ,  Kiyoshi Tsuji

    IPC分类号： C07D501/20 ,  C07D501/59

    CPC分类号： C07D501/59

    摘要： The invention relates to novel cephem compounds, of antimicrobial activity, of the formula ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.3 is lower alkoxy, andR.sup.4 is carboxy or protected carboxy,and a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及抗微生物活性的新颖的头孢烯化合物，其中R1是氨基或被保护的氨基，R2是羧基（低级）烷基或被保护的羧基（低级）烷基，R3是低级烷氧基，R4是羧基 或保护的羧基及其药学上可接受的盐。

    Cephalosporin derivatives and use as antimicrobial agents
    45.
    发明授权
    Cephalosporin derivatives and use as antimicrobial agents 失效
    头孢菌素衍生物并用作抗微生物剂

    公开(公告)号：US4477448A

    公开(公告)日：1984-10-16

    申请号：US390323

    申请日：1982-06-21

    申请人： Helmut Hamberger ,  Hans Fliri

    发明人： Helmut Hamberger ,  Hans Fliri

    IPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/18 ,  C07D231/38 ,  C07D231/40 ,  C07D501/20 ,  A61K31/545 ,  C07D501/56

    CPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/18 ,  C07D231/38 ,  C07D231/40

    摘要： Novel compounds of formula I, ##STR1## in which R.sub.1 is hydrogen, alkyl, phenylalkyl, carbalkoxyalkyl, acyl, carboxyalkyl, alkoxyalkyl, hydroxyalkyl, cyanoalkyl, or carbamoylalkyl,R.sub.2 is hydrogen, pivaloyloxymethyl or the residue of an easily splittable ester grouping,R.sub.3 is a pyrazolyl radical, unsubstituted or mono- or di-substituted by alkyl, phenyl, alkoxy, alkylthio, carboxy, carboxyalkyl, carbamoyl, carbamoylalkyl, alkylsulphonyl, azido, acylamino, hydrazino, acylhydrazino alkylidenehydrazino, phenylidenehydrazino, in which the phenyl nucleus is unsubstituted or substituted by NH.sub.2, lower alkoxy or lower alkyl, furylidenehydrazino, carbalkoxy or a group R.sub.5 R.sub.6 N--, in which R.sub.5 and R.sub.6 are the same or different and are hydrogen or alkyl, provided that the nitrogen atoms and the 4-position of the pyrazole nucleus are either unsubstituted or substituted by alkyl, phenyl, or carbalkoxy, andR.sub.4 is hydrogen, acetoxy, carbamoyloxy or --S--Rh, in which Rh is a heterocyclic radical.

    摘要翻译： 新的式I化合物，其中R 1是氢，烷基，苯基烷基，烷氧基烷基，酰基，羧基烷基，烷氧基烷基，羟烷基，氰基烷基或氨基甲酰基烷基，R2是氢，新戊酰氧基甲基或易裂解酯基 苯基，苯基，烷氧基，烷硫基，羧基，羧基烷基，氨基甲酰基，氨基甲酰基烷基，烷基磺酰基，叠氮基，酰氨基，肼基，酰肼基亚烷基肼基，苯基亚肼基，其中苯基核是未取代的 或被NH 2，低级烷氧基或低级烷基，亚芳基亚肼基，烷氧基或R5R6N-基团取代，其中R5和R6相同或不同，为氢或烷基，条件是吡唑核的氮原子和4-位 未取代或被烷基，苯基或烷氧基取代，R4是氢，乙酰氧基，氨基甲酰氧基或-S-Rh，其中Rh是杂环基。

    7-Acylaminocephalosporanic acid derivatives
    46.
    发明授权
    7-Acylaminocephalosporanic acid derivatives 失效
    7-酰氨基头孢烷酸衍生物

    公开(公告)号：US4477447A

    公开(公告)日：1984-10-16

    申请号：US351858

    申请日：1982-02-24

    申请人： Ikuo Ueda ,  Tsutomu Teraji ,  Takao Takaya ,  Keiji Takai ,  Hisashi Takasugi ,  Fumio Shimojo ,  Shigetaka Nishino

    发明人： Ikuo Ueda ,  Tsutomu Teraji ,  Takao Takaya ,  Keiji Takai ,  Hisashi Takasugi ,  Fumio Shimojo ,  Shigetaka Nishino

    IPC分类号： A61K20060101 ,  A61K31/545 ,  C07D20060101 ,  C07D501/14 ,  C07D501/16 ,  C07D501/20 ,  C07D501/22 ,  C07D501/46 ,  C07D501/60

    CPC分类号： C07D501/20

    摘要： This invention relates to novel 7-acylaminocephalosporanic acid derivatives of high antimicrobial activity, to processes for their preparation, and to pharmaceutical compositions comprising said derivatives, said derivatives being of the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is dialkanoyloxy(lower)alkyl; alkyl having one or more substituents selected from the group consisting of hydroxy, protected hydroxy, alkoxy, carboxy, protected carboxy, cycloalkylcarbonyloxy and heterocyclic group; lower alkoxycarbonyloxy(lower)alkyl; azido(lower)alkoxycarbonyloxy(lower)alkyl; aroyloxy(lower)alkyl; higher alkanoyloxy(lower)alkyl; phthalidyl; or phthalidylidene(lower)alkyl,R.sup.3 is lower alkyl,Y is thio (--S--) or sulfinyl (--S--), and the dotted line represents 2- or 3-cephem nuclei.

    摘要翻译： 本发明涉及高抗微生物活性的新型7-酰基氨基头孢烷酸衍生物及其制备方法，以及包含所述衍生物的药物组合物，所述衍生物具有下式：其中R1是氨基或被保护的氨基，R2是二烷酰氧基 （低级）烷基; 具有一个或多个选自羟基，保护的羟基，烷氧基，羧基，保护的羧基，环烷基羰基氧基和杂环基的取代基的烷基; 低级烷氧基羰氧基（低级）烷基; 叠氮基（低级）烷氧基羰氧基（低级）烷基; 芳氧基（低级）烷基; 高级烷酰氧基（低级）烷基; 苯酞; 或低级烷基，R 3为低级烷基，Y为硫代（-S-）或亚磺酰基（-S-），虚线表示2-或3-头孢烯核。

    Alkyloximes of 7-amino-thiazolyl-acetamido-cephalosporanic acids
    48.
    发明授权
    Alkyloximes of 7-amino-thiazolyl-acetamido-cephalosporanic acids 失效
    7-氨基 - 噻唑基 - 乙酰氨基 - 头孢烷酸的肟基

    公开(公告)号：US4476122A

    公开(公告)日：1984-10-09

    申请号：US969208

    申请日：1978-12-13

    申请人： Rene Heymes ,  Andre Lutz

    发明人： Rene Heymes ,  Andre Lutz

    IPC分类号： C07D501/06 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D277/20 ,  C07D277/38 ,  C07D501/04 ,  C07D501/20 ,  C07D501/22 ,  C07D501/36 ,  C07D501/56

    CPC分类号： C07D277/20 ,  C07D277/38 ,  C07D277/587

    摘要： Novel alkyloximes of 7-amino-thiazolyl-acetamido-cephalosporanic acids of the formula ##STR1## wherein R is selected from the group consisting of alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms and --CH.sub.2 --SR', R' is selected from the group consisting of acyl of an alkanoic acid of 2 to 4 carbon atoms, 1-methyl-tetrazolyl and 2-methyl-1,3,4-thiadiazolyl, R.sub.1 is selected from the group consisting of hydrogen and a group easily removeable by acid hydrolysis or hydrogenolysis, R.sub.2 is selected from the group consisting of alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, A is selected from the group consisting of hydrogen, an alkali metal cation, an equivalent of an alkaline earth metal or magnesium, or organic amine base cation and an ester group easily removeable by acid hydrolysis or hydrogenolysis with the proviso that when R.sub.1 is hydrogen, A is not an ester group easily removeable by hydrogenolysis or acid hydrolysis and the wavy line means that OR.sub.2 is in one or the other of the two possible syn or anti isomeric positions having a very good antibiotic activity and novel processes and intermediates for their preparation.

    摘要翻译： 具有下式的其中R选自1至5个碳原子的烷基，3至5个碳原子的环烷基和-CH 2 -SR'的7-氨基 - 噻唑基 - 乙酰氨基 - 头孢烷酸的新的烷基肟， R'选自2至4个碳原子的链烷酸的酰基，1-甲基 - 四唑基和2-甲基-1,3,4-噻二唑基，R 1选自氢和 可通过酸解或氢解容易除去的基团，R 2选自1至4个碳原子的烷基和2至4个碳原子的烯基和炔基，A选自氢，碱金属阳离子 ，相当于碱土金属或镁或有机胺碱阳离子和酯基，可以通过酸水解或氢解容易地除去，条件是当R1是氢时，A不是通过氢解或酸水解容易除去的酯基， 波浪线意味着O R2具有非常好的抗生素活性的两种可能的顺式或反式异构体位置中的一种或另一种，以及用于其制备的新方法和中间体。

    Cephalosporin compounds
    49.
    发明授权
    Cephalosporin compounds 失效
    头孢菌素化合物

    公开(公告)号：US4474779A

    公开(公告)日：1984-10-02

    申请号：US433247

    申请日：1982-10-07

    申请人： Noriaki Nagano ,  Kohji Nakano ,  Tadao Shibanuma ,  Yukiyasu Murakami

    发明人： Noriaki Nagano ,  Kohji Nakano ,  Tadao Shibanuma ,  Yukiyasu Murakami

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D277/20 ,  C07D501/20 ,  C07D501/24 ,  C07D501/36 ,  C07D501/56

    CPC分类号： C07D277/587 ,  Y02P20/55

    摘要： Cephalosporin compounds represented by the general formula ##STR1## wherein R represents a group shown by formula ##STR2## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group of 1-3 carbon atoms and R.sup.2 represents a hydrogen atom, a lower alkyl group of 1-3 carbon atoms, a phenyl group which may be substituted by an amino or hydroxy group, a cyano group, a carboxy group, or a carboxymethyl group; said R.sup.1 and R.sup.2 may form a cycloalkylidene group of 4-6 carbon atoms together with the carbon atom to which they are bonded) or a group shown by formula --CH.sub.2 --R.sup.3 (wherein R.sup.3 represents a hydrogen atom, a halogenomethyl group, a carbamoyl group, a carboxymethyl group, .alpha.4-carboxy-3-hydroxyisothiazol-5-yl-thiomethyl group, or .alpha.2-carboxyphenylthiomethyl group); R' represents a group shown by formula ##STR3## (wherein R.sub.a represents a carboxy group, a cyano group, or a carbamoyl group which may be substituted by a lower alkyl group of 1-3 carbon atoms and R.sub.b represents a hydrogen atom or an amino group) or a group shown by formula ##STR4## (wherein R.sub.a and R.sub.b have the same significance as above); and the waveline .about. shows an anti-form or syn-form bond and the salts thereof. They possess excellent antibacterial activities against gram positive bacteria and gram negative bacteria, in particular, pseudomonas aeruginosa and are useful as anti-bacterial agents.

    摘要翻译： 由通式表示的头孢菌素化合物（其中R表示由式表示的基团，其中R1表示氢原子或1-3个碳原子的低级烷基，R2表示氢原子，低级烷基 1-3个碳原子的苯基，可以被氨基或羟基，氰基，羧基或羧甲基取代的苯基;所述R 1和R 2可以一起形成4-6个碳原子的亚环烷基 与其结合的碳原子）或式-CH 2 -R 3（其中R 3表示氢原子，卤代甲基，氨基甲酰基，羧甲基，α4-羧基-3-羟基异噻唑-5 - 基 - 硫代甲基或α2-羧基苯硫基甲基）; R'表示式IMA图示的基团（其中，Ra表示羧基，氰基或可被1-3个碳原子的低级烷基取代的氨基甲酰基，Rb表示氢原子或 氨基）或由式IMA IMA表示的基团（其中Ra和Rb具有与上述相同的含义）; 并且波纹差异显示出抗形式或顺式键及其盐。 它们对革兰氏阳性细菌和革兰氏阴性细菌，特别是铜绿假单胞菌具有优异的抗菌活性，可用作抗菌剂。