利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

12 条记录 (耗时 0.012 秒)

    Penem derivatives, their preparation and pharmaceutical compositions containing them
    6.
    发明授权
    Penem derivatives, their preparation and pharmaceutical compositions containing them 失效
    Penem衍生物，它们的制备和含有它们的药物组合物

    公开(公告)号：US5747483A

    公开(公告)日：1998-05-05

    申请号：US414081

    申请日：1995-03-17

    申请人： Maria Altamura ,  Federico Maria Arcamone ,  Enzo Perrotta ,  Vittorio Pestellini ,  Piero Sbraci ,  Giuseppe Cascio

    发明人： Maria Altamura ,  Federico Maria Arcamone ,  Enzo Perrotta ,  Vittorio Pestellini ,  Piero Sbraci ,  Giuseppe Cascio

    IPC分类号： C07D499/88 ,  A61K31/43 ,  A61K31/48 ,  A61P31/04 ,  C07D499/883 ,  C07D499/897 ,  C07D499/861

    CPC分类号： C07D499/88

    摘要： Penem derivatives of general formula (I), below, and pharmaceutically acceptable salts thereof are disclosed. ##STR1## wherein: R.sub.1 is H, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.7 cycloalkyl, or an optionally protected C.sub.1 -C.sub.6 hydroxyalkyl; R.sub.2 is a free or esterified carboxyl group or a carboxylate anion; R.sub.3 is H or C.sub.1 -C.sub.6 alkyl; R.sub.4 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 mercaptoalkyl, C.sub.1 -C.sub.6 aminoalkyl, C.sub.1 -C.sub.6 alkyl substituted by a quaternary ammonium group, C.sub.1 -C.sub.6 carboxyalkyl, cycloalkyl, aryl, arylalkyl, heterocyclyl-alkyl optionally substituted, saturated or unsaturated heterocycle, or R.sub.3 and R.sub.4 are linked together to form a heterocyclic ring having 3-7 atoms; R.sub.5 and R.sub.6 independently are H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 mercaptoalkyl, C.sub. -C.sub.6 aminoalkyl, alkenyl, cycloalkyl, aryl, arylalkyl, alkylaryl, heterocyclyl-alkyl, C.sub.1 -C.sub.6 alkyl carboxyamide, or R.sub.5 and R.sub.6 are taken together to form a heterocyclic ring having 3-7 atoms, and n is an intiger from 1 to 3.

    摘要翻译： 公开了下述通式（I）的苦味衍生物及其药学上可接受的盐。 （I）其中：R 1是H，C 1 -C 6烷氧基，C 3 -C 7环烷基或任选保护的C 1 -C 6羟烷基; R2是游离的或酯化的羧基或羧酸根阴离子; R3是H或C1-C6烷基; R4是H，C1-C6烷基，C1-C6羟基烷基，C1-C6巯基烷基，C1-C6氨基烷基，被季铵基团取代的C1-C6烷基，C1-C6羧基烷基，环烷基，芳基，芳基烷基， 取代的饱和或不饱和杂环，或者R 3和R 4连接在一起形成具有3-7个原子的杂环; R5和R6独立地是H，C1-C6烷基，C1-C6羟基烷基，C1-C6巯基烷基，C-C6氨基烷基，烯基，环烷基，芳基，芳基烷基，烷基芳基，杂环基 - 烷基，C1-C6烷基羧酰胺或R5和 R6一起形成具有3-7个原子的杂环，并且n是1至3的酸酐。

    Oxidation process for preparing 4-acyloxy azetidinones in a two-phase system
    7.
    发明授权
    Oxidation process for preparing 4-acyloxy azetidinones in a two-phase system 失效
    在两相体系中制备4-酰氧基氮杂环丁酮的氧化方法

    公开(公告)号：US5043440A

    公开(公告)日：1991-08-27

    申请号：US107050

    申请日：1987-10-13

    申请人： Marco Ricci ,  Maria Altamura ,  Daniele Bianchi ,  Walter Cabri ,  Norberto Gatti

    发明人： Marco Ricci ,  Maria Altamura ,  Daniele Bianchi ,  Walter Cabri ,  Norberto Gatti

    IPC分类号： A61K31/397 ,  A61P31/04 ,  C07D205/08

    CPC分类号： C07D205/08 ,  Y02P20/55

    摘要： Process for preparing compounds according to formula (I) ##STR1## wherein R.sub.1 and R.sub.2 represent a hydrogen atom or a protective group and R.sub.3 represents a C.sub.1 -C.sub.10 alkyl or an aryl group, by oxidation of compounds according to formula (II) ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 have the above-mentioned meanings, in a two-phase system comprising:a) an organic phase including a 4-acylazetidinone compound (II) and an "onium" salt dissolved in a medium immiscible with water,b) an aqueous solution including an alkali or alkaline-earth metal salt of an organic or inorganic peracid.4-Acyloxyazetidinones (I) are useful intermediates in the synthesis of anti-bacterial compounds.

    摘要翻译： 制备式（I）化合物的方法其中R 1和R 2表示氢原子或保护基，R 3表示C 1 -C 10烷基或芳基，通过式（II）化合物的氧化 ）其中R1，R2和R3具有上述含义，在两相体系中，包括：a）包含4-酰基氮杂环丁酮化合物（II）和溶于 与水不混溶的介质，b）包含有机或无机过酸的碱金属或碱土金属盐的水溶液。 4-酰氧基氮杂环丁酮（I）是合成抗菌化合物的有用中间体。