利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

192 条记录 (耗时 0.026 秒)

    Derivatives of macrolide antibiotics
    82.
    发明授权
    Derivatives of macrolide antibiotics 失效
    大环内酯类抗生素衍生物

    公开(公告)号：US4463171A

    公开(公告)日：1984-07-31

    申请号：US502480

    申请日：1983-06-09

    申请人： Hamao Umezawa ,  Tomio Takeuchi ,  Kuniaki Tatsuta ,  Tomoyuki Ishikura ,  Rokuro Okamoto ,  Masao Yamamoto ,  Kohki Kiyoshima

    发明人： Hamao Umezawa ,  Tomio Takeuchi ,  Kuniaki Tatsuta ,  Tomoyuki Ishikura ,  Rokuro Okamoto ,  Masao Yamamoto ,  Kohki Kiyoshima

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： Compounds of the following general formula ##STR1## wherein R.sup.1 and R.sup.2 represent a hydrogen atom or a lower alkanoyl group;R.sup.3 represents a hydrogen atom or the group --COCH.sub.2 R.sup.5 in which R.sup.5 represents a lower alkyl group or an aryl or pyridyl group bonded through a sulfur atom;R.sup.4 represents a methyl group which may be substituted by aryl, pyridyl, pyridylthio, hydroxyl or arylthioamino, an aryl group, a nitrile group, a 5- or 6-membered heterocyclic group having 1 to 4 hetero atoms selected from nitrogen and sulfur atoms, or a tetrahydropyranyl group which may be substituted by methoxy;A represents the group --OCO--, --OSO.sub.2 --, --O-- or --S--, or A and R.sup.4, taken together, represent a halogen atom, a nitrile group or a group of the formula ##STR2## in which R.sup.6 represents two lower alkyl groups, the group ##STR3## or an alkylene group having 4 to 6 carbon atoms which may have in the chain an oxygen atom or a lower alkyl-substituted nitrogen atom; and said aryl group and heterocyclic group may optionally be substituted by a methyl, methoxy or nitro group, and when R.sup.1 represents a lower alkyl group,R.sup.3 does not represent a lower alkyl group,or their salts.These novel derivatives of macrolide antibiotics have excellent antibacterial activity.

    摘要翻译： 下列通式的化合物：其中R 1和R 2表示氢原子或低级烷酰基; R3表示氢原子或基团-COCH2R5，其中R5表示低级烷基或通过硫原子键合的芳基或吡啶基; R 4表示可以被芳基，吡啶基，吡啶硫基，羟基或芳硫基氨基，芳基，腈基，具有1-4个选自氮和硫原子的杂原子的5或6元杂环基取代的甲基， 或可被甲氧基取代的四氢吡喃基; A代表基团-OCO-，-OSO 2 - ， - O-或-S-，或A和R 4一起代表卤素原子，腈基或式（IMAGE）基团，其中R6代表二 低级烷基，基团或具有4-6个碳原子的亚烷基，其可以在链中具有氧原子或低级烷基取代的氮原子; 并且所述芳基和杂环基可任选被甲基，甲氧基或硝基取代，并且当R 1表示低级烷基时，R 3不表示低级烷基或其盐。 这些大环内酯类抗生素的新型衍生物具有优良的抗菌活性。