知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

611 条记录 (耗时 0.019 秒)

    Substituted 14-desoxy-mutilin compositions
    94.
    发明授权
    Substituted 14-desoxy-mutilin compositions 失效
    取代的14-脱氧 - 突变体组合物

    公开(公告)号：US4278674A

    公开(公告)日：1981-07-14

    申请号：US98333

    申请日：1979-11-29

    申请人： Helmut Egger ,  Hellmuth Reinshagen

    发明人： Helmut Egger ,  Hellmuth Reinshagen

    IPC分类号： C07D243/08 ,  C07C67/00 ,  C07C229/16 ,  C07C313/00 ,  C07C319/14 ,  C07C323/52 ,  C07C323/58 ,  C07C323/62 ,  C07D245/02 ,  C07D295/08 ,  C07D295/12 ,  C07D295/14 ,  A01N37/36 ,  A01N43/36 ,  A01N43/60 ,  A01N43/84

    CPC分类号： C07C323/58

    摘要： This invention relates to new pleuromutilins of the formula: ##STR1## wherein either R.sub.1 is ethyl or vinyl,n is an integer from 2 to 5,x is sulphur,a group ##STR2## or a group .dbd.N--R.sub.4 .sup.I, wherein eitherY and Z are both sulphur, orone of Y and Z is oxygen and the other is sulphur, andR.sub.4.sup.I is hydrogen or a group of the formula: ##STR3## wherein R.sub.1 is as defined above, each of R.sub.2 and R.sub.3 is alkyl of 1 to 10 carbon atoms, orR.sub.2 and R.sub.3 together with the nitrogen atom form a heterocycle of 5 to 7 ring members containing one nitrogen atom or one nitrogen atom and a further hetero member selected from sulphur, oxygen and a group .dbd.N--R.sub.5.sup.I,wherein R.sub.5.sup.I is alkyl of 1 to 5 carbon atoms or hydroxyalkyl of 1 to 4 carbon atoms, orR.sub.2 and R.sub.3 together with the nitrogen atom form a piperazinyl radical, the second nitrogen atom of which is substituted by a radical R.sub.5.sup.II,whereby R.sub.5.sup.II is (acyloxy of 2 to 5 carbon atoms)alkyl of 1 to 4 carbon atoms or (benzoyloxy)alkyl of 1 to 4 carbon atoms,or wherein R.sub.1 is as defined above,n is the number 2,R.sub.3 is alkyl of 1 to 10 carbon atoms, hydroxyalkyl of 1 to 4 carbon atoms, (acyloxy of 2 to 5 carbon atoms)alkyl of 1 to 4 carbon atoms or (benzoyloxy)alkyl of 1 to 4 carbon atoms,X is the group .dbd.N--R.sub.4.sup.II, andR.sub.2 together with R.sub.4.sup.II forms an ethylene bridge between both nitrogen atoms,and pharmaceutically acceptable acid addition salts and quaternary salts thereof.Processes for the preparation of such compounds are described.The compounds are antibiotics with an antibacterial effect.

    摘要翻译： 本发明涉及下式的新型表柔比星：其中R 1为乙基或乙烯基，n为2至5的整数，x为硫，基团或基团= N-R 4 I，其中或 Y和Z都是硫，Y和Z中的一个是氧，另一个是硫，R4I是氢或下式的基团：其中R 1如上所定义，R 2和R 3中的每一个是 1至10个碳原子，或R 2和R 3与氮原子一起形成5至7个含有一个氮原子或一个氮原子的环成员的杂环，以及选自硫，氧和基团= N-R5I的另外的杂原子， 其中R5I为1〜5个碳原子的烷基或1〜4个碳原子的羟基烷基，或R2和R3与氮原子一起形成哌嗪基，其第二个氮原子被基团R 5 II取代，其中R 5II是（ 2至5个碳原子的酰氧基）1至4个碳原子的烷基或1至4个碳原子的（苯甲酰氧基）烷基，或其中R1为 n为2，R3为1〜10个碳原子的烷基，1〜4个碳原子的羟基烷基，2〜5个碳原子的酰氧基，1〜4个碳原子的烷基或1（1）的（苯甲酰氧基）烷基 至4个碳原子，X为基团= N-R4II，R2与R4II一起形成两个氮原子之间的乙烯桥，以及其药学上可接受的酸加成盐和季盐。 描述了制备这些化合物的方法。 这些化合物是具有抗菌作用的抗生素。