Pleuromutilin derivatives as antimicrobials
    4.
    发明公开
    Pleuromutilin derivatives as antimicrobials 有权
    Pleuromutilin-Derivate als antimikrobielle Wirkstoffe

    公开(公告)号:EP1930330A1

    公开(公告)日:2008-06-11

    申请号:EP08152170.0

    申请日:1998-10-27

    摘要: Derivatives of pleuromutilin in which the glycolic ester moiety at position 14 is replaced by R 2 (CH 2 ) m X(CH 2 ) n CH 2 COO are of use in antimicrobial therapy. In which: each of n and m is independently 0, 1 or 2; X is selected from -O-, -S-, -S(O)-, -SO 2 -, -CO.O-, -NH-, -CONH-, -NHCONH- and a bond;R 1 is vinyl or ethyl;R 2 is a non-aromatic monocyclic or bicyclic group containing one or two basic nitrogen atoms and attached through a ring carbon atom; R 3 is H or OH; or the moiety R 2 (CH 2 ) m X(CH 2 ) n CH 2 COO at position 14 of (IA) or (IB) is replaced by R a R b C=CHCOO in which one of R a and R b is hydrogen and the other is R 2 or R a and R b together form R 2 ; or a pharmaceutically acceptable salt thereof

    摘要翻译: 其中第14位的乙醇酸酯部分被R 2(CH 2)m X(CH 2)n CH 2 COO代替的去促胰岛素的衍生物在抗微生物治疗中是有用的。 其中:n和m各自独立地为0,1或2; X选自-O - , - S - , - S(O) - , - SO 2 - , - COO - , - NH - , - CONH - , - NHCONH-和键; R 1是乙烯基或 乙基; R 2是含有一个或两个碱性氮原子并通过环碳原子连接的非芳族单环或双环基团; R 3是H或OH; 或(IA)或(IB)的第14位上的部分R 2(CH 2)m X(CH 2)n CH 2 COO被R a R b C = CHCOO代替,其中R a和R b之一为 氢,另一个是R 2或R a和R b一起形成R 2; 或其药学上可接受的盐