Erythromycin derivatives
    5.
    发明授权
    Erythromycin derivatives 失效
    红霉素衍生物

    公开(公告)号:US5217960A

    公开(公告)日:1993-06-08

    申请号:US695176

    申请日:1991-05-03

    CPC分类号: A61K31/70 C07H17/08

    摘要: Antibacterial compounds are disclosed having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sup.1 is --NR.sup.4 R.sup.6, where R.sup.4 and R.sup.6 are independently selected from the group consisting of hydrogen, loweralkyl and arylalkyl or, together, R.sup.4 and R.sup.6 form a nitrogen-containing heterocycle attached at the nitrogen atom; R.sup.2 is selected from the group consisting of hydrogen, --OH and, when R.sup.3 is methylene, oxygen so as to form an epoxide; and R.sup.3 is selected from the group consisting of --CH.sub.2 OH, --NR.sup.4 R.sup.6, --(CH.sub.2).sub.n NR.sup.4 R.sup.6 and, when R.sup.2 is oxygen, methylene so as to form an epoxide, where n is 1-4 and R.sup.4 and R.sup.6 are as previously defined, with the proviso that when R.sup.2 is --OH, R.sup.3 may not be --NR.sup.4 R.sup.6 ; or R.sup.2 and R.sup.3 together are.dbd.CH.sub.2. Also disclosed are processes and intermediates useful in the preparation of the above compounds, as well as compositions containing the same and methods for their use.

    摘要翻译: 公开了具有下式的抗菌化合物及其药学上可接受的盐,其中R 1是-NR 4 R 6,其中R 4和R 6独立地选自氢,低级烷基和芳基烷基,或者R 4和R 6一起形成氮 - 在氮原子附着的杂环; R2选自氢,-OH,当R3为亚甲基时,为氧,形成环氧化物; 并且R 3选自-CH 2 OH,-NR 4 R 6, - (CH 2)n NR 4 R 6,并且当R 2为氧时,亚甲基以形成环氧化物,其中n为1-4,并且R 4和R 6如前所定义, 条件是当R 2是-OH时,R 3可以不是-NR 4 R 6; 或R 2和R 3一起为= CH 2。 还公开了可用于制备上述化合物的方法和中间体,以及含有其的组合物及其使用方法。