• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    Antibacterial 4 sec -epi-9-deoxo-9a-methyl-9a-aza-9a-homo-erythromycin A, pharmaceutically-acceptable salts thereof, pharmaceutical compositions comprising antibacterially-effectife amounts thereof, a method of treatment of bacterial infections with antibacterially effective amounts thereof, and intermediates for the synthesis thereof from erythromycin A.
    公开号:SU1272996A3
    申请号:SU833661803
    申请日:1983-11-14
    公开日:1986-11-23
    发明作者:Майкл Брайт Джен
    申请人:Пфайзер Инк.(Фирма)；
    IPC主号:
    专利说明:


    CM
    Table continuation
    权利要求:
    Claims (1)
    [1]
    In addition, the target compound is tested in vivo by means of a known technique for testing the protective ability of the mouse or by microbiological determination of serum levels in several mammals (for example, mice, rats, dogs). When using rats as a experimental mammal, it has been established that the target compound has an extremely high absorption capacity after oral administration, which ensures exceptionally high serum levels that persist for a long time. Compound 4-epi-9-deoxo-9methyl-9a-aza-9a-homoerythromycin A is less toxic than its epimer, and at a dose of 25 mg / kg / day for 36 days it does not detect changes in the cells of the kidney, spleen, or bile duct , mesenteric lymph nodes, stomach and intestines. The invention of the method for preparing 4 -epi-9-deoxo9a-methyl-9a-aza-9a-homoerythromycin A, characterized in that 4-epi-9-deoxo-.9a-aza9a-homoerythromycin A is methylated in chloroform in the presence of a reducing reagent. , selected from formic acid or hydrogen, and the catalyst - 10% palladium on coal in ethanol at room temperature.
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    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    US44197982A| true| 1982-11-15|1982-11-15|
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