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Water-soluble prodrugs of chloramphenicol, thiamphenicol, and analogs thereof

机译:氯霉素,甲砜霉素及其类似物的水溶性前药

摘要

The present invention discloses certain novel prodrugs of chloramphenicol or thiamphenicol, or of an analog of either, including prodrugs of pharmaceutically acceptable salts of chloramphenicol or thiamphenicol or of their analogs, including nitrogen-containing esters of both alcohol groups of such compounds. In certain embodiments these novel prodrugs are sufficiently water-soluble to serve the functions needed of a prodrug of chloramphenicol or thiamphenicol or of an analog of either. In one embodiment, a certain subclass of the compounds also possesses the hydrolytic stability needed to maintain the prodrug in solution in the subject's system until appropriate conditions exist when the prodrug can hydrolyze, releasing the active compound in question.
机译:本发明公开了氯霉素或噻吩酚或其类似物的某些新的前药,包括氯霉素或噻吩酚的药学上可接受的盐的前药或其类似物,包括此类化合物的两个醇基的含氮酯。在某些实施方案中,这些新颖的前药具有足够的水溶性,以发挥氯霉素或甲砜霉素或两者类似物的前药所需的功能。在一个实施方案中,化合物的某些亚类还具有维持前药在受试者系统中的溶液中所需的水解稳定性,直到当前药可以水解以释放所讨论的活性化合物时存在适当的条件。

著录项

  • 公开/公告号US8044230B2

    专利类型

  • 公开/公告日2011-10-25

    原文格式PDF

  • 申请/专利权人 TOMASZ W. GLINKA;

    申请/专利号US20070953972

  • 发明设计人 TOMASZ W. GLINKA;

    申请日2007-12-11

  • 分类号C07C229;C07D211/78;C07D285/14;C07D413;A61K31/44;A61K31/41;A61K31/225;

  • 国家 US

  • 入库时间 2022-08-21 18:12:14

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