This invention provides modified rapamycins that have specific monosaccharide(s), oligosaccharide(s), pseudosugar(s) or derivatives thereof attached through a linker to create rapamycin carbohydrate derivatives having enhanced pharmacokinetic and/or pharmacodynamic profiles. For example, administration of the rapamycin carbohydrate derivative results in altered pharmacokinetic profiles and reduced toxicities. Thus, the present invention provides compounds with characteristics that are distinct from other drugs in its class such as rapamycin.
这项发明提供了经过修改的
雷帕霉素,其中通过连接剂连接了特定的
单糖,
寡糖,假糖或其衍
生物,从而创建具有增强药代动力学和/或药效学特性的
雷帕霉素糖衍
生物。例如,给予
雷帕霉素糖衍
生物的治疗导致了改变的药代动力学特性和减少的毒性。因此,本发明提供了具有与其他类似药物(如
雷帕霉素)不同特性的化合物。