A vinca alkaloid compound that is substituted at the 20'-position with a urea or thiourea group is disclosed. The urea's proximal nitrogen atom bonded to the 20'-position carbon atom is secondary, whereas the distal nitrogen atom can be unsubstituted only when the compound contains an optionally present 10'-fluoro substituent, and is otherwise preferably mono- or di-substituted. Methods of preparing the compounds are disclosed as are compositions for their use and methods of treatment using a compound.
本发明涉及一种在20'-位置上用
脲或
硫脲基取代的长春花
生物碱化合物。
脲的近端氮原子与20'-位置碳原子结合是二级的,而远端氮原子只有在该化合物含有可选的10'-
氟取代基时才可能未取代,否则最好是单取代或双取代。揭示了制备该化合物的方法,以及使用该化合物的组合物和治疗方法。