发明名称 HARRINGTONINES SALTS IN THE CRYSTALLINE STATE AND THEIR USE FOR THE PURIFICATION OF THE CORRESPONDING DRUG SUBSTANCE
摘要 The present disclosure concerns harringtonines salts at the crystalline state exhibiting a protonated nitrogen seen in solid state analysis and having general formula 1,;;comprising solvates, made by reacting a cephalotaxine ester alkaloid base having formula 2,;;in which R1 is, but not limited to, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl or heterocycloalkyl, and R2 is, independently, but not limited to H, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl or heterocycloalkyl, with an acid having general formula AH in a non-aqueous crystallization solvent, wherein the said salt has a large water solubility. The disclosure is also related to a process for preparing and purifying these salts and their use as chemotherapeutic drugs.
申请公布号 US2016333023(A1) 申请公布日期 2016.11.17
申请号 US201415109254 申请日期 2014.12.30
申请人 ROBIN Jean-Pierre;RADOSEVIC Nina;BLANCHARD Julie;ROISNEL Thierry;BATAILLE Thierry 发明人 ROBIN Jean-Pierre;RADOSEVIC Nina;BLANCHARD Julie;ROISNEL Thierry;BATAILLE Thierry
分类号 C07D491/147 主分类号 C07D491/147
代理机构 代理人
主权项
地址 Genève CH