Hugh Griffith,Christopher McGuigan,Magdalena Slusarczyk,Michaela Serpi,Valentina Ferrari
申请号:
US15308491
公开号:
US10662213B2
申请日:
2015.06.25
申请国别(地区):
US
年份:
2020
代理人:
摘要:
This invention relates to a prodrug of the monophosphate nucleotide of the well-known oncology drug gemcitabine. Specifically, it relates to gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate when present as a single phosphate diastereoisomer and, in particular, it relates to the (S)-phosphate diastereoisomer which offers a remarkable and unexpected increase in solubility relative to the (R)-diastereoisomer. The (S)-phosphate epimer is also preferentially taken up into cyclodextrin solutions over the (R)-diastereoisomer.