PHADKE, Avinash,HASHIMOTO, Akihiro,ELY, Richard, James
申请号:
USUS2015/050142
公开号:
WO2016/044243A1
申请日:
2015.09.15
申请国别(地区):
WO
年份:
2016
代理人:
摘要:
The disclosure describes methods of synthesis of phosphoramidate ester derivatives. Also disclosed are morphic forms of (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(5-deutero-2,4- dioxo-3,4-dihydropyrimidin- 1(2H)-yl)-3,4-dihydroxy-4-methyltetrahydrofuran-2- yl)dideuteromethoxy)-(phenoxy)phosphoryl)amino)propanoate and antiviral therapy using (S)- isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(5-deutero-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-3,4- dihydroxy-4-methyltetrahydrofuran-2-yl)dideuteromethoxy)(phenoxy)phosphoryl)amino)- propanoate (e.g., anti-HCV therapies).Linvention concerne des procédés de synthèse de composés desters de phosphoramidate. Linvention concerne également des formes morphiques de (S)-isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(5-deutéro-2,4- dioxo-3,4-dihydropyrimidin- 1(2H)-yl)-3,4-dihydroxy-4-méthyltétrahydrofuran-2- yl)dideutérométhoxy)-(phénoxy)phosphoryl)amino)propanoate et une thérapie antivirale utilisant le (S)- isopropyl 2-(((S)-(((2R,3R,4R,5R)-5-(5-deutéro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-3,4- dihydroxy-4-méthyltétrahydrofuran-2-yl)dideutéromethoxy)(phénoxy)phosphoryl)amino)- propanoate (par exemple des thérapies anti-VHC).