NUCLEOSIDE PHOSPHORAMIDATE

• Main Authors: GANAPATI REDDY PAMULAPATI, RACHAKONDA SUGUNA, CHUN BYOUNG-KWON, ZHANG HAI-REN, MICHAEL JOSEPH SOFIA, ROSS BRUCE S, WANG PEIYUAN
• Format: Patent
• Language: English; Japanese
• Published: 19.11.2015
• Subjects: CHEMISTRY; DERIVATIVES THEREOF; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; SUGARS

PROBLEM TO BE SOLVED: To provide a novel nucleoside phosphoramidate compound for the treatment of viral diseases.SOLUTION: The invention provides crystalline 2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo 3,4-dihydropyrimidine-1(2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl) methoxy)(phenoxy) phosphoryl) amino) propanoic acid (S)-isopropyl represented by the following formula. The compounds are inhibitors of RNA-dependent RNA viral replication and are useful as inhibitors of HCV replication and as therapeutic agents for hepatitis C infection. 【課題】ウイルス性疾患の治療の為の新規ヌクレオシドホスホルアミデート化合物の提供。【解決手段】下記式で表される結晶性２−（（（Ｓ）−（（（２Ｒ，３Ｒ，４Ｒ，５Ｒ）−５−（２，４−ジオキソ−３，４−ジヒドロピリミジン−１（２Ｈ）−イル）−４−フルオロ−３−ヒドロキシ−４−メチルテトラヒドロフラン−２−イル）メトキシ）（フェノキシ）ホスホリル）アミノ）プロパン酸（Ｓ）−イソプロピル。【効果】該化合物は、ＲＮＡ依存性ＲＮＡウイルス複製の阻害剤であり、ＨＣＶ複製の阻害剤として、Ｃ型肝炎感染の治療剤として有用である。【選択図】図１