申请人:Zhong Bohua
公开号:US20120322764A1
公开(公告)日:2012-12-20
The present invention relates to an acyclic nucleoside phosphonate derivative and medical uses thereof. Specifically, the present invention relates to an acyclic nucleoside phosphonate derivative of Formula I having strong potency against viruses, such as hepatitis B virus, and low cytotoxicity, or a pharmaceutically acceptable salt, isomer, hydrate or solvate thereof, wherein R
1
is H or methyl; each R
2
is independently —R
3
or —OR
3
, each R
3
is independently C
1
-C
8
alkyl, C
3
-C
8
cycloalkyl. The present invention further relates to a process for preparing the compounds of Formula I, a pharmaceutical composition comprising the compound, and the medical uses of the compound. The acyclic nucleoside phosphonate derivative of the present invention has activity against virus such as hepatitis B virus and good in vivo behavioral traits.
本发明涉及一种无环核苷酸膦酸酯衍生物及其医药用途。具体而言,本发明涉及一种式I的无环核苷酸膦酸酯衍生物,其对病毒(如乙型肝炎病毒)具有强效力且细胞毒性低,或其药学上可接受的盐、异构体、水合物或溶剂化物,其中R1为H或甲基;每个R2独立地是—R3或—OR3,每个R3独立地是C1-C8烷基、C3-C8环烷基。本发明还涉及制备式I化合物的方法、包含该化合物的制药组合物以及该化合物的医药用途。本发明的无环核苷酸膦酸酯衍生物具有对乙型肝炎病毒等病毒的活性和良好的体内行为特性。