公开(公告)号：US20030220290A1

公开(公告)日：2003-11-27

申请号：US10437802

申请日：2003-05-13

申请人： Centre National da la Reserche Scientifique ,  L'Universite Montpellier II ,  Idenix Pharmaceuticals Inc.

发明人： Gilles Gosselin ,  Jean-Louis Imbach ,  Martin L. Bryant

IPC分类号： A61K031/7076 ,  A61K031/7072

CPC分类号： C07H19/16 ,  A61K31/70 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  C07H19/06 ,  A61K2300/00

摘要： This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2null-deoxy-null-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2null-deoxy-null-L-erythro-pentofuranonucleoside has the formula: 1 wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2null-deoxy-null-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2null-deoxy-null-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.

摘要翻译： 本发明涉及一种用于治疗感染乙型肝炎的宿主的方法，其包括施用有效量的抗HBV生物活性2'-脱氧-β-L-赤 - 戊呋喃核苷或其药学上可接受的盐或前药，其中 2'-脱氧-β-L-赤 - 戊呋喃核苷具有下式：其中R选自H，直链，支链或环状烷基，CO-烷基，CO-芳基，CO-烷氧基烷基，CO-芳氧基烷基 烷基磺酰基，芳基磺酰基，芳烷基磺酰基，氨基酸残基，单，二或三磷酸酯，或磷酸酯衍生物; 并且BASE是嘌呤或嘧啶碱基，其可任选被取代。 2'-脱氧-β-L-赤 - 戊呋喃核苷或其药学上可接受的盐或前药可以单独或与其它2'-脱氧-β-L-赤 - 戊呋喃核苷组合或与另一种抗 - 乙型肝炎药。