发明名称 2'-Fluoronucleosides
摘要 A class of 2'-fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae: wherein Base is a purine or pyrimidine base; R<SUP>1 </SUP>is OH, H, OR<SUP>3</SUP>, N<SUB>3</SUB>, CN, halogen, including F, or CF<SUB>3</SUB>, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy, and base refers to a purine or pyrimidine base; R<SUP>2 </SUP>is H, phosphate, including monophosphate, diphosphate, triphosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of providing a compound wherein R<SUP>2 </SUP>is H or phosphate; sulfonate ester including alkyl or arylalkyl sulfonyl including methanesulfonyl, benzyl, wherein the phenyl group is optionally substituted with one or more substituents as described in the definition of aryl given above, a lipid, an amino acid, peptide, or cholesterol; and R<SUP>3 </SUP>is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of being cleaved to the parent compound, or a pharmaceutically acceptable salt thereof.
申请公布号 US7307065(B2) 申请公布日期 2007.12.11
申请号 US20040796529 申请日期 2004.03.08
申请人 EMORY UNIVERSITY;THE UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC. 发明人 SCHINAZI RAYMOND F.;LIOTTA DENNIS C.;CHU CHUNG K.;MCATEE J. JEFFREY;SHI JUNXING;CHOI YONGSEOK;LEE KYEONG;HONG JOON H.
分类号 A61K38/00;C07D239/47;A01N61/00;A61K31/505;A61K31/506;A61K31/52;A61K31/522;A61K31/7042;A61K31/7052;A61K31/7064;A61K31/7068;A61K31/7072;A61K31/7076;A61K31/708;A61P31/20;A61P35/00;C07D405/04;C07D473/00;C07D473/18;C07D473/34;C07F7/18;C07F9/547;C07G3/00;C07H1/00;C07H19/06;C07H19/10;C07H19/16;C07H19/20;C07H19/207 主分类号 A61K38/00
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