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    2′-Fluoronucleosides
    6.
    发明授权
    2′-Fluoronucleosides 有权
    2'-氟核苷

    公开(公告)号：US07307065B2

    公开(公告)日：2007-12-11

    申请号：US10796529

    申请日：2004-03-08

    申请人： Raymond F. Schinazi ,  Dennis C. Liotta ,  Chung K. Chu ,  J. Jeffrey McAtee ,  Junxing Shi ,  Yongseok Choi ,  Kyeong Lee ,  Joon H. Hong

    发明人： Raymond F. Schinazi ,  Dennis C. Liotta ,  Chung K. Chu ,  J. Jeffrey McAtee ,  Junxing Shi ,  Yongseok Choi ,  Kyeong Lee ,  Joon H. Hong

    IPC分类号： A61K38/00 ,  A01N61/00 ,  C07H1/00 ,  C07G3/00

    CPC分类号： A61K31/7076 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/708 ,  C07D405/04 ,  C07D473/00 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16

    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; R1 is OH, H, OR3, N3, CN, halogen, including F, or CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy, and base refers to a purine or pyrimidine base; R2 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 R2 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 R3 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.

    摘要翻译： 公开了一类可用于治疗乙型肝炎感染，丙型肝炎感染，HIV和异常细胞增殖（包括肿瘤和癌症）的2'-氟 - 核苷化合物。 所述化合物具有以下通式：其中碱是嘌呤或嘧啶碱; R 1是OH，H，OR 3，N 3，CN，卤素，包括F或CF 3 N ，低级烷基，氨基，低级烷基氨基，二（低级）烷基氨基或烷氧基，碱是指嘌呤或嘧啶碱基; R 2是H，磷酸盐，包括单磷酸盐，二磷酸盐，三磷酸盐或稳定化的磷酸盐前药; 酰基或其它药学上可接受的离去基团，其当在体内施用时能够提供其中R 2是H或磷酸酯的化合物; 磺酸酯，包括烷基或芳基烷基磺酰基，包括甲磺酰基，苄基，其中苯基任选被一个或多个取代基取代，如上述芳基定义中所述，脂质，氨基酸，肽或胆固醇; 并且R 3是酰基，烷基，磷酸酯或其它药学上可接受的离去基团，当其在体内施用时，其能够被切割成母体化合物或其药学上可接受的盐。