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    Modified 2',3'-dideoxynucleosides for treatment infections caused by human immunodeficiency virus (HIV) multidrug resistant strains, method of their synthesis and the pharmaceutical agent containing these nucleosides
    2.
    发明公开
    Modified 2',3'-dideoxynucleosides for treatment infections caused by human immunodeficiency virus (HIV) multidrug resistant strains, method of their synthesis and the pharmaceutical agent containing these nucleosides 审中-公开
    方法那些包含修改2”，3'-二脱氧核苷造成的耐人类免疫缺陷病毒的多种药物株（HIV）感染的治疗中的合成和药物，这些核苷

    公开(公告)号：EP2402356A2

    公开(公告)日：2012-01-04

    申请号：EP10172854.1

    申请日：2010-08-15

    申请人： Instytut Biochemii I Biofizyki Pan

    发明人： ZIEMKOWSKI, Przemyslaw ,  MIAZGA, Agnieszka ,  KULIKOWSKI, Tadeusz ,  KLIMKAIT, Thomas ,  LOUVEL, Severine ,  HAMY, Francois ,  Lipniacki, Andrzej ,  PIASEK, Andrzej

    IPC分类号： C07H19/06 ,  A61K31/7052 ,  A61P31/18

    CPC分类号： A61K31/7068 ,  C07H19/06

    摘要： 2',3'-Dideoxy-3'-fluoro-4-thiothymidine (4-SFLT) derivatives according to the invention substituted at 5'-O position of 4-SFLT with 12-tetradodecanoyl, 12-bromododecanoyl, 12-metoxydodecanoyl, 12-ethylothiododecanoyl, 11-ethylothioundecanoyl or 12-azidodocanoyl group (represented by the symbols WA18, WA19, WA21,WA22,WA23 and WA20 in the deCIPhR™ cell system exert high antiviral activity against wild type HIV-1 strain, as well as against its drug and multidrug resistant strains, and moreover very low citotoxicity (CC 50 > 200 µM) and very high selectivity.
    The compounds, because of lack of toxicity may be applied at all AIDS phases i.e. also them the T4 lymphocytes level in patients drops down below 200/ µL of peripheral blood.
    2',3'-Dideoxy-3'-fluoro-4-thiothymidine derivatives according to the invention are synthesized by the transformation of the known compound 2',3'-dideoxy-3'-fluoro-4-thiothymidine (4-SFLT).

    摘要翻译： 2”，3'-二脱氧-3'-氟-4-硫代胸苷（4- SFLT）衍生物gemäß在4- SFLT具有12 tetradodecanoyl，12 bromododecanoyl，12 metoxydodecanoyl的5'-O-位置发明substituiertem， 12 ethylothiododecanoyl，11-ethylothioundecanoyl或12 azidodocanoyl组（用符号WA18，WA19，WA21，WA22，WA23和WA20在deCIPhR“¢电池系统发挥高的抗病毒活性对野生型HIV-1株，以及代表 针对它的药物和多重耐药的菌株，更超过非常低citotoxicity（CC50> 200微米）和非常高的选择性，由于缺乏毒性的化合物，也可以在所有艾滋病阶段应用即，使得它们的T4淋巴细胞患者滴水平 向下下面的外周血200 /微升。2“ 3'-二脱氧-3'-氟-4-硫代胸苷衍生物gemäß本发明，通过已知的化合物2' 的转化合成，3'-二脱氧-3” 氟-4-硫代胸苷（4- SFLT）。