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    2,3'-Anhydro-2'-deoxy-5-fluorouridine derivatives with cytotoxic activity, a manufacturing process and application
    3.
    发明公开
    2,3'-Anhydro-2'-deoxy-5-fluorouridine derivatives with cytotoxic activity, a manufacturing process and application 审中-公开
    具有细胞毒活性的2,3'-脱氢-2'-脱氧-5-氟尿苷衍生物，生产方法和应用

    公开(公告)号：EP3172216A1

    公开(公告)日：2017-05-31

    申请号：EP14772458.7

    申请日：2014-08-22

    申请人： Adam Mickiewicz University

    发明人： CELEWICZ, Lech ,  KACPRZAK, Karol ,  LEWANDOWSKA, Marta ,  RUSZKOWSKI, Piotr

    IPC分类号： C07F9/24 ,  C07H19/073 ,  A61K33/42 ,  A61P35/00

    CPC分类号： C07H19/10 ,  A61K33/42 ,  C07F9/24 ,  C07F9/6561 ,  C07H19/073

    摘要： The subject matter of the invention is novel 2,3′-anhydro-2′-deoxy-5-fluorouridine derivatives of general formula 1 where R is a trifluoromethyl, 2,2,2-trifluoroethyl, difluoromethyl, perfluoroethyl, 1-fluoroethyl, 2-fluoroethyl, 1,1-difluoroethyl, 1,2-difluoroethyl, 2,2-difluoroethyl, 1,1,2-trifluoroethyl, 1,2,2-trifluoroethyl, 1,1,2,2-tetrafluoroethyl, 1,2,2,2-tetrafluoroethyl group. In a second aspect, the subject matter of the invention is a process for the manufacture of 2,3′-anhydro-2′-deoxy-5-fluorouridine derivatives of general formula 1. In a third aspect, the subject matter of the invention is an application of 2,3′-anhydro-2′-deoxy-5-fluorouridine derivatives of general formula 1 in the anticancer treatment of breast cancer, cervical cancer, lung cancer and nasopharynx cancer.

    摘要翻译： 本发明的主题是通式1的新的2,3'-脱水-2'-脱氧-5-氟尿苷衍生物，其中R是三氟甲基，2,2,2-三氟乙基，二氟甲基，全氟乙基，1-氟乙基， 2-氟乙基，1,1-二氟乙基，1,2-二氟乙基，2,2-二氟乙基，1,1,2-三氟乙基，1,2,2-三氟乙基，1,1,2,2-四氟乙基， 2,2,2-四氟乙基。 第二方面，本发明的主题是制备通式1的2,3'-脱水-2'-脱氧-5-氟尿苷衍生物的方法。在第三方面，本发明的主题 是通式1的2,3'-脱水-2'-脱氧-5-氟尿苷衍生物在乳腺癌，宫颈癌，肺癌和鼻咽癌的抗癌治疗中的应用。

    APPLICATION OF CINCHONA ALKALOID DERIVATIVES AS CYTOTOXIC COMPOUNDS
    6.
    发明公开
    APPLICATION OF CINCHONA ALKALOID DERIVATIVES AS CYTOTOXIC COMPOUNDS 审中-公开
    USE金鸡纳生物碱衍生物作为细胞毒性化合物的

    公开(公告)号：EP3104859A1

    公开(公告)日：2016-12-21

    申请号：EP14716998.1

    申请日：2014-03-04

    申请人： Adam Mickiewicz University

    发明人： CELEWICZ, Lech ,  KACPRZAK, Karol ,  RUSZKOWSKI, Piotr

    IPC分类号： A61K31/4709 ,  A61P35/00

    CPC分类号： A61K31/49

    摘要： The subject matter of the invention is the application of
    9-O -propargyl ethers of cinchona alkaloids of general formula represented by formula (1) wherein respective ethers have the following absolute configuration at C-8 and C-9 atoms:
    (8R,9S) –cinchonine configuration or
    (8S,9R ) –cinchonidine configuration or
    (8R,9R) –9-epicinchonine configuration or
    (8S,9S) –9-epicinchonidine configuration for the manufacture of drugs used in cancer chemotherapy.