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    SALTS OF CONJUGATES FOR CANCER THERAPY
    2.
    发明申请
    SALTS OF CONJUGATES FOR CANCER THERAPY 有权

    公开(公告)号：US20210395285A1

    公开(公告)日：2021-12-23

    申请号：US17460335

    申请日：2021-08-30

    申请人： Biosight Ltd.

    发明人： Stela GENGRINOVITCH

    IPC分类号： C07H1/00 ,  C07H19/09

    摘要： The present invention relates to pharmaceutically acceptable salts of conjugates comprising a chemotherapeutic drug and an amino acid or a derivative thereof, which are readily taken up by a target cell and reduce side effects induced by the chemotherapeutic drug. In particular, the present invention relates to pharmaceutically acceptable salts of conjugates comprising cytidine analog drugs and aspartic or glutamic acid and analogs thereof, pharmaceutical compositions comprising these conjugates and use thereof for the treatment of cancer or a pre-cancer condition or disorder.

    RADIOLABELED NUCLEOSIDE ANALOGUE, AND PREPARATION METHOD AND USE THEREOF
    4.
    发明申请
    RADIOLABELED NUCLEOSIDE ANALOGUE, AND PREPARATION METHOD AND USE THEREOF 审中-公开
    放射性核苷类似物及其制备方法及其用途

    公开(公告)号：US20120178919A1

    公开(公告)日：2012-07-12

    申请号：US13194247

    申请日：2011-07-29

    申请人： HSIN-ELL WANG ,  CHIH-YUAN LIN ,  WEI-TI KUO ,  CHUAN-LIN CHEN ,  MEI-HUI WANG ,  HUNG-MAN YU ,  MAO-CHI WENG ,  YU CHANG ,  WUU-JYH LIN

    发明人： HSIN-ELL WANG ,  CHIH-YUAN LIN ,  WEI-TI KUO ,  CHUAN-LIN CHEN ,  MEI-HUI WANG ,  HUNG-MAN YU ,  MAO-CHI WENG ,  YU CHANG ,  WUU-JYH LIN

    IPC分类号： C07H19/067 ,  C07H19/09 ,  C07H19/073

    CPC分类号： C07H19/067 ,  C07B59/005 ,  C07H19/073 ,  C07H19/09

    摘要： A radiolabeled nucleoside analogue is provided, which includes radioactive iodine 123I/131I, and a nucleoside analogue selected from a group consisting of cytidine, thymidine, uridine, and a derivative thereof. A method for preparing the radiolabeled nucleoside analogue, and a use thereof are further provided. The nucleoside analogue, prepared through the preparation method with a short synthesis time and a high radiochemical yield, has a long in vivo physiological half life and a high stability in serum, and, as a radiopharmaceutical composition, is useful in development of tumor proliferation diagnosis or therapy prognosis evaluation, and further assists in observation of long-time in vivo metabolism of a drug.

    摘要翻译： 提供放射性标记的核苷类似物，其包括放射性碘123I / 131I和选自胞苷，胸苷，尿苷及其衍生物的核苷类似物。 还提供了制备放射性标记的核苷类似物的方法及其用途。 通过制备方法制备的核苷类似物，具有短的合成时间和高放射化学产率，具有长的体内生理半衰期和高血清稳定性，作为放射性药物组合物，可用于肿瘤增生诊断的发展 或治疗预后评估，进一步有助于观察药物的长时间体内代谢。

    L-nucleic acid derivatives and process for the synthesis thereof
    6.
    发明授权
    L-nucleic acid derivatives and process for the synthesis thereof 有权
    L-核酸衍生物及其合成方法

    公开(公告)号：US07125983B2

    公开(公告)日：2006-10-24

    申请号：US10433004

    申请日：2001-11-29

    申请人： Hajime Iizuka ,  Kazuhiko Togashi ,  Tsuneji Suzuki

    发明人： Hajime Iizuka ,  Kazuhiko Togashi ,  Tsuneji Suzuki

    IPC分类号： C07H19/06 ,  C07H19/09

    CPC分类号： C07D498/04 ,  C07D498/14 ,  C07H9/06 ,  C07H19/06 ,  C07H19/073 ,  C07H19/09

    摘要： A novel method has been found to produce 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine as a novel useful intermediate compound. A novel method has been further found to produce thymidine from 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine. A novel method has been further found to L-2′-deoxyribose derivatives as a useful synthetic intermediate through L-2,2′-anhydro-5,6-dihydrocyclouridine derivative. According to these methods, synthesis of various L-nucleic acid derivatives, synthesis of which has been difficult till now.

    摘要翻译： 已经发现一种新的方法生产2,2'-脱水-1-（β-L-阿拉伯呋喃糖基）胸腺嘧啶作为新的有用的中间体化合物。 已经进一步发现一种从2,2'-脱水-1-（β-L-阿拉伯呋喃糖基）胸腺嘧啶产生胸苷的新方法。 通过L-2,2'-脱水-5,6-二氢环尿苷衍生物，进一步发现L-2'-脱氧核糖衍生物作为有用的合成中间体的新方法。 根据这些方法，合成各种L-核酸衍生物，其合成迄今难以实现。