A CONJUGATE COMPRISING OXYNTOMODULIN AND AN IMMUNOGLOBULIN FRAGMENT, AND USE THEREOF
    65.
    发明公开
    A CONJUGATE COMPRISING OXYNTOMODULIN AND AN IMMUNOGLOBULIN FRAGMENT, AND USE THEREOF 审中-公开
    结合奥昔布霉素和免疫球蛋白片段及其用途

    公开(公告)号:EP2721062A4

    公开(公告)日:2014-11-12

    申请号:EP12801247

    申请日:2012-06-15

    摘要: The present invention relates to a conjugate comprising oxyntomodulin, an immunoglobulin Fc region, and non-peptidyl polymer wherein the conjugate being obtainable by covalently linking oxyntomodulin to immunoglobulin Fc region via non-peptidyl polymer, and a pharmaceutical composition for the prevention or treatment of obesity comprising the conjugates. The conjugate comprising oxyntomodulin and the immunoglobulin Fc of the present invention reduces food intake, suppresses gastric emptying, and facilitates lipolysis without side-effects, unlike native oxyntomodulin, and also shows excellent receptor-activating effects and long-term sustainability, compared to native oxyntomodulin. Thus, it can be widely used in the treatment of obesity with safety and efficacy.

    摘要翻译: 本发明涉及包含胃泌酸调节蛋白,免疫球蛋白Fc区和非肽基聚合物的缀合物,其中通过非肽基聚合物共价连接胃泌酸调节蛋白与免疫球蛋白Fc区域可获得的缀合物和用于预防或治疗肥胖症的药物组合物 包括缀合物。 与天然胃泌酸调节蛋白不同,包含胃泌酸调节素和本发明的免疫球蛋白Fc的缀合物与天然胃泌酸调节素相比减少食物摄入,抑制胃排空,并且促进无副作用的脂肪分解,并且与天然胃泌酸调节素相比也显示出优异的受体激活作用和长期可持续性 。 因此,可广泛用于治疗肥胖症的安全性和有效性。

    METHOD FOR THE PREPARATION OF 2'-DEOXY-2',2'-DIFLUOROCYTIDINE
    70.
    发明公开
    METHOD FOR THE PREPARATION OF 2'-DEOXY-2',2'-DIFLUOROCYTIDINE 审中-公开
    VERFAHREN ZUR HERSTELLUNG VON 2'-脱氧-2',2'-二氟胞嘧啶

    公开(公告)号:EP1831236A4

    公开(公告)日:2013-11-20

    申请号:EP05823850

    申请日:2005-12-29

    IPC分类号: C07H19/04

    CPC分类号: C07H19/04

    摘要: This invention relates to an improved method for stereoselectively preparing 2¢¥-deoxy-2¢¥,2¢¥-difluorocytidine of formula (I), which comprises the steps of reacting a 1-halo ribofuranose compound of formula (III) with a nucleobase of formula (IV) in a solvent to obtain a nucleoside of formula (II) with removing the silyl halide of formula (V) produced during the reaction; and deprotecting the nucleoside of formula (II) to obtain 2¢¥-deoxy-2¢¥,2¢¥-difluorocytidine of formula (I).

    摘要翻译: 本发明涉及立体选择性地制备式(I)的2β-脱氧-2β,2β-二氟胞苷的改进方法,该方法包括使式(III)的1-卤代呋喃核糖化合物与式 (IV)的核碱在溶剂中反应以获得式(II)的核苷,同时除去在反应期间产生的式(V)的甲硅烷基卤化物; (II)的核苷去保护,得到式(I)的2' - 脱氧-2',2'' - 二氟胞苷。