Novel human thrombopoietin mutein
    25.
    发明申请
    Novel human thrombopoietin mutein 审中-公开
    新型人血小板生成素突变蛋白

    公开(公告)号:US20030228666A1

    公开(公告)日:2003-12-11

    申请号:US10441729

    申请日:2003-05-20

    CPC分类号: C07K14/524

    摘要: The present invention relates to novel human thrombopoietin (; hTPO) derivatives, and to process of preparation thereof. Particularly, sugar chains are introduced into native hTPO by substituting amino acids such as asparagine for amino acids at specific positions in native hTPO, preparing novel hTPO derivatives with high activities enhancing the platelet production in vivo. Therefore, the novel hTPO derivatives of this invention may be useful for the treatment of thrombocytopenia associated with anticancer therapy or the transplantation of bone marrow.

    摘要翻译: 本发明涉及新型人血小板生成素(; hTPO)衍生物及其制备方法。 特别地,通过用氨基酸例如天门冬酰胺在天然hTPO中的特定位置取代氨基酸,将糖链引入天然hTPO,制备具有增强体内血小板产生的高活性的新型hTPO衍生物。 因此,本发明的新型hTPO衍生物可用于治疗与抗癌治疗或骨髓移植相关的血小板减少症。

    Method for producing intermediate useful for synthesis of SGLT inhibitor

    公开(公告)号:US11661406B2

    公开(公告)日:2023-05-30

    申请号:US17266844

    申请日:2019-08-09

    IPC分类号: C07D307/79

    CPC分类号: C07D307/79

    摘要: A method of preparing an intermediate useful for the synthesis of a diphenylmethane derivative that can be used as an SGLT inhibitor is described. A method of synthesizing a compound of Formula 7 can address problems of existing synthesis processes requiring the synthesis of the Grignard reagent and management of related substances. In addition, the method can minimize the generation of related substances, and thus does not require reprocessing of reaction products, thereby simplifying the process. Accordingly, the production yield of a diphenylmethane derivative can be maximized.

    INTERMEDIATE USEFUL FOR SYNTHESIS OF SGLT INHIBITOR AND METHOD FOR PREPARING SGLT INHIBITOR USING SAME

    公开(公告)号:US20230096670A1

    公开(公告)日:2023-03-30

    申请号:US17799054

    申请日:2021-02-26

    IPC分类号: C07D407/04 C07D307/79

    摘要: An intermediate useful for the synthesis of an SGLT inhibitor and a method for preparing an SGLT inhibitor are provided. By employing an intermediate having Chemical Formula 5, the difficulty of purification with existing processes can be solved, the quality requirements for related substances can be achieved with only one purification step, and the quality control problem in each step can be solved by performing several steps in situ. A method for synthesizing a compound of Chemical Formula 1 by using a compound of Chemical Formula 5 enables purification in an earlier step, thereby solving the problems of existing synthesis processes, in which the quality requirements for related substances were difficult to control step-by-step due to a continuous process, thereby minimizing the amount of related substances in the final product. In addition, the yield of a diphenylmethane derivative according to Chemical Formula 1 is increased.