Method for synthesis of Roxadustat and intermediate compounds thereof

    公开(公告)号:US11465970B2

    公开(公告)日:2022-10-11

    申请号:US16772535

    申请日:2018-12-14

    发明人: Yongxiang Xu

    IPC分类号: C07D217/26

    摘要: The present application provides a method for synthesis of Roxadustat. A compound as represented by formula (VIII) is used as a raw material, and is reacted with phenol, a vinyl-containing ether, an acid, hydroxylamine, and then the product is reacted with glycine. In addition, the present application also provides intermediate compounds as represented by formula (IX), formula (XI), formula (XII), formula (IV), and formula (V) for synthesis of Roxadustat. Herein, details of the substituents involved in formula (VIII), formula (IX), formula (XI), and formula (XII) are stated in the description

    SYNTHESIS PROCESS OF DASATINIB AND INTERMEDIATE THEREOF
    4.
    发明申请
    SYNTHESIS PROCESS OF DASATINIB AND INTERMEDIATE THEREOF 有权
    DASATINIB的合成方法及其中间体

    公开(公告)号:US20130030177A1

    公开(公告)日:2013-01-31

    申请号:US13576637

    申请日:2011-01-30

    IPC分类号: C07D417/14 C07D417/12

    CPC分类号: C07D417/12

    摘要: Synthesis process of dasatinib is disclosed, which includes the step of reacting the compound of formula I with that of formula II to obtain the compound of formula III. Also disclosed is the compound of formula III which is used as an intermediate for synthesizing dasatinib. The substituents of R1, R2, R3 or R4 in formulae I, II or III are defined as in the description.

    摘要翻译: 公开了达沙替尼的合成方法,其包括使式I化合物与式II化合物反应以获得式III化合物的步骤。 还公开了用作合成达沙替尼的中间体的式III化合物。 式I,II或III中的R 1,R 2,R 3或R 4的取代基如描述中所定义。

    Novel and Highly Stereoselective Process for Preparing Gemcitabine and Intermediates Thereof
    6.
    发明申请
    Novel and Highly Stereoselective Process for Preparing Gemcitabine and Intermediates Thereof 有权
    用于制备吉西他滨及其中间体的新型和高度立体选择性方法

    公开(公告)号:US20100179314A1

    公开(公告)日:2010-07-15

    申请号:US12601942

    申请日:2007-09-07

    IPC分类号: C07H19/073 C07H13/00

    CPC分类号: C07H19/073 C07H3/08

    摘要: The present invention provides a novel and highly stereoselective process for preparing gemcitabine, which is suitable for industrial production, wherein, it includes the following reactions. Additionally, the invention discloses the key intermediates. The definition for the groups of G1, G2, G3, G4, and G5 are described in the specification.

    摘要翻译: 本发明提供了一种适用于工业生产的吉西他滨的新型高度立体选择性方法,其中包括以下反应。 此外,本发明公开了关键中间体。 说明书中描述了G1,G2,G3,G4和G5组的定义。

    Pharmaceutical formulations comprising voriconazole and processes for preparation thereof
    7.
    发明授权
    Pharmaceutical formulations comprising voriconazole and processes for preparation thereof 有权
    包含伏立康唑的药物制剂及其制备方法

    公开(公告)号:US08586592B2

    公开(公告)日:2013-11-19

    申请号:US13140900

    申请日:2009-12-31

    申请人: Yongxiang Xu

    发明人: Yongxiang Xu

    IPC分类号: A61K31/506 A61P31/00

    摘要: The present invention provides a pharmaceutical formulation comprising voriconazole or a pharmaceutically acceptable derivative thereof, and an excipient of formula (I), i.e., monomethoxy poly(ethylene glycol)-poly (D,L-lactic acid) block copolymers (mPEG-PDLLA). The pharmaceutical formulation of the present invention has been shown to be stable and safe by experiments.

    摘要翻译: 本发明提供了包含伏立康唑或其药学上可接受的衍生物和式(I)的赋形剂,即单甲氧基聚(乙二醇) - 聚(D,L-乳酸)嵌段共聚物(mPEG-PDLLA) 。 通过实验证明本发明的药物制剂是稳定和安全的。

    Pharmaceutical Formulations Comprising Voriconazole and Processes for Preparation Thereof
    9.
    发明申请
    Pharmaceutical Formulations Comprising Voriconazole and Processes for Preparation Thereof 有权
    包含伏立康唑的药物制剂及其制备方法

    公开(公告)号:US20110257197A1

    公开(公告)日:2011-10-20

    申请号:US13140900

    申请日:2009-12-31

    申请人: Yongxiang Xu

    发明人: Yongxiang Xu

    IPC分类号: A61K31/506 A61P31/00

    摘要: The present invention provides a pharmaceutical formulation comprising voriconazole or a pharmaceutically acceptable derivative thereof, and an excipient of formula (I), i.e., monomethoxy poly(ethylene glycol)-poly (D,L-lactic acid) block copolymers (mPEG-PDLLA). The pharmaceutical formulation of the present invention has been shown to be stable and safe by experiments.

    摘要翻译: 本发明提供了包含伏立康唑或其药学上可接受的衍生物和式(I)的赋形剂,即单甲氧基聚(乙二醇) - 聚(D,L-乳酸)嵌段共聚物(mPEG-PDLLA) 。 通过实验证明本发明的药物制剂是稳定和安全的。