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    C- ARYL GLYCOSID DERIVATIVES, PHARMACEUTICAL COMPOSITION, PREPARATION PROCESS AND USES THEREOF
    5.
    发明申请
    C- ARYL GLYCOSID DERIVATIVES, PHARMACEUTICAL COMPOSITION, PREPARATION PROCESS AND USES THEREOF 有权
    C- ARYL GLYCOSID衍生物，药物组合物，制备方法及其用途

    公开(公告)号：US20170037038A1

    公开(公告)日：2017-02-09

    申请号：US15304493

    申请日：2015-04-01

    申请人： SHANGHAI DE NOVO PHARMATECH CO. LTD.

    发明人： Daxin GAO ,  Heping YANG ,  Pei WANG

    IPC分类号： C07D407/12 ,  A61K31/351 ,  A61K45/06

    CPC分类号： C07D407/12 ,  A61K31/351 ,  A61K45/06 ,  C07H7/04 ,  Y02P20/55

    摘要： This invention relates to a kind of C-aryl glycoside derivatives, its pharmaceutical compositions, preparation methods, and uses thereof. The preparation method comprises: method 1: in a solvent, deprotecting the acetyl protecting groups of compound 1-f in the presence of a base; method 2: 1) compound 2-g reacts with via Mitsunobu reaction; 2) deprotecting the acetyl protecting groups of compound 2-f obtained from step 1; method 3: 1) compound 2-g reacts with via nucleophilic substitution reaction; 2) deprotecting the acetyl protecting groups of compound 3-f obtained from step 1. The pharmaceutical composition comprises a kind of C-aryl glycoside derivatives; it's pharmaceutically acceptable salts and/or prodrugs thereof and excipient thereof. This invention further relates to a kind of C-aryl glycoside derivatives, it's pharmaceutically acceptable salts or pharmaceutical compositions thereof for the use in preparation of a SGLT inhibitor. The C-aryl glycoside derivatives of this invention provides a new direction for the study of SGLT inhibitors.

    摘要翻译： 本发明涉及一种C-芳基糖苷衍生物，其药物组合物，制备方法和用途。 制备方法包括：方法1：在溶剂中，在碱的存在下脱保护化合物1-f的乙酰基保护基; 方法2：1）化合物2-g通过Mitsunobu反应反应; 2）从步骤1获得的化合物2-f的乙酰基保护基脱保护; 方法3：1）化合物2-g通过亲核取代反应反应; 2）使从步骤1获得的化合物3-f的乙酰基保护基脱保护。药物组合物包含一种C-芳基糖苷衍生物; 其药学上可接受的盐和/或其前药和赋形剂。 本发明还涉及一种C-芳基糖苷衍生物，其用于制备SGLT抑制剂的药学上可接受的盐或其药物组合物。 本发明的C-芳基糖苷衍生物为研究SGLT抑制剂提供了新的方向。

    Dapagliflozin crystalline form and preparation method thereof
    6.
    发明授权
    Dapagliflozin crystalline form and preparation method thereof 有权
    达格列in晶形及其制备方法

    公开(公告)号：US09550747B2

    公开(公告)日：2017-01-24

    申请号：US15117533

    申请日：2015-01-19

    申请人： Jiangsu Hansoh Pharmaceutical Group Co., Ltd.

    发明人： Xifeng Zhu ,  Xiaobi Li ,  Tiancheng Zhang ,  Fuping Yuan

    IPC分类号： C07H7/04 ,  C07H1/06 ,  C07D309/10

    CPC分类号： C07D309/10 ,  A61K31/70 ,  C07B2200/13 ,  C07H1/06 ,  C07H7/04

    摘要： The present invention relates to a new crystalline form of dapagliflozin represented by formula (I). The crystalline form has a characteristic absorption peak at about 4.318 (20.45) in an X-ray powder diffraction pattern shown by angle 2 theta and interplanar spacing (value d). It can be prepared by dissolving dapagliflozin in good organic solvents, adding poor solvents, stirring to crystallization, filtering and drying. The new crystalline form of dapagliflozin of the present invention has the following superior features: good solubility, low hygroscopicity, high stability and good preparation reproducibility.

    摘要翻译： 本发明涉及由式（I）表示的新的达曲格列霉素结晶形式。 X射线粉末衍射图中所示的晶体形式在大约4.318（20.45）处具有特征吸收峰，如图2θ和晶面间距（值d）所示。 可以通过将达格列齐溶解成良好的有机溶剂，加入不良溶剂，搅拌，结晶，过滤和干燥来制备。 本发明的新型达曲格列结晶形式具有以下优异的特征：溶解性好，吸湿性低，稳定性高，制备再现性好。

    DAPAGLIFLOZIN CRYSTALLINE FORM AND PREPARATION METHOD THEREOF
    7.
    发明申请
    DAPAGLIFLOZIN CRYSTALLINE FORM AND PREPARATION METHOD THEREOF 有权
    DAPAGLIFLOZIN晶体形式及其制备方法

    公开(公告)号：US20160347731A1

    公开(公告)日：2016-12-01

    申请号：US15117533

    申请日：2015-01-19

    申请人： Jiangsu Hansoh Pharmaceutical Group Co., Ltd.

    发明人： Xifeng Zhu ,  Xiaobi Li ,  Tiancheng Zhang ,  Fuping Yuan

    IPC分类号： C07D309/10

    CPC分类号： C07D309/10 ,  A61K31/70 ,  C07B2200/13 ,  C07H1/06 ,  C07H7/04

    摘要： A crystalline form of dapagliflozin represented by formula (I) is provided. The crystalline form has a characteristic absorption peak in an X-ray powder diffraction pattern at a diffraction angle 2θ and interplanar spacing (value d) at about 4.318 (20.45) in an X-ray powder diffraction pattern. The crystalline form can be prepared by dissolving dapagliflozin in good organic solvents, adding poor solvents, stirring to crystallization, filtering and drying. The provided crystalline form of dapagliflozin has the following features: good solubility, low hygroscopicity, high stability and good preparation reproducibility.

    摘要翻译： 本发明涉及由式（I）表示的新的达曲格列霉素结晶形式。 X射线粉末衍射图中所示的晶体形式在大约4.318（20.45）处具有特征吸收峰，如图2θ和晶面间距（值d）所示。 可以通过将达格列齐溶解成良好的有机溶剂，加入不良溶剂，搅拌，结晶，过滤和干燥来制备。 本发明的新型达曲格列结晶形式具有以下优异的特征：溶解性好，吸湿性低，稳定性高，制备再现性好。

    GLUCOPYRANOSIDE COMPOUND
    9.
    发明申请
    GLUCOPYRANOSIDE COMPOUND 审中-公开
    葡萄糖苷化合物

    公开(公告)号：US20160108078A1

    公开(公告)日：2016-04-21

    申请号：US14981728

    申请日：2015-12-28

    申请人： MITSUBISHI TANABE PHARMA CORPORATION

    发明人： Sumihiro NOMURA ,  Eiji KAWANISHI ,  Kiichiro UETA

    IPC分类号： C07H19/056 ,  C07H19/044 ,  C07H19/04 ,  C07H19/048 ,  C07H7/04 ,  C07H7/06

    CPC分类号： C07H19/056 ,  A61K31/7042 ,  A61K31/7056 ,  A61K38/24 ,  A61K38/28 ,  A61K45/06 ,  C07H7/04 ,  C07H7/06 ,  C07H19/04 ,  C07H19/044 ,  C07H19/048 ,  A61K2300/00

    摘要： A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); or a pharmaceutically acceptable salt thereof, or a prodrug thereof.

    摘要翻译： 下式的化合物：其中环A和环B是：（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环，或 任选取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环或任选取代的不饱和稠环杂双环，或（3）环A是任选取代的不饱和稠合杂双环 环和环B独立地是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环; X是碳原子或氮原子; Y为 - （CH 2）n - （n为1或2）; 或其药学上可接受的盐，或其前药。