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    CRYSTAL FORM OF DABIGATRAN ETEXILATE MESYLATE AND PREPARATION METHOD AND USE THEREOF
    3.
    发明公开
    CRYSTAL FORM OF DABIGATRAN ETEXILATE MESYLATE AND PREPARATION METHOD AND USE THEREOF 审中-公开
    侠盗猎车手侠盗猎车手

    公开(公告)号：EP3115360A1

    公开(公告)日：2017-01-11

    申请号：EP15759282.5

    申请日：2015-03-04

    申请人： Zhejiang Hisun Pharmaceutical Co. Ltd.

    发明人： ZHANG, Liang ,  LIU, Chuan ,  XU, Jinyi ,  ZHANG, Zhaozhao ,  CHEN, Zhi ,  CHAI, Jian ,  YANG, Zhiqing ,  LUO, Hairong ,  ZHANG, Xiangyang

    IPC分类号： C07D401/12 ,  C07C303/44 ,  C07C309/04 ,  A61K31/4439 ,  A61P7/02

    CPC分类号： C07D401/12 ,  C07B2200/13 ,  C07C303/44 ,  C07C309/04 ,  C07D403/12

    摘要： The present invention relates to novel crystal forms M and N of dabigatran etexilate mesylate and preparation method and uses thereof, wherein the X-Ray powder diffractogram of the crystal form M has characteristic peaks at the following 2θ diffraction angles: 5.7±0.2°, 6.2±0.2°, 11.2±0.2°, 12.4±0.2°, 18.2±0.2°, 21.4±0.2°, 21.8±0.2° and 23.6±0.2°; and the X-Ray powder diffractogram of the crystal form N has characteristic peaks at the following 2θ diffraction angles: 6.0±0.2°, 11.8±0.2°, 18.2±0.2°, 21.6±0.2°, 24.4±0.2°, 27.7±0.2° and 29.7±0.2°. The crystal forms of the present invention have excellent properties in the aspects of leaching time, biological release, chemical stability and processing adaptability.

    摘要翻译： 本发明涉及甲磺酸达比加群酯的新型结晶形式M和N及其制备方法和用途，其中晶型M的X射线粉末衍射图在以下2θ衍射角为5.7±0.2°处具有特征峰， 6.2±0.2°，11.2±0.2°，12.4±0.2°，18.2±0.2°，21.4±0.2°，21.8±0.2°和23.6±0.2°; 晶体形式N的X射线粉末衍射图在以下2θ衍射角处具有特征峰：6.0±0.2°，11.8±0.2°，18.2±0.2°，21.6±0.2°，24.4±0.2°，27.7± 0.2°和29.7±0.2°。 本发明的结晶形式在浸出时间，生物释放，化学稳定性和加工适应性方面具有优异的性能。

    AZETIDINONE COMPOUNDS AND MEDICAL USE THEREOF
    6.
    发明公开
    AZETIDINONE COMPOUNDS AND MEDICAL USE THEREOF 有权
    AZETIDINONVERBINDUNGEN UND IHRE MEDISINISCHE VERWENDUNG

    公开(公告)号：EP2465847A1

    公开(公告)日：2012-06-20

    申请号：EP10807852.8

    申请日：2010-08-09

    申请人： Zhejiang Hisun Pharmaceutical Co. Ltd.

    发明人： BAI, Hua ,  ZHAO, Xuyang ,  XU, Xiaojie ,  LIU, Xiaoyu ,  ZHANG, Yuncai ,  CHEN, Ying ,  ZHENG, Xiaohe ,  GU, Maojian ,  ZHU, Qifeng ,  ZHANG, Yong ,  LUO, Hairong

    IPC分类号： C07D205/08 ,  C07D263/26 ,  A61K31/397 ,  A61P3/06 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10

    CPC分类号： A61K31/397 ,  C07D205/08 ,  C07D263/26

    摘要： Preparation of azetidinone compounds and medical use thereof are provided by the present invention. More particularly, azetidionne compounds, shown as formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are defined in description, and preparation methods thereof are provided by the present invention. The compounds of the present invention can reduce the levels of total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C) in plasma, and can be used as medicaments for reducing cholesterol in blood. Therefore the compounds of the present invention can be used to treat or prevent diseases of atherosclerosis, cacergasia of blood vessel, cardiac failure, coronary artery disease, angiocardiopathy, myocardial, angina, hyperlipoidemia and hypercholesteremia and the like. Preparation method of compounds of formula (I) and intermediate compounds are also provided by the present invention.

    摘要翻译： 氮杂环丁酮化合物的制备及其医疗用途由本发明提供。 更具体地说，式（I）所示的氮杂环丁烷化合物，其中R 1，R 2，R 3，R 4，R 5和R 6在说明书中定义，其制备方法由本发明提供。 本发明的化合物可以降低血浆中总胆固醇（TC）和低密度脂蛋白胆固醇（LDL-C）的水平，可用作降低血液中胆固醇的药物。 因此，本发明的化合物可用于治疗或预防动脉粥样硬化，血管紧张素，心力衰竭，冠状动脉疾病，心血管病，心肌，心绞痛，高脂血症和高胆固醇血症等疾病。 式（I）化合物和中间体化合物的制备方法也由本发明提供。