公开(公告)号：US09718802B2

公开(公告)日：2017-08-01

申请号：US15123378

申请日：2015-03-04

申请人： Zhejiang Hisun Pharmaceutical Co., Ltd.

发明人： Liang Zhang ,  Chuan Liu ,  Jinyi Xu ,  Zhaozhao Zhang ,  Zhi Chen ,  Jian Chai ,  Zhiqing Yang ,  Hairong Luo ,  Xiangyang Zhang

IPC分类号： C07D401/12 ,  C07C309/04 ,  C07C303/44 ,  C07D403/12

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.

公开(公告)号：US20170073327A1

公开(公告)日：2017-03-16

申请号：US15123378

申请日：2015-03-04

申请人： Zhejiang Hisun Pharmaceutical Co., Ltd.

发明人： Liang Zhang ,  Chuan Liu ,  Jinyi Xu ,  Zhaozhao Zhang ,  Zhi Chen ,  Jian Chai ,  Zhiqing Yang ,  Hairong Luo ,  Xiangyang Zhang

IPC分类号： C07D401/12 ,  C07C309/04

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 20 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射线粉末衍射图具有以下2θ衍射角的特征峰：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°和23.6±0.2°; 并且晶体形式N的X射线粉末衍射图在随后的20个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。