Title:
NOVEL CRYSTAL FORM OF DABIGATRAN ETEXILATE ETHYL ESTER HYDROCHLORIDE, PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/198361
Kind Code:
A1
Abstract:
Disclosed is a novel crystal form of dabigatran etexilate ethyl ester hydrochloride, the X-ray powder diffraction pattern thereof having diffraction peaks at 2θ ± 0.2°, and 2θ is at least selected from any one of 5.42 ± 0.2°, 9.08 ± 0.2°, 11.88 ± 0.2° and 14.14 ± 0.2°. The disclosed novel crystal form of dabigatran etexilate ethyl ester hydrochloride can be used as a pharmaceutically active ingredient, and has the following advantages: (1) a good physical stability and chemical stability; (2) a controllable production cost; (3) in the production process, being excellent in purification and impurity removal effects, simple and convenient in operation and high in yield, which are beneficial to industrial production; (4) having good water solubility, and being used as a raw drug in the subsequent process without adopting a special solubilization technology; and (5) the solubility thereof not being pH-dependent within a physiological pH range.
Inventors:
JIA HUIJUAN (CN)
HOU WEI (CN)
WANG YANXIN (CN)
JIA TIANGE (CN)
REN XIAOHUI (CN)
HOU WEI (CN)
WANG YANXIN (CN)
JIA TIANGE (CN)
REN XIAOHUI (CN)
Application Number:
PCT/CN2021/082000
Publication Date:
September 29, 2022
Filing Date:
March 22, 2021
Export Citation:
Assignee:
TIANJIN CREATRON BIOTECHNOLOGY CO LTD (CN)
BEIJING CREATRON INSTITUTE OF PHARMACEUTICAL RES CO LTD (CN)
BEIJING CREATRON INSTITUTE OF PHARMACEUTICAL RES CO LTD (CN)
International Classes:
C07D401/12; A61K31/4439; A61P7/02; C07D401/04
Domestic Patent References:
| WO2010045900A1 | 2010-04-29 | |||
| WO2012077136A2 | 2012-06-14 | |||
| WO2013111163A2 | 2013-08-01 | |||
| WO2014020555A2 | 2014-02-06 | |||
| WO2014041559A2 | 2014-03-20 | |||
| WO2014192030A2 | 2014-12-04 | |||
| WO2016132296A1 | 2016-08-25 |
Foreign References:
| CN105294651A | 2016-02-03 | |||
| CN105153118A | 2015-12-16 | |||
| CN105566297A | 2016-05-11 | |||
| CN106543144A | 2017-03-29 | |||
| CN109125274A | 2019-01-04 |
Attorney, Agent or Firm:
FAIRSKY LAW OFFICE (CN)
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