CRYSTAL FORM OF DABIGATRAN ETEXILATE MESYLATE AND PREPARATION METHOD AND USE THEREOF

Title:

CRYSTAL FORM OF DABIGATRAN ETEXILATE MESYLATE AND PREPARATION METHOD AND USE THEREOF

Document Type and Number:

WIPO Patent Application WO/2015/131829

Kind Code:

A1

Abstract:

The present invention relates to novel M and N crystal forms of dabigatran etexilate mesylate and preparation methods and uses thereof, wherein the X-Ray powder diffractogram of the M crystal form has a characteristic peak at the following 2 θ-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 N crystal form has a characteristic peak at the following 2 θ-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.

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Inventors:

ZHANG LIANG (CN)
LIU CHUAN (CN)
XU JINYI (CN)
ZHAGN ZHAOZHAO (CN)
CHEN ZHI (CN)
CHAI JIAN (CN)
YANG ZHIQING (CN)
LUO HAIRONG (CN)
ZHANG XIANGYANG (CN)

Application Number:

PCT/CN2015/073650

Publication Date:

September 11, 2015

Filing Date:

March 04, 2015

Export Citation:

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Assignee:

ZHEJIANG HISUN PHARM CO LTD (CN)

International Classes:

C07D401/12; A61K31/4439; A61P7/02; C07C303/44; C07C309/04

Domestic Patent References:

WO2006114415A2	2006-11-02
WO2008043759A1	2008-04-17

Foreign References:

CN102167695A	2011-08-31
EP2631234A1	2013-08-28
CN101189224A	2008-05-28
CN102391250A	2012-03-28
CN102858762A	2013-01-02
CN102050815A	2011-05-11
CN103288800A	2013-09-11

Other References: