Crystalline form I of tyrosine kinase inhibitor dimaleate and preparation methods thereof
AssigneeJiangsu Hengrui Medicine Co., Ltd.
InventorsPiaoyang Sun, Guaili Wu, Bo Yuan, Yongjiang Chen
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Abstract
Provided are crystalline Form I of (R,E)-N-(4-(3-chloro-4-(pyridin-2-yl-methoxy)-phenylamino)-3-cyano-7-ethoxy-quinolin-6-yl)-3-(1-methylpyrrolidin-2-yl) propenamide dimaleate (called SHR1258 dimaleate for short), preparation methods thereof, and pharmaceutical compositions containing the same. The crystalline Form I of SHR1258 dimaleate has good crystal stability and chemical stability, and can be used in the preparation of medicaments for treating diseases related to EGFR receptor tyrosine kinase or HER-2 receptor tyrosine kinase.
Claims14
A form I crystal of (R,E)-N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)-phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl) acrylamide dimaleate, wherein using Cu—Kα radiation to obtain an X-ray diffraction pattern represented by 2θ angle (interplanar crystal spacing), the form I crystal has the X-ray diffraction pattern comprising characteristic peaks at 6.28 (14.06), 6.74 (13.10), 10.60 (8.34), 11.58 (7.64), 13.50 (6.55), 14.90 (5.94), 15.80 (5.60), 18.26 (4.85), 20.66 (4.30), 21.14 (4.20), 22.96 (3.87), 24.34 (3.65), 25.54 (3.49), and 26.12 (3.41).
Dependencies are inferred from the claim text.