New crystal form of axitinib fumarate and preparation method thereof

A technology of nifumarate and axitinib, applied in the field of medicinal chemistry, can solve the problems of limited oral bioavailability, poor photostability of axitinib, clinical application limitations, etc., and achieves easy control and good crystallization process. Effects of photostability, large apparent solubility
CN112174933AInactive Publication Date: 2021-01-05TIANJIN UNIVERSITY OF TECHNOLOGY
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
TIANJIN UNIVERSITY OF TECHNOLOGY
Publication Date
2021-01-05
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a new crystal form of axitinib fumarate and a preparation method thereof. In the new crystal form, the molar ratio of axitinib to fumaric acid is 1: 1.5, and the X-ray powder diffraction pattern of the crystal form has characteristic peaks when the 2 theta value is 7.1 + / -0.2 degrees, 12.5 + / -0.2 degrees, 15.1 + / -0.2 degrees, 17.4 + / -0.2 degrees and 23.4 + / -0.2 degrees. Thecrystal form preparation method provided by the invention is simple in process, easy in crystallization process control, good in reproducibility and suitable for industrial production. The new crystal form of the axitinib fumarate is remarkably improved in the aspects of light stability and dissolution property, and is beneficial to improving the safety and oral bioavailability of axitinib.
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Description

technical field

[0001] The invention relates to the technical field of medicinal chemistry, in particular to a new crystal form of axitinib fumarate and a preparation method thereof. Background technique

[0002] The chemical name of Axitinib is N-methyl-2-[[3-[(1E)-2-(2-pyridyl)vinyl]-1H-indazol-6-yl]thio ] benzamide, its chemical structural formula is:

[0003] Axitinib is a second-generation VEGFR inhibitor that can selectively inhibit the activity of vascular endothelial growth factor VEGF-1, VEGF-2, and VEGF-3 receptors to exert anti-cancer effects. The drug was developed by Pfizer under the trade name On January 27, 2012, it was approved by the FDA for the treatment of early to advanced kidney cancer, and in September of the same year, it was approved by the EMA for marketing in Europe. Currently, the drug is used in several countries for the treatment of advanced renal cell carcinoma. Patent US20060094763 discloses crystal forms I, II, III, IV, VI, VII, VIII an...

Claims

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