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Novel crystal form of lenvatinib mesylate

A mesylate salt and crystal form technology, applied in the preparation of organic compounds, organic chemistry, organic chemistry methods, etc., can solve problems affecting the bioavailability of drugs, affecting the dissolution and release of pharmaceutical compositions, etc.

Pending Publication Date: 2019-12-13
北京赛思源生物医药技术有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Different crystal forms of 4-[3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxy-6-quinolinecarboxamide methanesulfonate, possible in terms of solubility and stability There are differences, which affect the dissolution and release of its pharmaceutical composition in vitro, and then affect the bioavailability of the drug in vivo

Method used

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  • Novel crystal form of lenvatinib mesylate
  • Novel crystal form of lenvatinib mesylate
  • Novel crystal form of lenvatinib mesylate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Get 10g of 4-[3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxyl-6-quinoline carboxamide methanesulfonate and add it to a mixture with a volume ratio of 2:1 Organic solvent (N,N-dimethylformamide and dioxane) and aqueous solution, stirred and dissolved at room temperature, then lowered to 0-5 ° C, added 5 times the volume of water, stirred until crystals slowly precipitated; centrifuged Gained solid is collected, and the X-ray diffraction pattern of gained product is as follows figure 1 shown.

Embodiment 2

[0052] Get 30g of 4-[3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxyl-6-quinoline carboxamide methanesulfonate and join in the mixing mixture whose volume ratio is 4:1 Organic solvent (N,N-dimethylformamide and dioxane) and aqueous solution, stirred and dissolved at room temperature, then lowered to 0-5°C, added 10 times the volume of water, stirred until crystals slowly precipitated; centrifuged The obtained solid was collected, and the X-ray diffraction spectrum of the product obtained was basically consistent with that of Example 1.

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Abstract

The invention discloses a novel crystal form of lenvatinib mesylate. In an X-ray powder diffraction pattern, obtained through determination using Cu-Ka ray, of the new crystal form, at least followingcharacteristic peaks are contained: diffraction angles 2 theta are at 4.19 + / -0.2 DEG, 10.15 + / -0.2 DEG, 12.40 + / -0.2 DEG, 18.93 + / -0.2 DEG, 22.05 + / -0.2 DEG and 29.26 + / -0.2 DEG. The obtained new crystal form has good solubility and stability, and is suitable for industrial production. In addition, the invention also provides a preparation method and a medicinal composition of the new crystal form.

Description

technical field [0001] The present invention relates to the crystal form of pharmaceutical compound, particularly relates to the new Crystal form, its preparation method and pharmaceutical composition. Background technique [0002] Lenvatinib (trade name: LENVIMA), developed by Japan's Eisai (Eisai), is a multi-target receptor tyrosine kinase (RTK) inhibitor, the drug's chemical name is: 4- [3-Chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxy-6-quinolinecarboxamide methanesulfonate. In 2015, the US FDA and the European Medicines Agency EMA approved lenvatinib for the treatment of aggressive, locally advanced or metastatic differentiated thyroid cancer. In 2016, the US FDA and the European EMA successively approved lenvatinib combined with everolimus for the treatment of advanced renal cell carcinoma. In March 2018, lenvatinib was approved in Japan for the first-line treatment of patients with unresectable hepatocellular carcinoma (HCC). [0003] Japan's Eisai Co...

Claims

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Application Information

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IPC IPC(8): C07D215/48C07C303/44C07C309/04A61K31/47
CPCC07D215/48C07C303/44C07C309/04C07B2200/13
Inventor 赵紫岭王守亮
Owner 北京赛思源生物医药技术有限公司
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