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Ceritinib compound and pharmaceutical composition thereof

A compound and composition technology, applied in the field of medicinal chemistry, can solve the problems of not providing Ceritinib crystal information, not obtaining the free base solid form, and not seeing Ceritinib public reports, etc., and achieve the effect of simple preparation process and good reproducibility

Inactive Publication Date: 2016-02-03
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Example 7 of Chinese patent application CN200780051064.2 discloses a preparation method of Ceritinib hydrochloride, the preparation process does not obtain the solid form of free base, and does not provide any crystal information of Ceritinib
In addition, there are no other new crystalline forms of Ceritinib publicly reported

Method used

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  • Ceritinib compound and pharmaceutical composition thereof
  • Ceritinib compound and pharmaceutical composition thereof
  • Ceritinib compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Preparation of Embodiment 1 Ceritinib Compound Amorphous Crystalline Form

[0046] At room temperature, dissolve Ceritinib dihydrochloride (5g) in 25g of purified water, add dichloromethane (75ml), slowly add 50% sodium hydroxide solution dropwise under stirring, adjust the pH of the aqueous solution to 7-10, and after standing The organic layer was separated, and the organic layer was concentrated to dryness under reduced pressure at 45°C to obtain a foamy solid. X-ray powder diffraction pattern shows an amorphous crystalline form.

Embodiment 2

[0047] Preparation of Embodiment 2 Ceritinib Formula I Compound Crystal Form

[0048] The Ceritinib amorphous crystalline form (3g) obtained in Example 1 was added to purified water (15g), stirred and heated to 60°C for beating for 2-5h, filtered, and dried under reduced pressure at 40°C for 3h to obtain 2.5g of solid. X-ray powder diffraction diagram, DSC diagram, TGA diagram are respectively attached figure 1 , figure 2 , image 3 shown.

Embodiment 3

[0049] Preparation of Embodiment 3 Ceritinib Formula I Compound Crystal Form

[0050] Take the Ceritinib amorphous crystal form (3g) obtained in Example 1, add it to purified water (30g), stir and heat to 80°C for beating for 2-5h, filter, and dry under reduced pressure at 40°C for 3h to obtain a solid, X-ray powder diffraction pattern same figure 1 Basically the same.

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Abstract

The invention belongs to the field of medical chemistry, and discloses a crystal form of a ceritinib compound and a pharmaceutical composition of the ceritinib compound. The compound has the characteristic of being high in stability, and conforms to the medicinal requirements. According to the invention, the preparation technology is stable, the reproducibility is good, and the requirements of industrial mass production are met.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to the crystal form and preparation method of Ceritinib compound, including the pharmaceutical composition containing the compound and the treatment method using it. Background technique [0002] Ceritinib (LDK378, also known as: Ceritinib) is an ALK inhibitor for the treatment of various types of advanced metastatic non-small cell lung cancer (NSCLC). Ceritinib is an anaplastic lymphoma enzyme (ALK) tyrosine kinase inhibitor developed for ALK+ patients who have previously received Crizotinib (crizotinib), the only approved drug prior to Ceritinib ALK kinase inhibitors. Structural formula is as shown in formula I: [0003] [0004] Ceritinib was developed by Novartis and was approved by the FDA on April 29, 2014. It is the second ALK inhibitor approved by the FDA. It is used as a specific drug for ALK-positive non-small cell lung cancer for crizotinib resistance o...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61K31/506A61P35/00A61P35/02
Inventor 赵俊张建义宗在伟
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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