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Crystal form of brutinib and preparation method of crystal form

A Ni crystal form and crystal form technology, applied in the field of medicine and its preparation, can solve the problems of no novelty, no characterization data and beneficial effects, etc., to facilitate storage and transportation, avoid the risk of crystal transformation, and avoid biological The effects of changes in availability and potency

Pending Publication Date: 2022-01-18
LUOXIN PHARM SHANGHAI CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The Indian patent IN201741016390 applied by Dr Reddy’s discloses the crystalline form SP5 of brigatinib, which only has an XRPD pattern, which is completely consistent with the crystalline form N6, without novelty, and does not give any other characterization data and beneficial effects

Method used

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  • Crystal form of brutinib and preparation method of crystal form
  • Crystal form of brutinib and preparation method of crystal form
  • Crystal form of brutinib and preparation method of crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0101] Preparation of brigatinib crystal form LX-1

[0102] Dissolve brigatinib 50mg in 250μl methanol at 70°C. Add 250 μl n-butyl acetate and 750 μl n-heptane at room temperature. Place it in a freezer at -20°C to volatilize to obtain a solid powder. It was detected as the crystal form LX-1. Its XRPD spectrum is attached figure 1 , DSC spectrum see attached figure 2 , TGA spectrum see attached image 3 .

[0103] From figure 1 It can be seen that the X-ray powder diffraction pattern of brigatinib crystal form LX-1 represented by 2θ angle is at 5.4±0.2°, 10.4±0.2°, 10.8±0.2°, 11.1±0.2°, 12.9±0.2°, 14.9 Available at ±0.2°, 15.9±0.2°, 17.2±0.2°, 17.8±0.2°, 19.2±0.2°, 20.2±0.2°, 20.6±0.2°, 22.0±0.2°, 24.0±0.2° and 25.6±0.2° Diffraction peaks. The specific X-ray powder diffraction data are shown in the table below.

[0104] Numbering 2θ angle (°) Relative Strength(%) Numbering 2θ angle (°) Relative Strength(%) 1 5.4 63.3 17 21.7 18.3 2 ...

Embodiment 2

[0107] Preparation of brigatinib crystal form LX-1

[0108] Dissolve brigatinib 200mg in 1ml methanol at 70°C. Add 1ml of n-butyl acetate at room temperature, and add 3ml of n-heptane. Place it in a freezer at -20°C to volatilize to obtain a solid powder. It was detected as the crystal form LX-1. The solid-state characterization data are the same as in Example 1.

Embodiment 3

[0110] Preparation of brigatinib crystal form LX-1

[0111] Dissolve brigatinib 200mg in 2ml methanol at 70°C. 2 ml of ethyl acetate was added at room temperature, and 5 ml of cyclohexane was added. Place it in a freezer at -25°C to volatilize to obtain a solid powder. It was detected as the crystal form LX-1. The solid-state characterization data are the same as in Example 1.

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Abstract

The invention discloses a crystal form of brutinib and a preparation method of the crystal form. The crystal form LX-3 of brutinib is an anhydrous substance, and an X-ray powder diffraction pattern expressed by a 2 theta angle has diffraction peaks at 5.7 + / -0.2 degrees, 8.5 + / -0.2 degrees, 11.4 + / -0.2 degrees, 16.0 + / -0.2 degrees, 17.1 + / -0.2 degrees, 21.4 + / -0.2 degrees, 27.3 + / -0.2 degrees and 28.7 + / -0.2 degrees. Compared with the prior art, the novel crystal form of the brutinib has obvious advantages in the aspects of solubility, flowability and the like, and meanwhile, the crystal form is good in stability, simple in preparation process and suitable for industrial production and preparation production, and has a good patent medicine prospect.

Description

technical field [0001] The invention relates to a medicine and a preparation method thereof, in particular to a crystal form of brigatinib and a preparation method thereof. Background technique [0002] Brigatinib, English name: Brigatinib, chemical formula is [0003] [0004] The drug is a multi-targeted tyrosine kinase inhibitor used to treat non-small cell lung cancer (NSCLC) and other diseases. It is a potent inhibitor of ALK (anaplastic lymphoma kinase) and is in clinical development for the treatment of adult patients with ALK-driven NSCLC and can be used in patients who are intolerant after treatment with crizotinib In patients, resistance to crizotinib can be reversed. [0005] The CN107108559B crystal form patent applied by the original research company discloses various crystal forms of brigatinib, including crystal form A, crystal form B, crystal form C, crystal form D, crystal form E, crystal form F, crystal form G, Crystal form H, crystal form J, crystal ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6558
CPCC07F9/65583C07B2200/13
Inventor 许炜黄继霆唐伟
Owner LUOXIN PHARM SHANGHAI CO LTD
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