Fasotinib crystal form and preparation method thereof

A crystal form and crystallization technology, which is applied in organic chemical methods, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems affecting drug safety and effectiveness, drug solubility, stability and fluidity differences, clinical different effects

Pending Publication Date: 2021-06-29
SHANGHAI ACEBRIGHT PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Different crystal forms can cause differences in the solubility, stability, and fluidity of the drug,

Method used

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  • Fasotinib crystal form and preparation method thereof
  • Fasotinib crystal form and preparation method thereof
  • Fasotinib crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0105] Example 1: Preparation of crystal form XM-I

[0106] The 50 mg of formula (I) compound was sunedressed in 1 ml of 2-butanone, filtered, and 3 ml of petroleum ether was slowly added to the filtrate, stirred at 25 ° C for 16 h, and there was solid precipitation, the resulting solid was formula (I) Compound type XM -I. The obtained solid was performed, and the X-ray powder diffraction data was shown in Table 1, and its XRPD is shown in Table 1. figure 1 Down; TGA testing of the resulting solid, whose spectrum is figure 2 Down; DSC testing of the resulting solid, whose spectrum is image 3 Disted; for the resulting solid 1 H NMR test, whose spectrum is Figure 4 As shown, nuclear magnetic data: 1 H NMR (400MHz, DMSO-D 6 Δ9.18 (S, 1H), 8.01 (D, J = 7.1 Hz, 1H), 7.69 (S, 1H), 7.55-7.47 (M, 2H), 7.01 (S, 2H), 6.25 (DD, J = 17.1, 10.2 Hz, 1H), 6.06 (DD, J = 17.1, 2.1 Hz, 1H), 5.55 (DD, J = 10.2, 2.1 Hz, 1H), 4.34 (S, 2H), 3.97 (s, 6h) 3.85 (D, J = 11.6Hz, 2H), 3.65 (D, J = 10.4 Hz, 1...

Embodiment 2

[0110] Example 2: Preparation of crystalline XM-I

[0111] It is weighed with 50 mg of the compound of formula (I) to dissolve in 1 ml of acetonitrile, filtered, and 15 ml of diethyl ether was slowly added to the filtrate, stirred at 25 ° C for 16 h, there was solid precipitation, the resulting solid was formula (I) Compound crystal type XM-I, obtained The solid is the formula (I) Compound crystal type XM-I. The obtained solid was performed, and the X-ray powder diffraction data was shown in Table 2.

[0112] Table 2

[0113]

[0114]

Embodiment 3

[0115] Example 3: Preparation of crystalline XM-I

[0116] It is weighted 15 mg of the compound of formula (I) in 0.2 ml of ethanol / n-heptane (1: 4, v / v) at 40 ° C, filtered, stirred at 5 ° C for 16 h, there is solid precipitation, resulting solid For the formula (I) compound crystal type XM-I. The obtained solid is performed, and the X-ray powder diffraction data is shown in Table 3.

[0117] table 3

[0118]

[0119]

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PUM

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Abstract

The invention provides a novel crystal form of N-((3S,4S)-3-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)tetrahydro-2H-pyran-4-yl)acrylamide and a preparation method of the novel crystal form.

Description

Technical field [0001] The present invention relates to the field of pharmaceutical chemistry, and more particularly to N - ((3S, 4S) -3 - ((6- (2,6-dichloro-3,5-dimethoxyphenyl) quinazoline-2-ylide Netcard form and preparation method thereof of amino) tetrahydro-2H-pyran-4-yl) acrylamide. Background technique [0002] FGFR4 is a carcinogenic drive factor of local late or metastatic hepatocellular carcinoma (HCC) patients. The FGF19 is an FGFR4 ligand, which activates FGFR4 to promote hepatocyte proliferation and regulate the balance of liver. About 30% of HCC patients have an abnormal activation of the FGF19 / FGFR4 signaling pathway. Non-Swarda (BLU-554) is a strong, high selective fibroblast growth factor receptor-4 (FGFR4) inhibitor developed by Blueprint Medicines, is used to treat FGFR4 driven advanced HCC. The drug has not yet been launched, and its clinical I-phase test data showed clinical efficacy and good tolerance in patients with local advanced or metastatic hepatocy...

Claims

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Application Information

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IPC IPC(8): C07D405/12A61K31/517A61P35/00A61P1/16
CPCA61P1/16A61P35/00C07B2200/13C07D405/12
Inventor 彭欢钟仁欢张良
Owner SHANGHAI ACEBRIGHT PHARMA CO LTD
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