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A kind of crystal form B of triazolopyrazine derivative and its preparation method

A technology of azolopyrazine and derivatives, applied in the field of triazolopyrazine derivative B crystal form and preparation thereof, can solve the problem that triazolopyrazine derivatives are unstable, easily converted to other crystal forms, disadvantageous Drug processing and other issues, to achieve the effect of excellent high humidity stability, good bioavailability, and stable solubility

Active Publication Date: 2018-09-11
SHANGHAI SUNTRONG BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The problem to be solved by the present invention is that the existing triazolopyrazine derivatives have instability, low solubility and easy conversion to other crystal forms, which are unfavorable for pharmaceutical processing and use in pharmaceutical compositions. The triazolopyrazine derivatives of the present invention The new crystal form of pyrazine derivatives provides more qualitative and quantitative information for the curative effect research of solid drugs

Method used

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  • A kind of crystal form B of triazolopyrazine derivative and its preparation method
  • A kind of crystal form B of triazolopyrazine derivative and its preparation method
  • A kind of crystal form B of triazolopyrazine derivative and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 to 2 3

[0034] Embodiment 1 to 2 Preparation of triazolopyrazine derivative B crystal form

[0035] Weigh 500 mg of the triazolopyrazine derivative raw material into a container, add 100 mL of the mixed solvent (analytical grade) in Table 1, suspend at 35° C. for 24 hours, evaporate the solvent to obtain a solid, and obtain an off-white powder after vacuum drying. Weigh to calculate its yield.

[0036] Table 1 Preparation of triazolopyrazine derivative B crystal form

[0037] Example

Embodiment 3

[0038] Example 3. Characterization of triazolopyrazine derivative B crystal form by XRPD pattern

[0039] The measurement of the X-ray powder diffraction (XRPD) pattern is carried out using the Rigaku UltimaIV model combined multifunctional X-ray diffractometer, and the specific collection information is as follows: Cu anode (40kV, 40mA), scanning speed 20° / min, scanning range (2θ range )5~45°, scan step size 0.02, slit width 0.01. Samples were processed using glass slides pressed directly onto the test plate. Subsequent XRPD patterns all adopt similar measurement methods.

[0040] Determination of the XRPD spectrum of the triazolopyrazine derivative B crystal form prepared according to the method described in Example 1, at 2θ=5.52, 7.954, 9.42, 10.821, 14.3, 16.18, 18.661, 19.459, 21.56, 23.461, 24.46, 26.238 , 30.12, 32.521, and 32.96 have diffraction peaks, such as figure 1 shown. The error range of 2θ value is ±0.2. After testing, the error range of 2θ value can also ...

Embodiment 4

[0042] Example 4. Investigation of the High Temperature Stability of Form B of Triazolopyrazine Derivatives

[0043] The triazolopyrazine derivative B crystal sample was placed in a 60°C oven, and after 5 days and 10 days, the samples were taken out for XRPD testing (such as figure 2 and Figure 5 Shown), in order to investigate the stability of the crystal form of the sample to temperature. The results show that the crystal form B samples have average stability under high temperature conditions.

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Abstract

The invention provides a triazolo pyrazine derivative B crystal form as shown in formula (I), and the formula (I) is described in the specification. The x-ray powder diffraction (XRPD) spectrum has diffraction peaks when 2 theta is equal to 5.52, 7.954, 9.42, 10.821, 14.3, 16.18, 18.661, 19.459, 21.56, 23.461, 24.46, 26.238, 30.12, 32.521 and 32.96, wherein the error range of the 2 theta value is + / -0.2. The triazolo pyrazine derivative B crystal form has good high-humidity stability and stable solubility, can be applied to the medicines used for inhibiting c-Met activity and the medicines for treating or preventing cancers inhibiting c-Met sensitivity, and has better bioavailability; furthermore, the qualitative and quantitative information provided by the triazolo pyrazine derivative B crystal form has important significance in further studying the treatment effect of the solid medicines.

Description

technical field [0001] The present invention relates to a polymorphic form of a triazolopyrazine derivative as a c-Met inhibitor, in particular to a crystal form B of a triazolopyrazine derivative and a preparation method thereof. Background technique [0002] The c-Met protein, also known as the hepatocyte growth factor (HGF) receptor, is a transmembrane 190 kDa heterodimer with tyrosine kinase activity, which is encoded by the c-Met oncogene. Studies have shown that the HGF / c-Met signaling pathway has a variety of cell response activities, including promoting cell mitosis, proliferation, shaping, angiogenesis and so on. Therefore, inhibition of the HGF / c-Met signaling pathway has significant potential for the treatment of cancer. [0003] The present invention provides a kind of triazolopyrazine derivative, the chemical name is (S)-1-(1-(imidazo[1,2-a]pyrazin-6-yl)ethyl)-6-( 1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazol[4,5-b]pyrazine, as shown in formula (I), [0004] ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D519/00A61P35/00
CPCC07B2200/13C07D519/00
Inventor 任国宾弋东旭陈金瑶
Owner SHANGHAI SUNTRONG BIOTECH
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