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Hydrochloride crystal form B of Lu AE58054 and preparation method for hydrochloride crystal form B

A hydrochloride and crystal form technology, which is applied in the crystal form B of LuAE58054 hydrochloride and its preparation field, can solve the problems of reporting the crystal form of LuAE58054 hydrochloride, etc., and achieve convenient long-term storage and placement, simple operation, and hygroscopicity low effect

Inactive Publication Date: 2017-01-11
CRYSTAL PHARMATECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the patent CN1610547A discloses the structure of Lu AE58054 hydrochloride and its preparation method, but there is no patent or other literature reporting the relevant crystal form of Lu AE58054 hydrochloride

Method used

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  • Hydrochloride crystal form B of Lu AE58054 and preparation method for hydrochloride crystal form B
  • Hydrochloride crystal form B of Lu AE58054 and preparation method for hydrochloride crystal form B
  • Hydrochloride crystal form B of Lu AE58054 and preparation method for hydrochloride crystal form B

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Preparation method of Lu AE58054 hydrochloride crystal form B:

[0051] Dissolve 10.3 mg of Lu AE58054 hydrochloride in 25 μL of methanol and slowly add dropwise to 1.5 mL of methyl tert-butyl ether. A solid precipitates out. Stir at room temperature for 24 hours, filter and dry, and collect the solid. It is the crystalline form B of Lu AE58054 hydrochloride.

[0052] The X-ray powder diffraction data of the crystal form obtained in this example is shown in Table 1. Its XRPD diagram is like figure 1 , Its DSC graph is like figure 2 .

[0053] Table 1

[0054] 2theta d interval strength% 4.5919.2660.15 6.8912.8430.23 9.199.622.19 13.866.39100.00 16.185.488.15 17.345.1114.27 17.705.014.57 19.274.6118.14 20.874.2686.14 21.414.159.34 22.843.8913.29 25.203.5313.87 26.573.355.83 27.843.201.45 28.853.102.88 30.342.956.68 32.362.772.10 32.892.723.47 35.182.554.69 36.482.464.38 38.672.332.28

Embodiment 2

[0056] Preparation method of Lu AE58054 hydrochloride crystal form B:

[0057] 2.0 mg of Lu AE58054 hydrochloride was dissolved in 50 μL of methanol, and it was volatilized at room temperature until a solid precipitated. The solid was collected, and it was detected as Lu AE58054 hydrochloride crystal form B.

[0058] The X-ray powder diffraction data of the crystal form obtained in this example is shown in Table 2.

[0059] Table 2

[0060] 2theta d interval strength% 4.5819.2858.03 6.8912.8425.48 11.517.692.82 13.856.39100.00 16.185.487.79 17.345.127.05 17.675.022.76 18.394.821.49 19.284.6013.00 20.134.412.24 20.864.2672.46 21.374.167.20 22.853.8910.56 23.213.832.66 24.943.575.93 25.203.535.14 25.593.481.97 26.153.411.87 26.593.355.03 27.973.191.51 30.352.955.97 32.342.771.83 35.182.553.92 36.502.463.83 38.662.332.24

Embodiment 3

[0062] Preparation method of Lu AE58054 hydrochloride crystal form B:

[0063] 2.0 mg of Lu AE58054 hydrochloride was dissolved in 20 μL of acetone, and it was volatilized at room temperature until a solid precipitated. The solid was collected, and it was detected as the crystalline form B of Lu AE58054 hydrochloride.

[0064] Table 3 shows the X-ray powder diffraction data of the crystal form obtained in this example.

[0065] table 3

[0066] 2theta d interval strength% 4.5819.3045.51 6.8912.8328.26 11.517.694.20 13.856.40100.00 16.165.497.61 17.355.113.62 19.294.605.94 20.854.2677.27 21.374.163.59 22.833.904.06 23.213.832.72 24.923.577.04 26.573.355.72 27.583.231.87 27.963.192.11 30.332.958.15 32.352.771.25 35.162.553.62 36.472.462.66 38.662.331.41

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Abstract

The invention provides a hydrochloride crystal form B of Lu AE58054 and a preparation method for the hydrochloride crystal form B. The crystal form B is characterized in that an X-ray powder diffractogram of the crystal form B has characteristic peaks when a 2theta value is 13.9+ / -0.2 degrees, 19.3+ / -0.2 degrees and 20.9+ / -0.2 degrees. The crystal form B is good in stability and low in hygroscopicity and is not prone to deliquescence caused by high-humidity effect, so that the long-term storage and placement of drugs are facilitated. Furthermore, a preparation process for the crystal form B is simple in operation and low in cost, thereby having an important value in the optimization and development of the drugs in the future.

Description

Technical field [0001] The present invention relates to the field of chemical medicine, in particular to the crystal form B of Lu AE58054 hydrochloride and a preparation method thereof. Background technique [0002] Lu AE58054 (the compound represented by formula I), also known as Idalopirdine, was first developed by Lilly Pharmaceuticals of the United States, and then jointly developed by Lundbeck Pharmaceuticals of Denmark and Otsuka Pharmaceuticals of Japan. Drugs for Zheimer's disease. Lu AE58054 is a selective 5-HT6 receptor antagonist for the treatment of cognitive disorders. 5-HT6 receptors are mainly expressed in the human brain, especially in areas related to cognition, such as the hippocampus and frontal cortex. In animal models, 5-HT6 receptor antagonists can improve cognitive function. The clinical Phase II results of the drug showed that Lu AE58054 helps to improve the cognitive function of patients with moderate Alzheimer's disease treated with donepezil. Curren...

Claims

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Application Information

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IPC IPC(8): C07D209/14A61K31/4045A61P25/28
CPCC07D209/14
Inventor 陈敏华张炎锋刘凯张晓宇
Owner CRYSTAL PHARMATECH CO LTD
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