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Lu AE58054 hydrochloride crystal form A, preparation method and uses thereof

A hydrochloride and crystal form technology, applied in the hydrochloride crystal form A of Lu AE58054 and its preparation and use fields, can solve problems such as unsatisfactory solubility, and avoid changes in bioavailability and efficacy, solubility High and simple preparation process

Inactive Publication Date: 2015-12-23
CRYSTAL PHARMATECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far, there has not been any relevant report about the crystal form of LuAE58054 hydrochloride, and according to the preparation method of LuAE58054 hydrochloride reported in CN1610547A, the properties of the prepared LuAE58054 hydrochloride solid, especially the stability, poor solubility

Method used

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  • Lu AE58054 hydrochloride crystal form A, preparation method and uses thereof
  • Lu AE58054 hydrochloride crystal form A, preparation method and uses thereof
  • Lu AE58054 hydrochloride crystal form A, preparation method and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] The preparation method of LuAE58054 hydrochloride crystal form A:

[0072] 10.1 mg of solid LUAE58054 hydrochloride was dissolved in 0.05 mL of ethanol to give a clear solution. With stirring, 0.4 mL of pure water was added dropwise until turbidity appeared, and stirring was continued for 48 hours at room temperature. The solid was collected to obtain Form A of LUAE58054 hydrochloride.

[0073] The X-ray powder diffraction data of the obtained hydrochloride crystal form A are shown in Table 1, and the XRPD figure is as follows figure 1 shown. Considering many factors such as d value, low angle, intensity, characteristic line and peak shape integrity, the diffraction peaks at 2theta values ​​of 17.05°, 17.85°, and 21.37° are characteristic peaks. The diffraction peaks at 2theta values ​​of 15.26°, 19.22°, and 20.73° are important peaks. The diffraction peaks at 2theta values ​​of 12.76°, 27.2, and 25.38° are the next most important peaks.

[0074] Table 1 X-ray powd...

Embodiment 2

[0081] The preparation method of LuAE58054 hydrochloride crystal form A:

[0082] 9.5 mg of solid LuAE58054 hydrochloride was dissolved in 0.025 mL of tetrahydrofuran to give a clear solution. With stirring, 0.3 mL of n-heptane was added dropwise until cloudiness appeared, and stirring was continued for 48 hours at room temperature. The solid was collected to obtain Form A of LuAE58054 hydrochloride.

[0083] Table 2 shows the X-ray powder diffraction data of the hydrochloride crystal form A obtained in this example. Considering many factors such as d value, low angle, intensity, characteristic line and peak shape integrity, the diffraction peaks at 2theta values ​​of 17.03°, 17.87°, and 21.35° are characteristic peaks. The diffraction peaks at 2theta values ​​of 15.27°, 19.24°, and 20.77° are important peaks. The diffraction peaks at 2theta values ​​of 12.72°, 27.30°, and 25.41° are the next most important peaks.

[0084] Table 2 X-ray powder diffraction data of crystal f...

Embodiment 3

[0088] The preparation method of LuAE58054 hydrochloride crystal form A:

[0089] 10.0 mg of LuAE58054 hydrochloride solid was dissolved in 0.6 mL of tetrahydrofuran: water = 2:25 (v:v, volume ratio) mixed solvent, and placed at 50° C. for 30 minutes. The above solution was filtered, and the resulting filtrate was immediately placed in a thermostat at 5° C. and stirred for 48 hours. The solid was collected to obtain Form A of LuAE58054 hydrochloride.

[0090] Table 3 shows the X-ray powder diffraction data of the hydrochloride crystal form A obtained in this example. Considering many factors such as d value, low angle, intensity, characteristic line and peak shape integrity, the diffraction peaks at 2theta values ​​of 17.11°, 17.91°, and 21.43° are characteristic peaks. The diffraction peaks at 2theta values ​​of 15.33°, 19.29° and 20.81° are important peaks. The diffraction peaks at 2theta values ​​of 12.82°, 27.27° and 25.47° are the next most important peaks.

[0091] T...

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Abstract

The present invention relates to a Lu AE58054 hydrochloride crystal form A, a preparation method and uses thereof, wherein the hydrochloride crystal form A has the characteristic peaks in the 25 DEG C X-ray powder diffraction spectrum (Cu K[alpha] radiation) when the 2[theta] value is 17.1+ / -0.2 DEG, 17.8+ / -0.2 DEG, and 21.4+ / -0.2 DEG. According to the present invention, the crystal form A preparation process has characteristics of simple operation and low cost, and the crystal form A has characteristics of good stability, low hygroscopicity, high solubility and easy drug absorption, and provides important significance for reduction of drug loading and preparation of Alzheimer's disease treatment preparations.

Description

technical field [0001] The invention relates to a new crystal form of LuAE58054 hydrochloride, a preparation method and application thereof. Background technique [0002] LuAE58054, also known as Idalopirdine, is a drug for the treatment of Alzheimer's disease that was first developed by Lilly in the United States, and then jointly developed by Lundbeck Pharmaceuticals in Denmark and Otsuka Pharmaceuticals in Japan. LUAE58054 is a selective 5-HT6 receptor antagonist indicated for the treatment of cognitive impairment. 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. Phase II results of the drug showed that LuAE58054 helped improve cognitive function in patients with moderate Alzheimer's disease treated with the drug donepezil. At present, Lundbeck Pharmaceuticals and Otsuka Pharmaceuticals have initiated...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/14A61K31/4045A61P25/28
CPCA61K31/4045C07D209/14C07B2200/13
Inventor 陈敏华张炎锋刘凯张晓宇
Owner CRYSTAL PHARMATECH CO LTD
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