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Crystal form of salt of sb-939 and its preparation method and use

A crystal form, CS1 technology, applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, drug combinations, etc., to achieve the effect of low moisture absorption, good stability, consistent and controllable quality standards

Active Publication Date: 2022-04-26
CRYSTAL PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there is no report on the crystal form information related to SB-939. Therefore, it is necessary to develop a new crystal form of SB-939 and find an advantageous crystal form suitable for pharmaceutical use, so as to meet the requirements of industrial production of drugs

Method used

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  • Crystal form of salt of sb-939 and its preparation method and use
  • Crystal form of salt of sb-939 and its preparation method and use
  • Crystal form of salt of sb-939 and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～2

[0134] Embodiment 1-2: Preparation of crystal form CS7

Embodiment 1

[0136] Weigh 200.1 mg of SB-939 free base solid, add it to 2.5 ml of a mixed system of isopropanol and isopropyl acetate with a volume ratio of 1:1, stir and slowly add 200 microliters of 6 mol / liter hydrochloric acid aqueous solution dropwise , stirred at room temperature for 24 h, the solid was collected by centrifugation, and the crystal form CS7 was obtained after vacuum drying. The crystal form CS7 is a hydrate, and its X-ray powder diffraction pattern is as follows: figure 1 , X-ray powder diffraction data are shown in Table 1.

[0137] The DSC curve of the crystal form CS7 obtained in embodiment 1 is as follows figure 2 As shown, the TGA curve is as image 3 shown.

[0138] Table 1

[0139]

[0140]

Embodiment 2

[0142] Weigh 10.3 mg of SB-939 dihydrochloride raw material, dissolve it in 0.3 ml of water at room temperature, stir and quickly add 3 ml of a mixed solvent system of isopropanol and ethyl acetate with a volume ratio of 1:1, and continue stirring Until a large amount of solids are precipitated, the solids are collected by centrifugation to obtain crystal form CS7, and its X-ray powder diffraction pattern is as follows: Figure 4 shown.

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Abstract

The present invention relates to the crystal form of the salt of compound (I) and its preparation method and application. The new crystal forms CS7, CS9, CS1 and CS3 provided by the present invention have low hygroscopicity, good stability, high purity, low degradation, high solubility and good mechanical stability. It provides new and better options for the preparation of drugs containing compound (I), and is of great significance for drug development.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical crystals. Specifically, it relates to the crystal form of the salt of SB-939 and its preparation method and use. Background technique [0002] Histone deacetylase (Histone Deacetylase, HDAC for short) inhibitors can inhibit the DNA replication and RNA transcription of tumor cells, and can achieve the purpose of treating and preventing tumors. As a class of epigenetic modification enzymes, HDACs play an important role in the structural modification of chromosomes and the regulation of gene expression. Studies have shown that HDAC inhibitors combined with demethylating drugs may have a synergistic effect on the epigenetics of blast cells in acute myeloid leukemia (AML), restoring the expression of tumor suppressor genes in the body. [0003] Pracinostat, also known as SB-939, is a potent oral HDAC inhibitor being developed by MEI Pharmaceuticals. SB-939 is clinically used in the treatment ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D235/08A61K31/4184A61K31/165A61P35/00A61P35/02
CPCA61K31/165A61K31/4184A61P35/00A61P35/02C07D235/08
Inventor 陈敏华张炎锋高慧刘启月张晓宇
Owner CRYSTAL PHARMA CO LTD
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