Crystal form of isoquinoline compound and preparation method of crystal form

A crystal form and diffraction peak technology, applied in the field of medicinal chemistry, can solve problems such as high energy consumption, long cycle time, and difficult process control in industrial production

Inactive Publication Date: 2021-01-08
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Form A has some disadvantages as a medicinal crystal form, such as: it is very difficult to prepare pure Form A. Patent CN109369524A provides three methods for preparing Form A. The cycle of preparing Form A by using the volatile crystallization method and the slurry crystallization method Longer, high energy consumption for industrial production; it is very difficult to control the process by reaction crystallization method, and in the link of adding acetic acid, oil precipitation will occur when the adding speed is fast. New crystalline form of roxadustat produced

Method used

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  • Crystal form of isoquinoline compound and preparation method of crystal form
  • Crystal form of isoquinoline compound and preparation method of crystal form
  • Crystal form of isoquinoline compound and preparation method of crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0171] Embodiment 1: the preparation of crystal form A

[0172] Mix 0.5g of roxadustat sample with 30mL of solvent mixed with acetone / water=3:1 by volume to dissolve all the sample, and let it stand at room temperature to evaporate the solvent to obtain a crystalline solid, which is crystal form A, purity 99.1%. Its X-ray diffraction pattern is as figure 1 shown.

Embodiment 2

[0173] Embodiment 2: the preparation of crystal form B

[0174] Mix 1 g of roxadustat sample with 50 ml of a solvent mixed with ethanol / water = 4:1 by volume to dissolve all the sample, and evaporate the solvent to dryness at room temperature to obtain a crystalline solid, which is Form B with a purity of 99.2%. Its X-ray diffraction pattern is as figure 2 shown.

Embodiment 3

[0175] Embodiment 3: the preparation of crystal form C

[0176] Mix 1g of roxadustat sample with 10ml of solvent mixed with acetone / water=3:1 by volume, heat to 55°C under magnetic stirring conditions, until the sample is completely dissolved, and rapidly cool down to 5°C at a rate of 20°C / h. ℃, kept stirring for 6 hours, and filtered to obtain 0.89 g of a crystal form C sample with a purity of 99.5%.

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Abstract

The invention discloses a crystal form of roxadustat, a preparation method of the crystal form, a pharmaceutical composition of roxadustat and an application of the crystal form in preparation of pharmaceutical preparations for treating diseases such as chronic renal anemia. The crystal form provided by the invention has good stability and druggability, and the preparation process is stable and simple to operate. The structure of roxadustat is shown in the specification;.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a crystal form of roxadustat, a preparation method and application thereof. Background technique [0002] Roxadustat, English name: Roxadustat, trade name: Arizon, chemical name: [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid , the structural formula is shown in formula (1): [0003] [0004] Roxadustat is the world's first oral hypoxia-inducible factor prolyl hydroxylase inhibitor jointly developed by FibroGen and AstraZeneca. It is marketed for the treatment of anemia in dialysis patients with chronic kidney disease (CKD), including hemodialysis and peritoneal dialysis patients. In August 2019, a second clinical indication study was carried out in China, that is, non-dialysis chronic kidney disease (NDD -CKD) anemia. Roxadustat exists in various crystal forms. CN109369525A discloses 12 crystal forms of roxadustat, which...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D217/26A61K31/472A61P7/06
CPCA61P7/06C07B2200/13C07D217/26
Inventor 连小刚何雷周炳城李响
Owner JIANGSU HANSOH PHARMA CO LTD
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