Crystal form of rosustat and preparation method thereof

A technology of roxadustat and crystal form, which is applied in the directions of organic chemical methods, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of poor solubility, insolubility, and low solubility of crystal form A, and achieves the preparation method. Simple, high crystal form purity, good crystal form stability

Active Publication Date: 2021-03-16
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent CN109369524A discloses four crystal forms of roxadustat, namely Form A, Form B, Form C and Form D, wherein Form A is a pure crystal form, and Form B is a hydrate crystal form, which can Spontaneously converted to Form A, Form C is a solvate containing hexafluoropropan-2-ol, and Form D is a solvate containing DMSO and water; patent WO2013013069 discloses seven crystal forms of roxadustat, which are Form I, Form II, FormIII, Form IV, Form V, Form VI and Form VII, most of these crystal forms are solvates and are not suitable for development as pharmaceutical crystal forms; patent CN109369525A discloses 12 crystal forms of roxadustat, They are crystalline form ARE-A, crystalline form ARE-B, crystalline form

Method used

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  • Crystal form of rosustat and preparation method thereof
  • Crystal form of rosustat and preparation method thereof
  • Crystal form of rosustat and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0224] Embodiment 1: Preparation of crystal form D

[0225] Mix 1g of roxadustat sample with 10mL of acetone / water=3:1 mixed solvent, heat to 55°C until the sample is completely dissolved, slowly cool down to 50°C, add 20ml of ethanol, add 20mg of seed crystals, keep stirring for 6h, filter , the sample was vacuum-dried at 50°C for 24 hours to obtain 0.91 g of Form D with a purity of 99.66%.

Embodiment 2

[0226] Embodiment 2: the preparation of crystal form D

[0227] Mix 1g of roxadustat sample with 10mL of acetone / water=4:1 mixed solvent, heat to 65°C until the sample is completely dissolved, slowly cool down to 50°C, add 30ml of ethanol, add 10mg of seed crystals, keep stirring for 6h, filter , the sample was vacuum-dried at 50°C for 24h to obtain 0.95g of Form D with a purity of 99.68%. Its X-ray diffraction pattern is as figure 1 shown. Its TGA spectrum is as figure 2 shown.

Embodiment 3

[0228] Embodiment 3: the preparation of crystal form D

[0229] Mix 1g of roxadustat sample with 10mL of acetone / water=3:1 mixed solvent, heat to 55°C until the sample is completely dissolved, slowly cool down to 35°C, add 30mg of seed crystals, keep stirring for 6h, and slowly cool down to 2°C , and filtered to obtain 0.93g of Form D with a purity of 99.65%.

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PUM

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Abstract

The invention discloses a crystal form of rosustat, a preparation method of the crystal form, a pharmaceutical composition of rosustat and an application of rosustat in treating diseases such as chronic renal anemia. The structure of rosustat is as follows in the specification.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a crystal form of roxadustat and a preparation method and application thereof. Background technique [0002] Roxadustat, the English name is Roxadustat, the Chinese name is: Trade name: The chemical name is [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, and the structural formula is as 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. Globally, this drug was first clinically studied in China, and was launched in December 2018. It was first launched in China in August 2019 for the treatment of anemia in dialysis patients with chronic kidney disease (CKD), including hemodialysis and peritoneal dialysis. Renal (NDD-CKD) anemia. This drug has four characteristics: First, its curative effect is not affected by ...

Claims

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Application Information

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IPC IPC(8): C07D217/26A61K31/472A61P13/12A61P7/06
CPCC07D217/26A61P13/12A61P7/06C07B2200/13
Inventor 连小刚李响周炳城魏娜
Owner JIANGSU HANSOH PHARMA CO LTD
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