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Novel crystal form of roxadustat and preparation method of novel crystal form

A crystal form, ARZ-A technology, applied in the field of medicinal chemistry, can solve the problems of unsuitability for industrial production, poor crystal form stability, poor solubility, etc.

Inactive Publication Date: 2019-02-22
ANLITE SHANGHAI PHARMA TECH CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] It can be seen from the above prior art that although roxasil has various crystal forms, most of the crystal forms have problems such as poor stability, poor solubility or unsuitable for industrial production.

Method used

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  • Novel crystal form of roxadustat and preparation method of novel crystal form
  • Novel crystal form of roxadustat and preparation method of novel crystal form
  • Novel crystal form of roxadustat and preparation method of novel crystal form

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preparation example Construction

[0157] Aiming at the problems and needs of the prior art, the present invention provides a new crystal form of roxadustat which has excellent solubility and stability and is very suitable for formulation production and a preparation method thereof.

[0158] The first aspect of the present invention provides the crystal form of roxadustat (that is, the compound of formula I), which is selected from the group consisting of crystal form ARZ-A, crystal form ARZ-B, and crystal form ARZ-C , crystal form ARZ-D, crystal form ARZ-E, crystal form ARZ-F, crystal form ARZ-G, crystal form ARZ-H, crystal form ARZ-I, crystal form ARZ-J, or crystal form ARZ-K.

[0159]

[0160] In a specific embodiment, the crystal form provided by the present invention is crystal form ARZ-A, and the crystal form ARZ-A is a monohydrate.

[0161] Furthermore, the X-ray powder diffraction pattern of the crystal form ARZ-A has characteristic peaks at 2θ of 6.7±0.2°, 8.0±0.2°, 9.3±0.2, and 13.2±0.2°.

[0162] F...

Embodiment 1

[0368] Example 1: Preparation of roxadustat crystal form ARZ-A

Embodiment 11

[0369] Example 1.1: Preparation of roxadustat crystal form ARZ-A

[0370] At 60°C, dissolve 30mg of roxadustat raw material in 1.5mL formic acid / methanol (1:1) to obtain a clear solution; cool to room temperature and filter, put the filtrate in a -20°C freezer to freeze, and then place it in a freezer Freeze-dried product was obtained by machine drying. The resulting solid was in crystalline form ARZ-A. Carry out XRPD test to the obtained solid, its X-ray powder diffraction pattern is as follows figure 1 Shown; Carry out TGA test to gained solid, its spectrogram is as figure 2 Shown; Carry out DSC test to gained solid, its spectrogram is as image 3 shown; the obtained solid was 1 H-NMR test, its spectrum is as follows Figure 4 shown.

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Abstract

The invention provides a novel crystal form of roxadustat and a preparation method of the novel crystal form. The crystal form ARZ-A has better stability and solubility than existing crystal forms. The preparation process of the crystal form is simple and feasible, a used solvent has low toxicity, stability of the crystal form is good, and the crystal form is more suitable for process scale-up production.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a new crystal form of roxadustat and a preparation method thereof. Background technique [0002] Roxadustat, English name Roxadustat, its chemical name: [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, trade name: can Bomei, the molecular formula is: C 19 h 16 N 2 o 5 , molecular weight: 352.11, CAS number: 808118-40-3, chemical structural formula: [0003] [0004] The drug is developed by FibroGen for the treatment of renal anemia. It was applied for marketing in China in November 2017. It is in phase III clinical trials in the United States and Europe. In the second half of 2018, an NDA application was submitted in the United States. [0005] WO2014014835 discloses roxadustat crystal forms Form A, Form B, Form C and Form D and their preparation methods, wherein: Form A is anhydrous, Form B is hemihydrate, and Form C is...

Claims

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Application Information

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IPC IPC(8): C07D217/26A61P13/12A61P7/06A61K31/472
CPCA61P7/06A61P13/12C07B2200/13C07D217/26
Inventor 李庆秋申淑匣修平张良
Owner ANLITE SHANGHAI PHARMA TECH CO LTD
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