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Crystal form of alkynylpyridine prolyl hydroxylase inhibitor and preparation method thereof

A crystal form and compound technology, which is applied to the crystal form of alkynylpyridine prolyl hydroxylase inhibitors and the field of preparation thereof, can solve the problems of poor fluidity, poor product stability, difficulty in production amplification and the like, and achieve HPLC purity changes. Small size, good crystal stability, and stable production process

Active Publication Date: 2022-06-21
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Generally speaking, amorphous pharmaceutical products have no regular crystal structure and often have other defects, such as poor product stability, difficult filtration, easy agglomeration, poor fluidity, etc. These differences often lead to difficulties in production scale-up
However, the stability of the existing crystal forms needs to be improved

Method used

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  • Crystal form of alkynylpyridine prolyl hydroxylase inhibitor and preparation method thereof
  • Crystal form of alkynylpyridine prolyl hydroxylase inhibitor and preparation method thereof
  • Crystal form of alkynylpyridine prolyl hydroxylase inhibitor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0106] Weigh 10 mg of the compound represented by formula (I) (prepared according to the method disclosed in WO2017059623) into a reaction flask, add 5 ml of dimethyl sulfoxide to dissolve, leave it at room temperature to evaporate to dryness, and obtain about 9 mg of a light yellow solid. The X-ray diffraction pattern of this crystalline sample is shown in figure 1 , whose DSC spectrum is shown in Figure 7 , define this crystal form as A crystal form, and its characteristic peak positions are shown in the table below:

[0107] Table 1. Characteristic peaks of crystal form A

[0108]

[0109]

Embodiment 2

[0111] Weigh 10 mg of the compound represented by formula (I) into a reaction flask, add 5 ml of dichloromethane, place at room temperature and 50° C. for beating for 3 days, filter, and vacuum dry at 40° C. for 2 hours. Both obtained about 8 mg of a light yellow solid, and the X-ray diffraction patterns of the two were consistent. The X-ray diffraction pattern of this crystalline sample is shown in figure 2 , whose DSC spectrum is shown in Figure 8 , define this crystal form as B crystal form, and its characteristic peak positions are shown in the table below:

[0112] Table 2. Characteristic peaks of crystal form B

[0113]

[0114]

Embodiment 3

[0116] Take by weighing the compound shown in 80mg formula (I) and join in the reaction bottle, add 40ml methanol / water mixed solvent (V 水 :V 甲醇 = 1:9) and stirred to dissolve, left at room temperature and evaporated to dryness. About 75 mg of light yellow solid was obtained. The X-ray diffraction pattern of this crystalline sample is shown in image 3 , whose DSC spectrum is shown in Figure 9 , define this crystal form as C crystal form, and its characteristic peak positions are shown in the table below:

[0117] Table 3. Characteristic peaks of crystal form C

[0118]

[0119]

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Abstract

The invention relates to a crystal form of an alkynylpyridine prolyl hydroxylase inhibitor and a preparation method thereof. Specifically, the present invention relates to a new crystal form of an alkynylpyridine prolyl hydroxylase inhibitor represented by formula (I). The new crystal form of the present invention has good stability and can be better used in clinical treatment.

Description

technical field [0001] The invention relates to a crystal form of an alkynylpyridine prolyl hydroxylase inhibitor and a preparation method thereof, and its use in preparing medicines for treating diseases mediated by prolyl hydroxylase. Background technique [0002] Anemia generally refers to any abnormality in hemoglobin or red blood cells that results in reduced oxygen levels in the blood. Anemia can also occur in association with chronic diseases such as chronic infection, neoplastic disease, chronic inflammation including lesions followed by inflammatory suppression of the bone marrow. Anemia of chronic disease is one of the most common syndromes in medicine, such as anemia of chronic kidney disease. The main cause of anemia in chronic kidney disease is insufficient secretion of erythropoietin (EPO) (NephrolDial Transplant 17 (2002) 2-7). Insufficient EPO secretion will hinder the production of red blood cells, leading to anemia. The expression and secretion of EPO ar...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D213/81A61K31/44A61K31/4709A61P7/06
CPCA61K31/44A61P7/06C07D213/81C07B2200/13
Inventor 翟丽娟杜振兴王立坤
Owner JIANGSU HENGRUI MEDICINE CO LTD
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