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Pharmaceutical salts, crystal form and preparation method of prolyl hydroxylase inhibitor

A technology of crystal form and sodium salt, applied in the preparation of amino hydroxy compounds, preparation of organic compounds, organic chemical methods, etc., can solve the problems of poor fluidity, fine crystallization, difficult filtration, etc.

Active Publication Date: 2019-09-17
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 drug products have no regular crystal structure and often have other defects, such as poor product stability, fine crystallization, difficult filtration, easy agglomeration, poor fluidity, etc.

Method used

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  • Pharmaceutical salts, crystal form and preparation method of prolyl hydroxylase inhibitor
  • Pharmaceutical salts, crystal form and preparation method of prolyl hydroxylase inhibitor
  • Pharmaceutical salts, crystal form and preparation method of prolyl hydroxylase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0104] Weigh 36 mg of the compound represented by formula (I) (prepared according to the method disclosed in WO2017059623) and add it to a reaction flask, add 1.2 ml of methanol, add 105 μl of 1 mol / L sodium hydroxide solution while stirring at room temperature, and stir at room temperature for 30 min. Raise the temperature to 45°C and keep it for 20 minutes; then lower the temperature to 10°C and keep it for 2 hours, centrifuge and dry it in vacuum at 30°C for 3 hours to obtain the I crystal form of the sodium salt of the compound represented by formula (I). Its X-ray diffraction pattern is shown in figure 1 , whose DSC spectrum is shown in Figure 10 , and its characteristic peak positions are shown in the table below:

[0105] Table 1. Characteristic peaks of sodium salt I crystal form

[0106]

Embodiment 2

[0108] Weigh 36 mg of the compound represented by formula (I) and add it to the reaction flask, add 1.2 ml of ethanol, add 105 μl of 1 mol / L sodium hydroxide solution while stirring at room temperature, and stir at room temperature for 30 min. The temperature was raised to 45°C and kept for 20 minutes; the temperature was then lowered to 10°C and kept for 2 hours, and after centrifugation, vacuum-dried at 40°C for 3 hours to obtain the II crystal form of the sodium salt of the compound represented by formula (I). Its X-ray diffraction pattern is shown in figure 2 , whose DSC spectrum is shown in Figure 11 , and its characteristic peak positions are shown in the table below:

[0109] Table 2. Characteristic peaks of sodium salt II crystal form

[0110]

Embodiment 3

[0112] Weigh 36 mg of the compound represented by formula (I) and add it to the reaction flask, add 1.2 ml of acetonitrile, add 105 μl of 1 mol / L sodium hydroxide solution while stirring at room temperature, and stir at room temperature for 30 min. Raise the temperature to 45°C and keep it for 20 minutes; then lower the temperature to 10°C and keep it for 2 hours, centrifuge and dry it in vacuum at 30°C for 3 hours to obtain the III crystal form of the sodium salt of the compound represented by formula (I). Its X-ray diffraction pattern is shown in image 3 , whose DSC spectrum is shown in Figure 12 , and its characteristic peak positions are shown in the table below:

[0113] Table 3. Characteristic peaks of sodium salt III crystal form

[0114]

[0115]

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Abstract

The invention relates to pharmaceutical salts, a crystal form and a preparation method of a prolyl hydroxylase inhibitor, in particular to the pharmaceutical salts, the crystal form and the preparation method of the compound shown in formula (I). The new pharmaceutical salts and the new crystal form have good stability, thus being better applied to clinic treatment.

Description

technical field [0001] The invention relates to a pharmaceutically acceptable salt, crystal form and preparation method of an alkynylpyridine prolyl hydroxylase inhibitor, and its role in the preparation of medicines for treating diseases mediated by prolyl hydroxylase use. 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. ...

Claims

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Application Information

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IPC IPC(8): C07D213/81C07C213/08C07C215/10A61K31/44A61P7/06
CPCC07D213/81C07C213/08C07C215/10A61P7/06C07B2200/13
Inventor 翟丽娟杜振兴王立坤
Owner JIANGSU HENGRUI MEDICINE CO LTD
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