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Vonoprazan fumarate compound and pharmaceutical composition thereof

A fumarate compound and compound technology, applied in the field of medicinal chemistry, can solve the problems of PPI can not fully inhibit the acid secretion at night, do not provide compound crystal information, can not continuously control the acid secretion, etc. Short, low-cost effects

Inactive Publication Date: 2016-05-11
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still some problems in PPI therapy in clinical practice: (1) PPI is unstable to acid, so it needs to be administered in the form of acid-protective preparations (such as enteric-coated tablets); The full effect can be achieved within 3 to 5 days after treatment; (3) In different patients, the efficacy of PPI is affected by the metabolism of CYP2C19. Acid secretion, in addition, PPIs have been found to not adequately suppress nocturnal acid secretion in some patients
[0007] Example 8 in CN101300229A discloses a 1-[5-(2-fluorophenyl)-1-(3-pyridylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethylamine fuma The preparation method of acid salt, the crystal information of the compound is not provided
In addition, the applicant also found that by adding titanium dioxide and a chain organic acid to the solid preparation containing the pharmaceutical active ingredient, the stability of the pharmaceutical active ingredient during light exposure can be improved, and the application documents did not provide crystal information of the compound

Method used

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  • Vonoprazan fumarate compound and pharmaceutical composition thereof
  • Vonoprazan fumarate compound and pharmaceutical composition thereof
  • Vonoprazan fumarate compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Suspend the crude product of Vonoprazan fumarate (1g) in a mixed solvent of ethanol / water (3:1, 10mL), heat to dissolve at an internal temperature of 60-65°C, slowly cool down to room temperature, stir for 1h, and then cool down to the internal temperature Stir and crystallize at 0-10°C for 1h, filter, and vacuum-dry at 50°C for 8h to obtain 0.741g of white crystalline powder with a yield of 74.1%.

Embodiment 2

[0037] Suspend the crude Vonoprazan fumarate (1g) in a mixed solvent of ethanol / water (1:1, 15mL), heat to dissolve at an internal temperature of 60-65°C, slowly cool down to room temperature, stir for 1h, and then cool down to the internal temperature Stir and crystallize at 0-10°C for 1h, filter, and vacuum-dry at 50°C for 8h to obtain 0.663g of white crystalline powder with a yield of 66.3%.

Embodiment 3

[0039] Suspend the crude Vonoprazan fumarate (1g) in a mixed solvent of ethanol / water (1:2, 21mL), heat to dissolve at an internal temperature of 50-60°C, slowly cool down to room temperature, stir for 3 hours, and then cool down to the internal temperature Stir and crystallize at 0-10°C for 3h, filter, and vacuum-dry at 40°C for 10h to obtain 0.654g of white crystalline powder with a yield of 65.4%.

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PUM

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Abstract

The invention provides a new crystal-form Vonoprazan fumarate compound and a preparation method and a pharmaceutical composition thereof. The Vonoprazan fumarate compound has the advantages of good stability and low hygroscopicity, and conforms to the medicinal requirements. The preparation process of the compound provided by the invention is stable and has good repeatability, conforms to the requirements of industrialized mass production, and has important application value in preparation of medicines.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a Vonoprazan fumarate compound in a new crystal form, a pharmaceutical composition and a preparation method thereof. Background technique [0002] At present, proton pump inhibitors (PPIs) have been widely used to treat various acid-related diseases, such as gastroesophageal reflux disease (GERD), peptic ulcer, and also used in combination with antibiotics to eradicate Helicobacter pylori. However, there are still some problems in PPI therapy in clinical practice: (1) PPI is unstable to acid, so it needs to be administered in the form of acid-protective preparations (such as enteric-coated tablets); The full effect can be achieved within 3 to 5 days after treatment; (3) In different patients, the efficacy of PPI is affected by the metabolism of CYP2C19. Acid secretion. In addition, PPIs were found to be insufficient in suppressing nocturnal acid secretion in some p...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61K31/4439A61P1/04
Inventor 陈庆财赵俊赵小伟宗在伟赵骞付锐周长岭吕伟
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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