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Ivabradine compound, preparation method and pharmaceutical composition thereof

A technology of ivabradine and compounds, applied in the field of new ivabradine compounds, can solve problems such as unfavorable left ventricular systolic function, and achieve the effects of being conducive to production and storage, less types of use, and easy to operate

Active Publication Date: 2012-01-04
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the most commonly used drug for lowering heart rate clinically is β-blocker, which can effectively reduce the occurrence of angina to a large extent by lowering heart rate, but its side effects (including fatigue, depression and sexual function) Obstacles, etc.) and its contraindications (including airway obstruction, atrioventricular block, decompensated heart failure, etc.) and the inherent negative inotropic effect of β-blockers have adverse effects on left ventricular systolic function , so that the use of β-blockers by clinicians and the compliance of patients are limited to a certain extent

Method used

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  • Ivabradine compound, preparation method and pharmaceutical composition thereof
  • Ivabradine compound, preparation method and pharmaceutical composition thereof
  • Ivabradine compound, preparation method and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1: the preparation of ivabradine hydrochloride

[0030] Dissolve 5.05g (0.01mol) of ivabradine in 400ml of acetone, add 40ml of acetone solution dissolved in 0.365g (0.01mol) of hydrochloric acid while stirring at room temperature, continue stirring for 60 minutes after the addition, and then put it in an ice bath Stir for another 40 minutes, filter, wash the filter cake with 80ml of acetone, and dry at 60°C for 2h in a circulating air drier to obtain 5.01g of ivabradine hydrochloride anhydrate, with a yield of 95.8%.

[0031] Elemental analysis:

[0032]

Embodiment 2

[0033] Embodiment 2: the preparation of ivabradine compound of the present invention

[0034] Take 2g of ivabradine hydrochloride in Example 1, add 100ml of hot water at 60°C to dissolve, cool to 15°C and stir for 1 hour, then cool to 10°C and stir for 1 hour, finally cool to -5°C, and stir for 10 hours, Crystals were precipitated, filtered, and the filter cake was dried at 20° C. and 50% relative humidity for 4 hours to obtain 1.73 g of the ivabradine compound of the present invention, with a yield of 86.3%.

[0035] Elemental analysis:

[0036]

[0037] The water in the ivabradine compound of the present invention measured by Karl Fischer method is 3.36% (theory: 3.44%); the thermogravimetric analysis result shows that it is the characteristic of monohydrate.

Embodiment 3

[0038] Embodiment 3: the preparation of ivabradine compound of the present invention

[0039] Take 2g of ivabradine hydrochloride in Example 1, add 100ml of 60°C hot water to dissolve, cool to 20°C and stir for 1 hour, then cool to 5°C and stir for 1 hour, finally cool to 0°C, stir for 10 hours, Crystals were precipitated, filtered, and the filter cake was dried at 40° C. and 70% relative humidity for 10 hours to obtain 1.75 g of the ivabradine compound of the present invention with a yield of 87.3%.

[0040] Elemental analysis:

[0041]

[0042] The moisture in the ivabradine compound of the present invention measured by Karl Fischer method is 3.48% (theory: 3.44%); the thermogravimetric analysis result shows that it is the characteristic of monohydrate.

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PUM

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Abstract

The invention relates to an ivabradine compound, a preparation method and a pharmaceutical composition thereof, in particular to 7,8-dimethoxy-3-{3-[[(1S)(4,5-dimethoxybenzo cyclobutane-1-yl)methyl]-methylamino]propyl}-1,3,4,5-tetrahydro-dihydro-benzoazepine-2-ketone, namely ivabradine hydrochloride hydrate, and further to a preparation method of the compound and a pharmaceutical composition by taking the compound as an active substance. Compared with the ivabradine hydrochloride, the compound disclosed by the invention has better stability and is better applied to preparing, storing and applying pharmaceutical preparations in various forms.

Description

technical field [0001] The invention relates to a new ivabradine compound, in particular to an ivabradine hydrate, a preparation method and a pharmaceutical composition thereof, belonging to the field of medicine. Background technique [0002] Heart rate is an important risk factor for coronary heart disease and other cardiovascular diseases. Reducing heart rate is not only beneficial to the prevention of angina pectoris, but also more conducive to the prognosis of patients with coronary heart disease, and plays an important role in improving the survival rate of patients with coronary heart disease. At present, the most commonly used drug for lowering heart rate clinically is β-blocker, which can effectively reduce the occurrence of angina to a large extent by lowering heart rate, but its side effects (including fatigue, depression and sexual function) Obstacles, etc.) and its contraindications (including airway obstruction, atrioventricular block, decompensated heart failu...

Claims

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Application Information

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IPC IPC(8): C07D223/16A61K31/55
Inventor 高志峰张文静董新明刘聪敏周杰孙鹏
Owner CSPC OUYI PHARM CO LTD
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