New process for obtaining the crystalline form v of agomelatine

A technology of crystal form and compound, applied in the field of V crystal form of agomelatine or N-[2-ethyl]acetamide, can solve problems such as short storage stability period

Inactive Publication Date: 2012-12-12
LES LAB SERVIER
View PDF6 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the shelf life is short and in all cases less than 6 months

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • New process for obtaining the crystalline form v of agomelatine
  • New process for obtaining the crystalline form v of agomelatine
  • New process for obtaining the crystalline form v of agomelatine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 : Form V of N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide

[0022] A 10 g / l solution of agomelatine in an ethanol / isopropyl ether mixture (50 / 50: v / v) was introduced into the atomizer of a BUCHI 190 mini spray dryer. The inlet temperature of the drying chamber was 90°C and the outlet temperature was 66°C. The aerosolized powder was recovered in a collection bowl and identified using the following crystallographic data:

[0023] 1) Spectrum obtained with a Siemens D5005 diffractometer, using a 2θ angle range of 3°-30°, a span of 0.04° and 4 seconds per span:

[0024] - crystal structure of the unit cell: monoclinic,

[0025] -Unit cell parameter: a=11.967 b=17.902 c=15.423 β=124.5°

[0026] - Space group: P2 1 / n

[0027] - Number of molecules in the unit cell: 8 (Z'=2)

[0028] - the volume of the unit cell: V 晶胞 =2720.0

[0029] 2) The X-ray powder diffraction pattern below, which is measured with a Siemens D5005 diffractometer (copper to cathod...

Embodiment 2

[0031] Example 2 : Stability over time of crystal form V of N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide obtained by nebulization

[0032] A 1 g sample of the compound obtained in Example 1 was placed under normal storage conditions: ambient pressure and temperature. After 21 months, the diffractogram of the obtained sample has not changed, it still has the characteristics of the obtained crystal form V.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

Process for preparing crystalline form of N-[2-(7-methoxy-naphthalen- 1-yl)-ethyl]-acetamide (or agomelatine) comprises dissolving a solution of agomelatine in one or two solvents miscible in all proportions, where the boiling temperature is less than 120[deg] C, and the solution is atomized in an atomizer. - ACTIVITY : Antidepressant; Hypnotic; Cardiovascular-Gen.; CNS-Gen.; Muscular-Gen.; Eating-Disorders-Gen.; Anorectic. - MECHANISM OF ACTION : 5-Hydroxytryptamine 2C receptor antagonist.

Description

technical field [0001] The present invention relates to a new process for obtaining the V crystal form of agomelatine or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide of formula (I): [0002] Background technique: [0003] Agomelatine or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide has valuable pharmacological properties. [0004] In fact, it has dual properties, on the one hand it is an agonist of receptors of the melatonergic system and on the other hand it is a 5-HT 2C receptor antagonists. These properties make it central nervous system active and more particularly useful in the treatment of major depression, seasonal affective disorder, sleep disorders, cardiovascular conditions, digestive conditions, insomnia and fatigue due to jet lag, appetite disorders and obesity. active. [0005] Agomelatine, its preparation and its use in therapy have been described in European patent EP 0 447 285 . [0006] Given its medicinal value, this compound is obtained in excellent puri...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Patents(China)
IPC IPC(8): C07C233/18C07C231/24A61P25/28A61P25/24A61P25/20A61P25/00A61P9/00A61P1/00A61P3/04
CPCC07C231/24C07C233/18A61P1/00A61P15/08A61P25/00A61P25/20A61P25/24A61P25/28A61P3/00A61P3/04A61P37/00A61P9/00C07C231/00C07C233/08
Inventor D·马丁斯G·科克雷尔J·里诺尔P·朗格卢瓦
Owner LES LAB SERVIER
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap