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Co Crystals of agomelatine, Preparation method thereof and Pharmaceutical compositions containing them
专利权人:
LES LABORATOIRES SERVIER
发明人:
LETELLIER PHILIPPE,LYNCH MICHAEL,PEAN JEAN-MANUEL
申请号:
ARP120102011
公开号:
AR086849A1
申请日:
2012.06.07
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
An acrylonitrile copolymer consisting of acrylonitrile or N - [2 - (7-methyl-1-naftl) ethyl] formula (1) and an organic acid. Drug demand 1: common glass characterized by added agommelatine: by agommelatine or N - [2 - (7) - metoxy-1-naphthyl) ethyl] acetamide of formula (1) and by an organic acid that has a solid state at room temperature. Claim 3: Co-crystal according to claim 1 or 2 characterized in that the organic acid used is parahydroxybenzoic acidcitric acid, oxalic acid, gallic acid, maleic acid, malonic acid, glutaric acid, glycolic acid or ketoglutaric acid. Claim 6: Co-crystal according to one of claims 1 to 5 which is N- [2- (7-methoxy-1-naphthyl) ethyl] acetamide / parahydroxybenzoic acid (2/1) characterized in its powder X diffraction diagram by the Bragg 2q angles (expressed in º ± 0.2) 13.16º,14.91 degrees17.37%Eighteen point three nine18.93 degrees19.04%19.65 degrees19.96 degreesTwenty point two fiveTwenty-one point four nine25 degrees 19. Claim 16: the procedure for obtaining copolymers according to one of the requirements from 1 to 15: two components are mixed in an ideal proportion in an organic solvent (one equivalent to 0.25-4 equivalent to an agomatine of an organic acid abrasive);The resulting solution will be shaken, optionally heated, at a temperature not exceeding the boiling temperature of the selected solution; the environment will cool due to disturbance; after the second solvent is collected, CO glass will accelerate naturally or hastily; the resulting precipitates will be filtered and dried. Claim 22: the pharmaceutical ingredients in claim 20 are used to produce drugs for the treatment of stress, sleep disorder and anxiety disorder, mainly general anxiety disorder, obsessive-compulsive disorder and emotional disorder, mainly bipolar disorder, Great DepressionSeasonal depression, cardiovascular disease, digestive system disease, insomnia and fatigue due to time difference, schizophrenia, panic attack, depression, anorexia, obesity, i
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