您的位置: 首页 > 农业专利 > 详情页

NEW CO-CRYSTALS OF AGOMELATINE, A PROCESS FOR THEIR PREPARATION 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:
NZ60047912
公开号:
NZ600479A
申请日:
2012.06.06
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
ABSTRACT - 600479 The disclosure relates to a co-crystal of agomelatine, characterised in that it is composed of: (i) agomelatine, or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide of formula (I), and (ii) an organic acid which is in a solid state at ambient temperature chosen from parahydroxybenzoic acid, citric acid, oxalic acid, gallic acid, maleic acid, malonic acid, glutaric acid, glycolic acid or ketoglutaric acid. Also disclosed is a process for obtaining said co-crystal comprising the following steps wherein: (i) the two constituents are mixed in an organic solvent in the desired proportions (1 equivalent of agomelatine per 0.25 to 4 molar equivalents of organic acid), preferably the two constituents are co-ground; (ii) the solution obtained is stirred and optionally heated at a temperature not greater than the boiling point of the selected solvent; (iii) the mixture is cooled, with stirring, and the co-crystal precipitates naturally or precipitates after taking up in a second solvent; (iv) the precipitate obtained is filtered and dried. These co-crystals are suitable for treating stress, sleep disorders, anxiety disorders and especially generalised anxiety disorder, obsessive-compulsive disorders, mood disorders and especially bipolar disorders, major depression, seasonal affective disorder, cardiovascular pathologies, pathologies of the digestive system, insomnia and fatigue due to jet-lag, schizophrenia, panic attacks, melancholia, appetite disorders, obesity, insomnia, pain, psychotic disorders, epilepsy, diabetes, Parkinson's disease, senile dementia, various disorders associated with normal or pathological ageing, migraine, memory loss, Alzheimer's disease, and also in cerebral circulation disorders, and also in sexual dysfunctions, and as ovulation inhibitors and immunomodulators and in the treatment of cancers.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

意 见 箱

匿名:登录

个人用户登录

找回密码

第三方账号登录

忘记密码

个人用户注册

必须为有效邮箱
6~16位数字与字母组合
6~16位数字与字母组合
请输入正确的手机号码

信息补充