首页> 外国专利> Process to prepare a base of (+) - norcisapride ((+) - 4 - amino - 5 - Chloro - N - (3 - (4 - methoxy piperidinil) - 2 - metoxibenzamida), The Compound, Salt thereof, Pharmaceutical composition containing itProcess for preparing the composition, its use for the manufacture of a Medicament and compounds

Process to prepare a base of (+) - norcisapride ((+) - 4 - amino - 5 - Chloro - N - (3 - (4 - methoxy piperidinil) - 2 - metoxibenzamida), The Compound, Salt thereof, Pharmaceutical composition containing itProcess for preparing the composition, its use for the manufacture of a Medicament and compounds

机译:制备(+)-正西沙必利((+)-4-氨基-5-氯-N-(3-(4--甲氧基哌啶子)-2-甲氧西ib]的碱的方法,化合物,其盐,包含用于制备组合物的方法,其在制备药物和化合物中的用途

摘要

A process to prepare a base of (+) - norcisapride ((+) - 4 - amino - 5 - Chloro - N - (4 - methoxy - 3 - 2 - metoxibenzamida piperidinil) of formula (i) comprising: (a) to separate the Enantiomers of cis - Ethyl 4 - (AMIno - 5 - Chloro - 2 - methoxy - benzoylamino) - 3 - methoxy - 3 - carboxylate piperidin through the cromatografu00edalu00edquida on a Chiral stationary Phase, and (b) Isolating The fraction that is dextrorotatorio,And (c) to (+) The fraction solvolizar - norcisapride; dichocompuesto, Salt thereof, Pharmaceutical composition containing itProcess for preparing the composition for use in the manufacture of a medicamentopara Treat Gastrointestinal Disorders whileAt the same time Preventing effects on the central nervous system and compuestosintermediarios for exclusive use in this process.In view of its activity 5-ht3 antagonist, (+) - norcisopride is useful for the treatment of disorders associated with over Stimulation of the activity of the 5-ht3 receptor, e.g.Vomiting, for example vomiting induced by a Drug and radiation etotoxica, irritable bowel syndrome, especially with diarrhea predominant irritable bowel syndrome.And trastornosrelacionados.
机译:制备式(i)的(+)-正西沙必利((+)-4-氨基-5-氯-N-(4--甲氧基-3-2-甲氧西ib苯甲酰胺哌啶啶)的碱的方法,包括:(a)至通过手性固定相上的cromatograf ueded u00edquida分离出顺式-乙基4-(AMIno-5-氯-2-甲氧基-苯甲酰氨基)-3-甲氧基-3-羧酸酯哌啶的对映体,并(b)分离(c)至(+)的部分为溶剂灵盐-诺西沙必利; dichocompuesto,其盐,含有该药物的药物组合物的制备用于制造药物的组合物的方法治疗胃肠道疾病,同时预防鉴于其具有5-ht3拮抗剂的活性,(+)-去甲西立必利可用于治疗与过度刺激5-ht3受体活性有关的疾病,例如:呕吐例如,由药物引起的呕吐和放射性毒素,肠易激综合症,尤其是腹泻为主的肠易激综合症。

著录项

  • 公开/公告号AR013200A1

    专利类型

  • 公开/公告日2000-12-13

    原文格式PDF

  • 申请/专利权人 JANSSEN PHARMACEUTICA N.V.;

    申请/专利号AR1998P103375

  • 发明设计人

    申请日1998-07-10

  • 分类号C07D211/58;A61K31/445;C07B57/00;

  • 国家 AR

  • 入库时间 2022-08-22 01:26:21

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