公开(公告)号：US20100197732A1

公开(公告)日：2010-08-05

申请号：US12663106

申请日：2008-06-05

申请人： Sonny Sebastian ,  Sasidhar Venkata Balla ,  Ramamurthy Katikareddy ,  Nitin Sharadchandra Pradhan ,  Jon Valgeirsson

发明人： Sonny Sebastian ,  Sasidhar Venkata Balla ,  Ramamurthy Katikareddy ,  Nitin Sharadchandra Pradhan ,  Jon Valgeirsson

IPC分类号： A61K31/4545 ,  C07D211/26 ,  C07D211/32 ,  A61K31/4453 ,  A61P3/10

CPC分类号： C07D295/135

摘要： The present invention provides highly pure repaglinide substantially free of dimer impurity, and process for the preparation thereof. The present invention also relates to 2-ethoxy-N-[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]-4-[2-[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzamide, an impurity of repaglinide, and a process for preparing and isolating thereof. The present invention further relates to pharmaceutical compositions comprising solid particles of pure repaglinide substantially free of dimer impurity or pharmaceutically acceptable salts thereof, wherein 90 volume-percent of the particles (D90) have a size of less than about 400 microns. The present invention also provides an optical resolution method of racemic 3-methyl-1-(2-piperidino-phenyl)-1-butylamine and use thereof for the preparation of repaglinide.

摘要翻译： 本发明提供了基本上不含二聚体杂质的高纯度瑞格列奈及其制备方法。 本发明还涉及2-乙氧基-N - [（1S）-3-甲基-1- [2-（1-哌啶基）苯基]丁基] -4- [2 - [[（1S）-3-甲基 -1- [2-（1-哌啶基）苯基]丁基]氨基] -2-氧代乙基]苯甲酰胺，瑞格列奈的杂质及其制备和分离方法。 本发明还涉及包含基本上不含二聚体杂质的纯瑞格列奈的固体颗粒或其药学上可接受的盐的药物组合物，其中90体积％的颗粒（D90）具有小于约400微米的尺寸。 本发明还提供外消旋3-甲基-1-（2-哌啶子基 - 苯基）-1-丁胺的光学拆分方法及其在制备瑞格列奈中的应用。