首页> 外国专利> 2-2-(HYDROXYACETYL)AMINO-4-PYRIDINYLMETHYLTHIO-N-4-(TRIFLUOROMETHOXY)PHENYL-3-PYRIDINECARBOXAMIDE BENZENESULFONATE CRYSTAL OF SAME CRYSTAL POLYMORPH THEREOF AND METHODS FOR PRODUCTION THEREOF

2-2-(HYDROXYACETYL)AMINO-4-PYRIDINYLMETHYLTHIO-N-4-(TRIFLUOROMETHOXY)PHENYL-3-PYRIDINECARBOXAMIDE BENZENESULFONATE CRYSTAL OF SAME CRYSTAL POLYMORPH THEREOF AND METHODS FOR PRODUCTION THEREOF

机译:相同晶体多晶型物的2-[[[[[2-[(羟基乙酰基)酰胺基] -4-吡啶基]甲基]硫代] -N- [4-(三氟代乙氧基)苯基] -3-吡啶甲酸苯磺酸磺酸盐结晶及其制备方法

摘要

In the course of developing 2-[[[2 - [(hydroxyacetyl) amino]- 4 -pyridinyl] methyl] thio]- N -[4 -(trifluoromethoxy) phenyl]- 3 -pyridinecarboxamide(compound A)  there are the multiple problems: 1) compound A or its salt is difficult to be recrystallized  the storage stability largely differs depending on the kind of the salt  and it is very difficult to obtain a salt of compound A having excellent storage stability; 2) in a crystallization process of compound A  it is very difficult to control a crystal polymorph  and 3) compound A (free body) causes mineral deposition in the stomach when it is orally administered repeatedly.
机译:在开发2-[[[[[2-[(羟基乙酰基)氨基]-4-吡啶基]甲基]硫代]-N-[4-(三氟甲氧基)苯基]-3-吡啶甲酰胺(化合物A)的过程中,存在多种问题:1)化合物A或其盐难以重结晶,其储存稳定性因盐的种类而异,很难获得具有优异储存稳定性的化合物A的盐; 2)在化合物A的结晶过程中,很难控制晶体多晶型物; 3)反复口服时,化合物A(游离体)在胃中引起矿物质沉积。

著录项

  • 公开/公告号IN1152DEN2012A

    专利类型

  • 公开/公告日2015-04-10

    原文格式PDF

  • 申请/专利权人 SANTEN PHARMACEUTICAL CO.  LTD.;

    申请/专利号IN2012DELNP1152

  • 发明设计人 MASASHI NIWA;HIROSHI DEGUCHI;

    申请日2012-02-07

  • 分类号C07D;

  • 国家 IN

  • 入库时间 2022-08-21 15:15:11

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