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1. 发明申请

US20160251314A1 2-[[[2-[(HYDROXYACETYL)AMINO]-4-PYRIDINYL]METHYL]THIO]-N-[4-(TRIFLUOROMETHOXY)PHENYL]-3-PYRIDINECARBOXAMIDE BENZENESULFONATE, CRYSTAL OF SAME, CRYSTAL POLYMORPH THEREOF, AND METHODS FOR PRODUCTION THEREOF 审中-公开
标题翻译： 2 - [[[2 - [（羟基乙基）氨基] -4-吡啶基]甲基]硫代] -N- [4-（三氟甲基）苯基] -3-吡啶甲酰氧基苯甲酸酯，其晶体，其晶体聚合物及其方法生产
公开(公告)号：US20160251314A1
公开(公告)日：2016-09-01
申请号：US15150901
申请日：2016-05-10
申请人： Santen Pharmaceutical Co., Ltd.
发明人： Masashi NIWA , Hiroshi DEGUCHI
IPC分类号： C07D213/82 , C07C309/29 , C07C303/32
CPC分类号： C07D213/82 , A61K31/455 , C07B2200/13 , C07C303/32 , C07C309/29 , C07D401/12
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. For solving these problems, we made examination focusing on the kind of the salt and, as a result, found that 1) benzenesulfonate of compound A does not decompose by light, humidity and other factors in a 1-week preliminary stability test (severe test), and has no problem in its storage stability, 2) a method of selectively producing two kinds of crystal forms of benzenesulfonate of compound A, and that 3) no mineral deposition in the stomach is observed even after a 4-week repeated oral administration.
摘要翻译：在开发2 - [[[2 - [（羟基乙酰基）氨基] -4-吡啶基]甲基]硫基] -N- [4-（三氟甲氧基）苯基] -3-吡啶甲酰胺（化合物A）的过程中，多个问题：1）化合物A或其盐难以重结晶，储存稳定性根据盐的种类而有很大差异，难以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，控制晶体多晶型是非常困难的，3）化合物A（游离体）在重复口服给药时会引起胃中的矿物质沉积。为了解决这些问题，我们考察了盐的种类，结果发现化合物A的1）苯磺酸盐在1周的初步稳定性试验（严重试验）中不会被光，湿度等因素分解），并且其储存稳定性没有问题; 2）选择性地生成化合物A的苯磺酸盐的两种晶体形式的方法，以及3）即使在4周的重复口服给药后也没有观察到在胃中的矿物质沉积。

2. 发明申请

US20150291560A1 2-[[[2-[(HYDROXYACETYL)AMINO]-4-PYRIDINYL]METHYL]THIO]-N-[4-(TRIFLUOROMETHOXY)PHENYL]-3-PYRIDINECARBOXAMIDE BENZENESULFONATE, CRYSTAL OF SAME, CRYSTAL POLYMORPH THEREOF, AND METHODS FOR PRODUCTION THEREOF 审中-公开
标题翻译： 2 - [[[2 - [（羟基乙酰基）氨基] -4-吡啶基]甲基]硫代] -N- [4-（三氟甲基）苯基] -3-吡啶甲酰氧基苯甲酸酯，其晶体，其晶体聚合物及其方法生产
公开(公告)号：US20150291560A1
公开(公告)日：2015-10-15
申请号：US14686577
申请日：2015-04-14
申请人： Santen Pharmaceutical Co., Ltd.
发明人： Masashi NIWA , Hiroshi DEGUCHI
IPC分类号： C07D401/12
CPC分类号： C07D213/82 , A61K31/455 , C07B2200/13 , C07C303/32 , C07C309/29 , C07D401/12
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. For solving these problems, we made examination focusing on the kind of the salt and, as a result, found that 1) benzenesulfonate of compound A does not decompose by light, humidity and other factors in a 1-week preliminary stability test (severe test), and has no problem in its storage stability, 2) a method of selectively producing two kinds of crystal forms of benzenesulfonate of compound A, and that 3) no mineral deposition in the stomach is observed even after a 4-week repeated oral administration.
摘要翻译：在开发2 - [[[2 - [（羟基乙酰基）氨基] -4-吡啶基]甲基]硫基] -N- [4-（三氟甲氧基）苯基] -3-吡啶甲酰胺（化合物A）的过程中，多个问题：1）化合物A或其盐难以重结晶，储存稳定性根据盐的种类而有很大差异，难以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，控制晶体多晶型是非常困难的，3）化合物A（游离体）在重复口服给药时会引起胃中的矿物质沉积。为了解决这些问题，我们考察了盐的种类，结果发现化合物A的1）苯磺酸盐在1周的初步稳定性试验（严重试验）中不会被光，湿度等因素分解），并且其储存稳定性没有问题; 2）选择性地生成化合物A的苯磺酸盐的两种晶体形式的方法，以及3）即使在4周的重复口服给药后也没有观察到在胃中的矿物质沉积。

3. 发明申请

US20170081286A1 2-[[[2-[(HYDROXYACETYL)AMINO]-4-PYRIDINYL]METHYL]THIO]-N-[4-(TRIFLUOROMETHOXY)PHENYL]-3-PYRIDINECARBOXAMIDE BENZENESULFONATE, CRYSTAL OF SAME, CRYSTAL POLYMORPH THEREOF, AND METHODS FOR PRODUCTION THEREOF 审中-公开
公开(公告)号：US20170081286A1
公开(公告)日：2017-03-23
申请号：US15368028
申请日：2016-12-02
申请人： Santen Pharmaceutical Co., Ltd.
发明人： Masashi NIWA , Hiroshi DEGUCHI
IPC分类号： C07D213/82
CPC分类号： C07D213/82 , A61K31/455 , C07B2200/13 , C07C303/32 , C07C309/29 , C07D401/12
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. For solving these problems, we made examination focusing on the kind of the salt and, as a result, found that 1) benzenesulfonate of compound A does not decompose by light, humidity and other factors in a 1-week preliminary stability test (severe test), and has no problem in its storage stability, 2) a method of selectively producing two kinds of crystal forms of benzenesulfonate of compound A, and that 3) no mineral deposition in the stomach is observed even after a 4-week repeated oral administration.

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