发明申请
US20160008341A1 CRYSTALLINE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONO MESYLATE MONOHYDRATE HAVING A SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND A SPECIFIC SURFACE AREA RANGE FOR USE IN PHARMACEUTICAL FORMULATIONS
有权
N- [5-（氨基甲酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基]乙酰胺单甲酸酯单磺酸盐具有特定颗粒尺寸 分配范围和用于制药配方的特定面积范围
![CRYSTALLINE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONO MESYLATE MONOHYDRATE HAVING A SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND A SPECIFIC SURFACE AREA RANGE FOR USE IN PHARMACEUTICAL FORMULATIONS](/docs/US/2016-01-14/US20160008341A1/abs.jpg.600x600.jpg)
- 专利标题： CRYSTALLINE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONO MESYLATE MONOHYDRATE HAVING A SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND A SPECIFIC SURFACE AREA RANGE FOR USE IN PHARMACEUTICAL FORMULATIONS
- 专利标题（中）： N- [5-（氨基甲酰基）-4-甲基-1,3-噻唑-2-基] -N-甲基-2- [4-（2-吡啶基）苯基]乙酰胺单甲酸酯单磺酸盐具有特定颗粒尺寸 分配范围和用于制药配方的特定面积范围
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申请号： US14840690申请日： 2015-08-31
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公开(公告)号： US20160008341A1公开(公告)日： 2016-01-14
- 发明人: Wilfried SCHWAB , Alexander BIRKMANN , Kerstin PAULUS , Kurt VOGTLI , Dieter HAAG , Stephan MAAS , Kristian RUEPP
- 申请人： AICURIS GMBH & CO. KG
- 申请人地址： DE Wuppertal
- 专利权人： AICURIS GMBH & CO. KG
- 当前专利权人： AICURIS GMBH & CO. KG
- 当前专利权人地址： DE Wuppertal
- 优先权： EP11007803.7 20110926
- 主分类号： A61K31/4439
- IPC分类号： A61K31/4439 ; A61K45/06 ; A61K9/16
![CRYSTALLINE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONO MESYLATE MONOHYDRATE HAVING A SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND A SPECIFIC SURFACE AREA RANGE FOR USE IN PHARMACEUTICAL FORMULATIONS](/abs-image/US/2016/01/14/US20160008341A1/abs.jpg.150x150.jpg)
摘要：
The present invention relates to the crystalline mono mesylate monohydrate salt of N-[5-(amino sulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide in a definite particle size range, particle size distribution and a specific surface area range, which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions, as well as to pharmaceutical compositions containing said crystalline N-[5-(amino sulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mono mesylate monohydrate having the afore-mentioned particle size range, particle size distribution and specific surface area range. Moreover, the present invention relates to the pharmacokinetic and pharmacodynamic in vivo profiles of the resultant free base of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]-acetamide after administration of the afore-mentioned crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]-acetamide mono mesylate monohydrate salt to a subject in need thereof.
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