- Patent Title: 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
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Application No.: US14840690Application Date: 2015-08-31
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Publication No.: US09889124B2Publication Date: 2018-02-13
- Inventor: Wilfried Schwab , Alexander Birkmann , Kerstin Paulus , Kurt Vogtli , Dieter Haag , Stephan Maas , Kristian Ruepp
- Applicant: AICURIS ANTI-INFECTIVE CURES GMBH
- Applicant Address: DE Wuppertal
- Assignee: AICURIS ANTI-INFECTIVE CURES GMBH
- Current Assignee: AICURIS ANTI-INFECTIVE CURES GMBH
- Current Assignee Address: DE Wuppertal
- Agency: Millen White Zelano and Branigan, PC
- Agent Csaba Henter; John Sopp
- Priority: EP11007803 20110926
- Main IPC: A61K45/06
- IPC: A61K45/06 ; A61K9/14 ; A61K31/4439 ; C07D417/12 ; A61K31/10 ; 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/2018/02/13/US09889124B2/abs.jpg.150x150.jpg)
Abstract:
The present invention relates to the crystalline mono mesylate monohydrate salt of N-[5 -(aminosulfonyl)-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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