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

US9119786B2 · kind B2 · utility

Assignee

• AiCuris GmbH & Co. KG · DE

Inventors

• Wilfried Schwab · Altentreptow, DE
• Alexander Birkmann · Wuppertal, DE
• Kerstin Paulus · Ratingen, DE
• Kurt Vogtli · Oberhofen, CH
• Dieter Haag · Ramlinsburg, CH
• Stephan Maas · Krefeld, DE
• Kristian Ruepp · Berlin, DE

Key dates

• Filing date: Nov 1, 2013
• Grant date: Sep 1, 2015
• Expiry date: Nov 1, 2033

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10T428/2982
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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-(aminosulfonyl)-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.