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

USRE49697E1 · kind E1 · reissue

Assignee

• AICURIS ANTI-INFECTIVE CURES AG · 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 25, 2020
• Grant date: Oct 17, 2023
• Expiry date: Nov 25, 2040

Classification

• Technology area (CPC —): General

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.