N-[5-(Aminosulfony1)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate

US9340535B2 · kind B2 · utility

Assignee

• AiCuris GmbH & Co. KG · DE

Inventors

• Wilfried Schwab · Altentreptow, DE
• Alexander Birkmann · Wuppertal, DE
• Kurt Vogtli · Oberhofen, CH
• Dieter Haag · Ramlinsburg, CH
• Andreas Lender · Wuppertal, DE
• Alfons Grunenberg · Wuppertal, DE
• Birgit Keil · Düsseldorf, DE
• Joachim Rehse · Leichlingen, DE

Key dates

• Filing date: Sep 26, 2012
• Grant date: May 17, 2016
• Expiry date: Sep 26, 2032

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to an improved and shortened synthesis of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide and the mesylate monohydrate salt thereof by using boronic acid derivatives or borolane reagents while avoiding toxic organic tin compounds and to the mesylate monohydrate salt of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions.