Fumarate salt of (R)-3-(1-(2,3-dichloro-4-(pyrazin-2-yl)phenyl)-2,2,2- trifluoroethyl)-1-methyl-1-(1-methylpiperidin-4-yl) urea, methods of preparation, and uses thereof

US11299472B2 · kind B2 · utility

Assignee

• Helsinn Healthcare SA · CH

Inventors

• Silvina Garcia Rubio · Princeton, US
• Mauro Perseghini · Biasca, CH
• Angelo Guainazzi · Iselin, US
• Claudio Pietra · Como, IT
• Claudio Giuliano · Como, IT

Key dates

• Filing date: Dec 7, 2018
• Grant date: Apr 12, 2022
• Expiry date: Dec 7, 2038

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07B2200/13
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Provided are various embodiments relating to fumarate salt of (R)-3-(1-(2,3-dichloro-4-(pyrazin-2-yl)phenyl)-2,2,2-trifluoroethyl)-1-methyl-1-(1-methylpiperidin-4-yl) urea, and methods of producing and using the same to treat conditions and disorders associated with an increase of ghrelin level, such as food abuse, alcohol addiction, and other disorders (e.g., Prader-Willi syndrome). Also provided are various embodiments relating to crystalline HM04 free base, different crystalline forms of HM04 fumarate salt, and methods of producing the same.