Polymorph of (s)-2-(((4'-trifluoromethylbiphenyl-4-yl)methyl)amino)propanamide methanesulfonate, and pharmaceutical composition comprising same
Novel crystalline and amorphous forms of (S)-2-(((4'-trifluoromethylbiphenyl-4-yl)methyl)amino)propanamide methanesulfonate address the transition rate challenge, offering enhanced solubility, hygroscopicity, and photostability for pharmaceutical applications.
Patent Information
- Application Number
- PCT/KR2025/020042
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2025-11-24
- Filing Date
- 2025-11-28
- Publication Date
- 2026-06-11
AI Technical Summary
Existing technologies face challenges in controlling the transition rate of metastable crystal polymorphs to stable polymorphs for (S)-2-(((4'-trifluoromethylbiphenyl-4-yl)methyl)amino)propanamide methanesulfonate, an alpha-aminoamide derivative, which is crucial for pharmaceutical applications, as they exhibit higher solubility and dissolution rates, requiring advanced crystal engineering studies.
The development of two novel crystalline forms and one amorphous form of (S)-2-(((4'-trifluoromethylbiphenyl-4-yl)methyl)amino)propanamide methanesulfonate, characterized by specific PXRD, TGA, and DSC patterns, which provide enhanced thermal stability, solubility, and photostability, overcoming the limitations of conventional crystallization methods.
The novel crystalline forms exhibit improved solubility, hygroscopicity, and photostability, ensuring stable pharmaceutical compositions for treating neurological diseases and obesity, with crystalline form 1 demonstrating superior photostability and form 2 showing reversible stability against humidity changes.