Crystaline forms of N-[6-(cis-2,6-dimethylmorpholine-4-yl)pyridine-3-yl]-2-Methyl-4′-(trifluoromethoxy) [1,1′-biphenyl]-3-Methanamide monophosphate, and process of preparation thereof

US10266523B2 · kind B2 · utility

Assignee

• CRYSTAL PHARMATECH CO., LTD. · CN

Inventors

• Minhua Chen · 安丰镇, CN
• Yanfeng Zhang · Suzhou, CN
• Fei Lu · 安丰镇, CN
• Xiaoyu Zhang · Suzhou, CN

Key dates

• Filing date: Mar 30, 2016
• Grant date: Apr 23, 2019
• Expiry date: Mar 30, 2036

Classification

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

Abstract

The present disclosure relates to novel crystalline forms of N-[6-(cis-2,6-dimethylmorpholine-4-yl)pyridine-3-yl]-2-methyl-4′-(trifluoromethoxy) [1,1′-biphenyl]-3-carboxamide monophosphate, and process of preparation thereof. The crystalline form of the monophosphate of a compound of formula (I) has low hygroscopicity, is convenient to store, has better stability than that of diphosphonate in prior art, can avoid the risk of crystal transformation in the development and production of the drug. The preparation method is simple, has low cost, and has important value for further optimization and development of the drug.