Hydrobromide of benzodiazepine derivative, preparation method and use thereof

US10618904B2 · kind B2 · utility

Assignee

• CHENGDU BRILLIANT PHARMACEUTICAL CO., LTD. · CN

Inventors

• Haoxi Huang · Sichuan, CN
• Guoqing ZHUO · Sichuan, CN
• Guoning Shang · Sichuan, CN
• Zhen Liang · 流花街道, CN
• Ting L. Chu · Dallas, US
• Cuicui Chen · Sichuan, CN
• Ming Luo · Birmingham, US
• Yingfu Li · Schreiber, CA
• Zhonghai Su · Sichuan, CN

Key dates

• Filing date: Dec 13, 2016
• Grant date: Apr 14, 2020
• Expiry date: Dec 13, 2036

Classification

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

Abstract

The present invention provides a hydrobromide of methyl 3-[(4s)-8-bromo-1-methyl-6-(2-pyridyl)-4H-imidazol[1,2-a][1,4]benzodiazepine-4-yl] propionate and its related crystal forms, preparation method and use thereof. The hydrobromide has excellent solubility (>100 mg/ml), which is significantly superior to other currently commercially available or developed salt products, and is especially suitable for the preparation of injections, has relatively good stability in various crystal forms, and has good practical value and market prospects.