Crystal form of bisulfate of JAK inhibitor and preparation method therefor

US10150770B2 · kind B2 · utility

Assignee

• JIANGSU HENGRUI MEDICINE CO., LTD. · CN

Inventors

• Piaoyang Sun · Lianyungang, CN
• Guaili Wu · 安丰镇, CN
• Xiaohui Gao · 安丰镇, CN
• Yongjiang Chen · 安丰镇, CN
• Lingjia Shen · 安丰镇, CN

Key dates

• Filing date: Sep 9, 2015
• Grant date: Dec 11, 2018
• Expiry date: Oct 15, 2035

Classification

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

Abstract

A crystal form I of a Janus Kinase (JAK) inhibitor (3aR,5s,6aS)—N-(3-methoxyl-1,2,4-thiadiazole-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidine-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-formamide bisulfate of formula (I) is provided. Also provided is a method of preparing the crystal form I of the JAK inhibitor of formula (I). The preparation method includes crystallizing any crystal form or amorphous compound solid of formula (I) in a single organic solvent to obtain the form I crystal. The crystal form I has excellent crystal stability and chemical stability. Additionally, the crystal solvent used to produce the crystal form I has low toxicity and a relatively low content of residual solvent, making the compound better suited for clinical treatment.