A crystalline form i of a benzodiazepine derivative and a process for its preparation

By optimizing the preparation method, a benzodiazepine derivative crystal form I with good solubility and stability was prepared, which solved the problem of poor solubility and stability in the existing technology and realized efficient and low-cost large-scale production.

CN122404337APending Publication Date: 2026-07-17CHENGDU EASTON BIOPHARMACEUTICALS CO LTD

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
CHENGDU EASTON BIOPHARMACEUTICALS CO LTD
Filing Date
2026-01-15
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

In the prior art, different crystal forms of 7-chloro-3-(5-dimethylaminomethyl-[1,2,4]oxadiazol-3-yl)-5-methyl-4,5-dihydro-imidazo[1,5-α][1,4]benzodiazepine-6-one exhibit differences in solubility and stability in the pharmaceutical field, lacking effective preparation methods and making it difficult to achieve large-scale production.

Method used

A crystalline form I of a benzodiazepine derivative and its preparation method are provided. By controlling the specific ratio of solvent and seed crystals and the dropping temperature, crystalline form I with good solubility, stability and bioavailability can be prepared. The method is simple, reproducible, uses little solvent and is easy to recover, and is suitable for large-scale production.

Benefits of technology

This study achieved high yield, stability, and bioavailability of benzodiazepine derivative crystal form I, reduced reagent costs, simplified the operation process, made it suitable for large-scale production, and improved the solubility and stability of the drug.

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Abstract

本发明涉及药物晶型领域,具体涉及一种苯二氮䓬衍生物的晶型I及其制备方法;所述苯二氮䓬衍生物的晶型I具有较好的溶解度、稳定性、流动性以及良好的生物利用度;所述晶型I的制备方法简单重复性好,收率高,易于操作,绿色环保,所需溶剂量小且有利于回收利用,能够有效降低试剂成本,容易实现规模化放大生产。
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