Toolerutinib amorphous form as well as preparation method and application thereof

By preparing tolebrutinib in Form 1, Form 2, and amorphous forms, the stability and solubility issues of tolebrutinib in drug development were resolved, enabling its effective application in pharmaceuticals, particularly for the treatment of cancer, autoimmune diseases, and thromboembolic diseases.

CN122059957APending Publication Date: 2026-05-19SOLIPHARMA
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Patent Information

Application Number
CN202610300829.6
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2021-04-30
Filing Date
2022-04-22
Publication Date
2026-05-19

AI Technical Summary

Technical Problem

The crystal form of tolebrutinib is not disclosed in the existing technology, which leads to problems such as poor stability, high hygroscopicity, and insufficient solubility in drug development, thus limiting its medicinal value.

Method used

Methods for preparing Form 1 and Form 2 of tolebrutinib are provided, as well as an amorphous form of tolebrutinib with good stability and solubility, prepared by crystal and amorphous processes under specific solvents and conditions to ensure its stability and solubility during pharmaceutical use.

Benefits of technology

Tolebrutinib Form 1 and Form 2 exhibit good stability and solubility, making them suitable for the industrial production and storage of pharmaceutical formulations. This improves the bioavailability of the drug and the stability of the formulation, making them suitable for the treatment of cancer, autoimmune diseases, and thromboembolic diseases.

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Abstract

The invention provides a toleburtinib crystal form and amorphous form and a preparation method and application thereof. The toleburtinib crystal form at least has the following advantages that stability is good, hygroscopicity is low, particle size distribution is uniform, solubility meets the medicinal requirement, stable storage can be achieved, crystal transformation of medicine in the development process and storage process is avoided, the preparation method is reliable, and the toleburtinib crystal form is suitable for industrial production. The method has great development value. The toleburtinib amorphous form provided by the invention still has good placement stability and acceptable hygroscopicity while having better solubility than that of the toleburtinib in a crystalline state, and has a very high medicinal value.
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