Crystal form of pyrimidine aniline compound, preparation method, and use

By developing the acid salt crystal form of pyrimidinaniline compounds, the problem of insufficient pharmacodynamic and pharmacokinetic performance of EGFR/HER2 mutant tumor treatment compounds in the prior art was solved, and the quality stability and bioavailability of the compounds were improved.

WO2025059801A1 Publication Date: 2025-03-27TYK MEDICINES INC +1
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Patent Information

Application Number
PCT/CN2023/119440
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Filing Date
2023-09-18
Publication Date
2025-03-27

AI Technical Summary

Technical Problem

In the prior art, compounds used to treat EGFR/HER2 mutant tumors have problems with insufficient pharmacodynamic and pharmacokinetic performance, resulting in unsatisfactory efficacy.

Method used

The acid salt crystal form of a pyrimidinaniline compound was developed, including citrate crystal form I, maleate crystal form I, oxalate crystal form I, etc. Through the combination of different acid reagents and solvent systems, crystal forms with excellent stability and high solubility were screened.

Benefits of technology

The quality stability and bioavailability of the compounds are improved, the side effects caused by drug instability are reduced, and the effectiveness of the treatment is improved.

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Abstract

The present invention relates to a polymorphic form of an acid salt of a pyrimidine aniline compound, a preparation method, and a use. Specifically, disclosed in the present invention are a polymorphic form of an acid salt of a compound of formula (A), a preparation method for the polymorphic form, and a use of the polymorphic form. Taking into account a thermodynamic stability relationship and a solid-state property evaluation result, the present invention provides a citrate crystal form I of formula (A) as a preferred crystal form, and the citrate crystal form I has stable physicochemical properties and can be better used clinically.
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