Crystalline forms of (4S)-24-chloro-4-ethyl-73-fluoro-35-methoxy-32,5-dioxo-14-(trifluoro-methyl)-32h-6-aza-3(4,1)-pyridina-1(1)-[1,2,3]triazola-2(1,2),7(1)-dibenzenaheptaphane-74-carboxamide, uses and preparation process thereof

TWI940428BActive Publication Date: 2026-09-21BAYER AG
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Patent Information

Application Number
TW114150159
Authority / Receiving Office
TW · TW
Patent Type
Patents
Current Assignee / Owner
Priority Date
2021-03-09
Filing Date
2022-03-07
Publication Date
2026-09-21
Estimated Expiration
2042-03-06

AI Technical Summary

Technical Problem

Existing methods fail to produce crystalline, solvent-free forms of the compound (4S)-24-chloro-4-ethyl-73-fluoro-35-methoxy-32,5-dioxy-14-(trifluoromethyl)-32-hydro-6-aza-3(4,1)-pyridine-1(1)-[1,2,3]triazole-2(1,2),7(1)-diphenylheptane-74-carboxamide, which are essential for effective oral administration in treating thrombotic and thromboembolic conditions.

Method used

The amorphous form of the compound is crystallized into crystalline variant I by seeding with crystalline variant A, using solvents like acetonitrile or ethanol, resulting in forms with superior hygroscopicity and thermal stability.

Benefits of technology

The crystalline variant I exhibits enhanced stability and solubility, making it suitable for pharmaceutical compositions and effective in treating cardiovascular and cerebrovascular conditions.

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Abstract

This invention relates to the crystalline forms of (4S)-24-chloro-4-ethyl-73-fluoro-35-methoxy-32,5-dioxy-14-(trifluoromethyl)-32-hydro-6-aza-3(4,1)-pyridine-1(1)-[1,2,3]triazole-2(1,2),7(1)-diphenylheptane-74-carboxamide, including crystalline variants I and II, methods for their preparation, pharmaceutical compositions comprising them, and their use in disease control.
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Citation Information

Patent Citations

  • Preparative process

    TW202002969A