Salts of compounds and their crystalline forms, methods of preparation and uses

Triphenylacetate salts and crystalline forms of rifamycins address solubility and stability issues, enhancing their pharmaceutical potential by providing improved stability and solubility profiles.

JP2026507085APending Publication Date: 2026-02-27テンノア セラピューティクス(スーチョウ)リミテッド
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Patent Information

Application Number
JP2025549721
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2023-02-24
Filing Date
2024-02-23
Publication Date
2026-02-27

AI Technical Summary

Technical Problem

Rifamycins and their derivatives face challenges with high relative molecular mass, high lipophilicity, low water solubility, hygroscopicity, and low bioavailability, leading to difficulties in meeting pharmaceutical requirements for drug discoverability and stability, particularly in crystalline forms.

Method used

Development of triphenylacetate salts and their stable crystalline forms, characterized by specific X-ray powder diffraction peaks and differential scanning calorimetry profiles, which enhance stability and solubility, as well as methods for their preparation and use.

Benefits of technology

The triphenylacetate salts and crystalline forms exhibit improved stability and solubility, addressing the limitations of rifamycins and enabling their pharmaceutical application.

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Abstract

The present application provides a salt of a compound, or a hydrate, solvate, prodrug, metabolite, or deuterated salt thereof, wherein the salt is a triphenylacetate salt of a compound of Formula (I), wherein L is a bond, an alkyl group, or an alkoxy group substituted at any central carbon atom with an aryl group, and G is hydrogen, an alkyl group, a haloalkyl group, an alkenyl group, an alkynyl group, an optionally substituted cycloalkyl group, or an optionally substituted heterocyclyl group. The present application also provides several crystalline forms of the salt, as well as methods for making and using the same. JPEG2026507085000048.jpg6668
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