Crystalline forms of glucosylceramide synthase inhibitors and their uses

The development of stable crystalline forms of Compound 1, characterized by distinct XRPD patterns, addresses the need for improved stability and bioavailability, enabling effective pharmaceutical compositions for treating GCS-related diseases.

JP2025527600APending Publication Date: 2025-08-22ACELINK THERAPEUTICS INC
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Patent Information

Application Number
JP2025510295
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2022-08-18
Filing Date
2023-08-10
Publication Date
2025-08-22

AI Technical Summary

Technical Problem

There is a need for stable crystalline forms of the GCS inhibitor (E)-N-((1R,2R)-1-(3-chloro-4-cyclopropoxyphenyl)-1-hydroxy-3-(pyrrolidin-1-yl)propan-2-yl)-2-(6-chloronaphthalen-2-yl)-2-(hydroxyimino)acetamide (Compound 1) with advantageous chemical and physical properties to ensure quality, safety, and efficacy in pharmaceutical applications.

Method used

The development of various crystalline forms, anhydrates, hydrates, solvates, and salts of Compound 1, characterized by specific X-ray powder diffraction patterns, including forms A, B, C, D, and their respective salts, such as L-malate and L-tartrate, to enhance stability and bioavailability.

Benefits of technology

The crystalline forms provide improved stability, reproducibility, and favorable physicochemical properties, facilitating the development of effective pharmaceutical compositions for treating GCS-related diseases.

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Abstract

The present disclosure relates to crystalline forms of (E)-N-((1R,2R)-1-(3-chloro-4-cyclopropoxyphenyl)-1-hydroxy-3-(pyrrolidin-1-yl)propan-2-yl)-2-(6-chloronaphthalen-2-yl)-2-(hydroxyimino)acetamide, methods for preparing same, pharmaceutical compositions containing same, and uses thereof.
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