Crystalline form of compound and method of producing crystalline form of compound

JP2024028460A5Pending Publication Date: 2026-06-03VIKING THERAPEUTICS INC
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
VIKING THERAPEUTICS INC
Filing Date
2024-01-11
Publication Date
2026-06-03

AI Technical Summary

Technical Problem

There is a need for improved crystalline forms of thyroid hormone receptor β (TRβ) agonists to facilitate pharmaceutical development and enhance their stability and efficacy in treating conditions such as adrenoleukodystrophy (ALD) and lipid disorders.

Method used

The development of crystalline forms of TRβ agonists, including tert-butyl methyl ether (TBME) solvate, toluene solvate, ethanol solvate, tetrahydrofuran (THF) solvate, ethyl acetate (EtOAc) solvate, acetone solvate, and unsolvated crystalline Form C, which exhibit improved stability, processability, and low water adsorption, achieved through controlled crystallization methods.

Benefits of technology

These crystalline forms provide long-term stability, ease of manufacture, and effective treatment of ALD and lipid disorders like hypercholesterolemia and fatty liver disease, with unsolvated Form C demonstrating non-hygroscopic properties and high melting point, ensuring clinical efficacy.

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Abstract

To provide improved forms of phosphonate TRβ agonists to facilitate pharmaceutical development.SOLUTION: The present invention relates to methods of crystallizing the compound of Formula I, as well as the compound of Formula I, wherein crystalline forms of the compound of Formula I include the TBME solvate crystalline form, toluene solvate crystalline form, ethanol solvate crystalline form, THF solvate crystalline form, EtOAc solvate crystalline form, acetone solvate crystalline form and crystalline Form C.SELECTED DRAWING: None
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