Solid dispersion of myeloid quinorm inhibitors and pharmaceutical compositions containing the same

A solid dispersion of 5-chloro-N-(3-cyclopropyl-5-{[(3R,5S)-dimethylpiperazine-1-yl]methyl}phenyl)-4-(6-methyl-1H-indole-3-yl)pyrimidine-2-amine with a hydrophilic polymer carrier addresses delivery challenges, significantly improving pharmacokinetic properties and therapeutic efficacy for treating acute myeloid leukemia.

JP2026519563APending Publication Date: 2026-06-16HANMI PHARM CO LTD

Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
HANMI PHARM CO LTD
Filing Date
2024-05-31
Publication Date
2026-06-16

AI Technical Summary

Technical Problem

Current formulations of 5-chloro-N-(3-cyclopropyl-5-{[(3R,5S)-dimethylpiperazine-1-yl]methyl}phenyl)-4-(6-methyl-1H-indole-3-yl)pyrimidine-2-amine, a potent inhibitor of myeloid kinases, face challenges in achieving effective and safe delivery for treating conditions like acute myeloid leukemia due to limitations in pharmacokinetic properties.

Method used

A solid dispersion of the compound is formulated with a hydrophilic polymer carrier, such as hydroxypropyl methylcellulose acetate succinate, using methods like spray drying, to enhance its pharmacokinetic properties, resulting in improved drug exposure and bioavailability.

Benefits of technology

The solid dispersion significantly increases maximum plasma concentration (Cmax) and area under the curve (AUC) by 2 to 3 times, enhancing the therapeutic efficacy of the compound in treating conditions like acute myeloid leukemia.

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Abstract

Provision of solid dispersions and preparation of the solid dispersions. [Solution] A solid dispersion of 5-chloro-N-(3-cyclopropyl-5-{[(3R,5S)-dimethylpiperazine-1-yl]methyl}phenyl)-4-(6-methyl-1H-indole-3-yl)pyrimidine-2-amine and a process for preparing the solid dispersion are provided.
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