Crystalline forms of 7-((2r,4s)-4-((2,3-dihydrobenzo[b][1,4] dioxin-6-YL-2,2,3,3-d 4)OXY)-2-methylpiperidin-1-YL)-8-methyl-4h-pyrimido[1,2-b]pyridazin -4-one

The crystalline hydrochloride Form X of Compound 129 addresses the selectivity and adverse effect issues of mAChR M4 compounds by providing improved stability and solubility, enhancing its potential as a therapeutic for neurological and psychiatric disorders.

WO2025122733A9PCT designated stage Publication Date: 2026-06-04NEUMORA THERAPEUTICS INC +1
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Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
NEUMORA THERAPEUTICS INC
Filing Date
2024-12-05
Publication Date
2026-06-04

AI Technical Summary

Technical Problem

Existing compounds targeting muscarinic acetylcholine receptor M4 (mAChR M4) for treating neurological and psychiatric disorders lack selectivity and induce adverse effects, limiting their clinical utility.

Method used

Development of crystalline hydrochloride salts of 7-((2R,4S)-4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl-2,2,3,3-d4)oxy)-2-methylpiperidin-1-yl)-8-methyl-4H-pyrimido[1,2-b]pyridazin-4-one (Compound 129) with a specific polymorph, Form X, exhibiting improved stability, solubility, and lipophilicity, suitable for selective mAChR M4 agonism.

Benefits of technology

The crystalline hydrochloride Form X of Compound 129 offers enhanced stability, solubility, and lipophilicity, making it a promising candidate for treating neurological and psychiatric disorders with reduced side effects.

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Abstract

Disclosed herein are solid forms of 7-((2R,4S)-4-((2,3-Dihydrobenzo[b][1,4]dioxin-6-yl-2,2,3,3-d4)oxy)-2-methylpiperidin-1-yl)-8-methyl-4H-pyrimido[1,2-b]pyridazin-4-one hydrochloride, including a crystalline Form X of exhibiting at least X-ray lines (in degrees 2θ ± 0.2°) at 6.69, 8.52, 10.29, 17.42, 20.64, 21.08, 26.22 and 29.52 in a powder diffraction pattern when measured using Cu Kα radiation. Also disclosed herein are pharmaceutical compositions containing the same, and to methods of their use and preparation.
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