Crystalline forms of compound or salts and solvates thereof having USP1 inhibitory activity

The development of crystalline forms of USP1 inhibitors addresses the need for improved bioavailability and physical properties, enhancing stability and solubility for effective drug production.

WO2026139039A1PCT designated stage Publication Date: 2026-07-02LAEKNA PHARMACEUTICAL NINGBO CO LTD
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Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
LAEKNA PHARMACEUTICAL NINGBO CO LTD
Filing Date
2025-12-26
Publication Date
2026-07-02

AI Technical Summary

Technical Problem

There is a need for polymorph forms of USP1 inhibitors that have improved bioavailability and physical properties.

Method used

Development of crystalline forms of 1-(4-(2-(4-((4'-cyclopropyl-5,6'-dimethoxy-[2,5'-bipyrimidin]-4-yl)amino)methyl)phenyl)-6-(trifluoromethyl)pyridin-3-yl)piperidin-1-yl)ethan-1-one and its salts and solvates, which exhibit good stability, solubility, and low hygroscopicity, enhancing pharmacodynamic activity and pharmacokinetic behavior.

Benefits of technology

The crystalline forms demonstrate improved stability and solubility, contributing to better drug production and application in the pharmaceutical industry.

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    Figure PCTCN2025146027-FTAPPB-I100003
Patent Text Reader

Abstract

Provided herein are crystalline form of 1- (4- (2- (4- ( ( (4'-cyclopropyl-5, 6'-dimethoxy- [2, 5'-bipyrimidin] -4-yl) amino) methyl) phenyl) -6- (trifluoromethyl) pyridin-3-yl) piperidin-1-yl) ethan-1-one (Compound I) or salts or solvate thereof. Also provided herein are process for preparing the crystalline form. Also provided herein are pharmaceutical compositions comprising the crystalline form, and method of use of the crystalline form and pharmaceutical compositions in the treatment of diseases or conditions.
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