A new crystal form of a PI3K / AKT signaling pathway inhibitor and a preparation method thereof

CN122255137APending Publication Date: 2026-06-23成都硕德药业有限公司
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Patent Information

Application Number
CN202511927806.X
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2024-12-21
Filing Date
2025-12-19
Publication Date
2026-06-23

AI Technical Summary

Technical Problem

In the existing technology, the crystal forms A and C of the compound of formula I are semi-crystalline, which have the risks of unqualified purity and crystal transformation. Although crystal form B is crystalline, its stability and bioavailability are insufficient and cannot meet the requirements of drug formulation development. It is necessary to develop one or more crystal forms that are simple to prepare, have high purity, good stability and good solubility.

Method used

Three new crystal forms, I, II, and III, are provided. After ultrasonic dissolution and rotary drying in different solvents, followed by suspension at high temperature or room temperature and filtration drying, crystal forms with excellent stability and solubility are obtained. The specific steps include dissolving in tetrahydrofuran and then adding solvents such as dimethyl carbonate, methyl tert-butyl ether, and isopropyl acetate for suspension and filtration.

Benefits of technology

The prepared crystal form II maintains good physicochemical stability and low hygroscopicity, while exhibiting high crystallinity and improved bioavailability, making it suitable for pharmaceutical development. Furthermore, the preparation steps are simple and the conditions are mild, making it suitable for industrial production.

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Abstract

The application relates to the field of drug crystal forms, in particular to a new crystal form of a compound of formula I and a preparation method thereof. The crystal form II of the compound of formula I has the comprehensive advantages of good physical and chemical stability, low moisture absorption, good solubility and bioavailability, and thus has certain drug property and drug development value. In addition, the preparation method of the crystal form II of the compound of formula I is simple in steps, mild in conditions, good in process repeatability, high in purity and low in cost, and is suitable for industrial large-scale production.
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Citation Information

Patent Citations

  • Crystalline forms of (s) -4-amino-n- (1- (4 - chlorophenyl) - 3 - hydroxypropyl) -1- (7h - pyrrolo [2, 3-d] pyrimidi n-4-yl) piperidine-4-carboxamide

    CN104203953A