Salt of aminocyclobutane derivative, crystal form thereof, and preparation method and application thereof

By preparing and characterizing the acid salt crystal form of 3-amino-6'-chloro-2'-methyl-1',2'-dihydro-3'H-spiro[cyclobutane-1,4'-isoquinoline]-3'-one, the stability and solubility issues of the compound were resolved, thus enhancing its medicinal value.

CN122233985APending Publication Date: 2026-06-19SUZHOU NHWA PHARM RES CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SUZHOU NHWA PHARM RES CO LTD
Filing Date
2023-01-03
Publication Date
2026-06-19

AI Technical Summary

⚠Technical Problem

Existing 3-amino-6'-chloro-2'-methyl-1',2'-dihydro-3'H-spiro[cyclobutane-1,4'-isoquinoline]-3'-one compounds have shortcomings in terms of stability and solubility, which affects their pharmaceutical prospects.

⚗Method used

Crystal forms of different acid salts of the compound, including inorganic and organic acid salts, were provided and characterized by powder X-ray diffraction, DSC and TGA analysis to optimize their thermodynamic stability, solubility and hygroscopicity.

🎯Benefits of technology

This improved the stability and solubility of the compound, reduced its hygroscopicity, and enhanced its potential as a drug.

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Abstract

This invention relates to salts of aminocyclobutane derivatives, their crystal forms, preparation methods, and applications. Specifically, it provides the acid salt and crystal form of trans-3-amino-6'-chloro-2'-methyl-1',2'-dihydro-3'H-spiro[cyclobutane-1,4'-isoquinoline]-3'-one, its preparation method, pharmaceutical compositions containing the acid salt, and its application in the pharmaceutical field. The acid salt provided by this invention significantly improves the stability of the compound trans-3-amino-6'-chloro-2'-methyl-1',2'-dihydro-3'H-spiro[cyclobutane-1,4'-isoquinoline]-3'-one, overcoming the disadvantage of easy oxidation of free bases. In addition, the acid salt and its crystal form provided by this invention also have the advantages of improved solubility and low hygroscopicity, making them particularly suitable for the preparation of oral formulations.
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