A quinazoline compound, precursors, derivatives and uses thereof

By designing quinazoline compounds and their derivatives, and introducing rigid cyclic structures and specific chiral bicyclic structures, the chemical stability and in vivo metabolic stability of existing PET probes have been solved. This has resulted in high affinity for TSPO and improved imaging performance, providing reliable molecular imaging data for the precise diagnosis and treatment of gliomas and neuroinflammatory diseases.

CN122036692BActive Publication Date: 2026-07-24MAJOR BRAIN DISEASES RES CENT OF CAPITAL MEDICAL UNIV (BEIJING INST OF MAJOR BRAIN DISEASES)
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Patent Information

Application Number
CN202610500619.1
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2026-04-16
Publication Date
2026-07-24
Estimated Expiration
2046-04-16

AI Technical Summary

Technical Problem

Existing PET probes have shortcomings in terms of chemical stability and in vivo metabolic stability, which affect the accurate diagnosis of gliomas and image clarity. Furthermore, existing probe precursors are prone to deliquescence, have low labeling yields, and the radiochemical purity of the products is easily affected by degradation products.

Method used

A quinazoline compound and its derivatives were designed, introducing rigid cyclic structures and specific chiral bicyclic structures. By using the bioisosteric principle to constrain conformation, chemical stability and in vivo metabolic stability were improved, while maintaining a high affinity for TSPO.

Benefits of technology

This study improved the imaging performance of quinazoline compounds in glioma models, providing more reliable molecular imaging data and offering a new tool for the precision diagnosis and treatment of gliomas and neuroinflammatory diseases, demonstrating good potential for clinical translation.

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Abstract

The present application relates to the technical field of pharmaceutical chemistry, and particularly relates to a quinazoline compound and precursors, derivatives and applications thereof. The quinazoline compound provided by the present application has excellent precursor chemical stability and in-vivo metabolic stability, and has an ideal imaging performance in a brain glioma model, thereby providing more reliable molecular imaging data for precise diagnosis of brain glioma and other cancers and diagnosis and treatment of neuroinflammation-related diseases, and having a good clinical transformation potential.
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