Radioactive triazolidinedionyl derivatives, their preparation methods and applications

By synthesizing triazolidinedimethyl derivatives, the problem of slow pharmacokinetics in existing adenosine A2A receptor imaging agents has been solved, enabling rapid imaging for the diagnosis of A2A receptor-related diseases and tumors, thus improving diagnostic efficiency and clinical application value.

CN117946123BActive Publication Date: 2026-06-30BEIJING INST FOR BRAIN DISORDERS
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Patent Information

Application Number
CN202410115590.6
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2024-01-26
Publication Date
2026-06-30
Estimated Expiration
2044-01-26

AI Technical Summary

Technical Problem

Existing adenosine A2A receptor imaging agents suffer from slow pharmacokinetics, pharmacokinetic instability, and limited clinical applications, making it difficult to meet the needs for rapid diagnosis and assessment of A2A receptor-related diseases and tumors.

Method used

A class of triazolopyrimidine derivatives were designed and synthesized. Through skeletal transition, a PET probe targeting the A2A receptor with fast pharmacokinetics was prepared, which can be used for tumor diagnosis. The compound was prepared using a radiolabeling method.

Benefits of technology

It enables compounds to quickly reach equilibrium in the brain, allowing for rapid quantification and qualitative analysis of A2A receptors. This is applicable to the diagnosis of A2A receptor-related brain diseases and the diagnosis and treatment evaluation of tumors, reducing patient waiting time and improving diagnostic efficiency.

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Abstract

This invention discloses a radioactive triazolidinedimethylpyrimidine derivative, its preparation method, and its applications. The derivative has the structure shown in Formula I. Compared with the prior art, this invention provides a class of high-affinity adenosine A derivatives. 2A Radioactive triazolidinedimethyl derivatives of the receptor. This class of compounds belongs to the diagnostic category A. 2A Novel compounds for receptor-related diseases, and derivatives thereof prepared to target A 2A Imaging of the receptor, compared with previously reported targeting of A 2A Compared to receptor-specific radiopharmaceuticals, the radioactive compounds of this invention can rapidly reach equilibrium in the brain, thereby facilitating A. 2A Rapid quantification and qualitative analysis of receptors. The compounds of this invention can be applied not only to A... 2A The diagnosis of receptor-related brain diseases can also be applied to A 2A Diagnosis and efficacy evaluation of tumors with high receptor expression.
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Citation Information

Patent Citations

  • Adenosine A2A receptor antagonists

    CN1451007A