Nucleotide compounds, methods of making and using the same, radionuclide targeting probes, methods of making and using the same, pharmaceutical compositions

By developing CD73-targeting nucleotide compounds and radionuclide-targeting probes, and combining them with nuclear medicine imaging technology, the challenge of detecting CD73 expression in tumors has been solved, achieving highly efficient tumor diagnosis and treatment, and improving the response rate of tumor immunotherapy.

CN117924394BActive Publication Date: 2026-07-24XIAMEN UNIV
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Patent Information

Application Number
CN202311133397.7
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-09-05
Publication Date
2026-07-24
Estimated Expiration
2043-09-05

AI Technical Summary

Technical Problem

The lack of high-resolution and high-sensitivity molecular imaging techniques for detecting CD73 expression in tumors, coupled with the limited application of combined therapy of CD73 inhibitors and immunomodulators, has resulted in low response rates for tumor immunotherapy.

Method used

Develop nucleotide compounds and their pharmaceutically acceptable salts with CD73 targeting properties, as well as radionuclide targeting probes and their pharmaceutically acceptable salts. Visualize and quantitatively analyze the dynamic expression of CD73 in the tumor microenvironment using nuclear medicine imaging techniques, and combine them with immune checkpoint inhibitors for combination therapy.

Benefits of technology

This improved the specificity and sensitivity of CD73-targeting probes, enhanced the detection capability of CD73 protein in the tumor microenvironment, promoted tumor diagnosis and treatment, overcame the shortcomings of traditional detection methods, and enhanced the efficacy of tumor immunotherapy.

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Abstract

The application belongs to the technical field of biological medicine, and particularly relates to a nucleotide compound and a preparation method and application thereof, a nuclide targeting probe and a preparation method and application thereof, and a pharmaceutical composition. The nucleotide compound and the nuclide labeled complex provided by the application have excellent in-vivo biological performance, have high specific uptake in a lesion with high expression of CD73 protein, have a high target / non-target ratio, and have low non-specific background. The characteristics can reduce unnecessary radioactive damage to normal tissues and organs, and are very suitable for use in diagnosis and treatment of tumors. In addition, the nuclide targeting probe can also be combined with other immune checkpoint inhibitors (such as PD-1 / PD-L1 monoclonal antibodies) for combined treatment. The nuclide targeting probe can be used for visualizing and quantitatively analyzing the dynamic expression of CD73 in a tumor microenvironment through a nuclear medicine imaging method, and overcomes the defects of sampling errors and poor accuracy in traditional detection methods.
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