Benzimidazo 2-amino-1, 3, 4-thiadiazole derivative as well as preparation method and pharmaceutical application thereof

By synthesizing benzimidazol-2-amino-1,3,4-thiadiazole derivatives and targeting the STAT3 SH2 domain, the problem of the lack of efficient STAT3 inhibitors in the existing technology was solved, and effective inhibition of STAT3-overexpressing tumor cells and cancer treatment were achieved.

CN120647642APending Publication Date: 2025-09-16INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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Patent Information

Application Number
CN202410261026.5
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-03-07
Publication Date
2025-09-16

AI Technical Summary

Technical Problem

The existing technology lacks STAT3-targeted anti-tumor compounds that are highly effective, low-toxic, have suitable physicochemical properties, and are highly specific for inhibiting tumor cells with high STAT3 expression.

Method used

Benzimidazolo-2-amino-1,3,4-thiadiazole derivatives were designed and synthesized. By splicing the anti-tumor skeleton and the active fragment 2-amino-1,3,4-thiadiazole, new compounds were formed to target the STAT3 SH2 domain, interfering with STAT3 protein dimerization and the formation of dimer-DNA complexes.

Benefits of technology

It achieves effective inhibition of STAT3-overexpressing tumor cells, has high efficiency, low toxicity and specificity, and is suitable for the prevention and treatment of cancer.

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Abstract

The invention belongs to the technical field of medicines, and relates to a benzimidazo 2-amino-1, 3, 4-thiadiazole compound and a pharmaceutical application thereof, in particular to a benzimidazo 2-amino-1, 3, 4-thiadiazole derivative shown as a formula I, a pharmaceutical salt thereof, a preparation method of the benzimidazo 2-amino-1, 3, 4-thiadiazole derivative, a composition containing one or more of the compounds, and a pharmaceutical application of the benzimidazo 2-amino-1, 3, 4-thiadiazole compound. The invention also discloses application of the compound as an STAT3 signal channel inhibitor in the aspect of treating tumor diseases. # imgabs0 #
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