New rhoj / cdc42 inhibitors for the treatment of cancer, benign tumors, retinal disorders, vascular disorders and cardiomyopathy

By developing novel 2,4,6-trisubstituted pyrimidine compounds targeting RhoJ/CDC42, the limitations of existing therapies in treating melanoma and vascular diseases have been addressed, achieving both melanoma inhibition and effective treatment of various vascular conditions.

CN122374300APending Publication Date: 2026-07-10FOND INST ITAL DI TECH +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
FOND INST ITAL DI TECH
Filing Date
2024-08-01
Publication Date
2026-07-10

AI Technical Summary

Technical Problem

Existing therapies such as dacarbazine, IL-2, BRAF inhibitors, and immunotherapy have limited efficacy and significant toxicity in melanoma patients. Treatment options for benign tumors and hereditary vascular diseases are limited. There is insufficient data on the inhibitory activity of existing RhoJ/CDC42 inhibitors in cell lines A375, WM3248, SKMEL3, SKMEL28, or SW480.

Method used

Novel 2,4,6-trisubstituted pyrimidine compounds were developed, characterized by piperidine nitrogen with different heterocyclic or aromatic ring substitutions, which inhibit tumor growth by targeting RhoJ/CDC42, blocking tumor cell signal transduction and vascular system supply.

Benefits of technology

These compounds exhibit high specificity, slowing melanoma growth, reducing the impact on normal tissues, and effectively treating cardiomyopathy, retinal diseases, and various vascular conditions, including aneurysms and varicose veins.

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Abstract

Disclosed are novel compounds having Rho / Cdc42 inhibitory activity, excellent selectivity, and robust anti-proliferative activity.
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Citation Information

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