Substituted oxoisoindolylpiperidin-2,6-dione compounds

By targeting and degrading the cell cycle protein E1 in cancer cells with the oxoisodihydroindolylpiperidine-2,6-dione compound, the problems of low therapeutic index and drug resistance in existing technologies are solved, and the effect of selectively reducing the protein level in cancer cells is achieved.

CN122422306APending Publication Date: 2026-07-17BRISTOL MYERS SQUIBB CO
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Patent Information

Application Number
CN202480071776.4
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2023-09-13
Filing Date
2024-09-12
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing technologies struggle to effectively target and reduce cyclin E1 protein levels in cancer while simultaneously minimizing GSPT1 degradation in normal tissues, leading to low therapeutic index and drug resistance issues.

Method used

A substituted oxoisodihydroindolylpiperidine-2,6-dione compound is provided that selectively reduces cyclin E1 protein levels in cancer cells by promoting its degradation through interaction with the E3 ubiquitin ligase complex of cyclin E1 protein.

Benefits of technology

It achieves selective reduction of cyclin E1 protein, reduces GSPT1 degradation, improves the therapeutic index, overcomes drug resistance, and enhances clinical response in cancer treatment.

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Abstract

本文公开了式(I)的化合物：(I)或其立体异构体、互变异构体或盐，其中：R是；并且环A、L、R1、R2、R3、m和n如本文所定义。还公开了使用此类化合物来降低细胞周期蛋白E1水平的方法；以及包含此类化合物的药物组合物。这些化合物可用于治疗增殖性疾病，例如癌症。(I) R是
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Citation Information

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