GSPT1 degradation compound and pharmaceuticals containing this compound.

VN128467APending Publication Date: 2026-09-03CYRUS THERAPEUTICS INC
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Patent Information

Application Number
VN1202507076
Authority / Receiving Office
VN · VN
Patent Type
Applications
Current Assignee / Owner
Priority Date
2023-04-13
Filing Date
2024-04-12
Publication Date
2026-09-03

AI Technical Summary

Technical Problem

Current compounds for degrading GSPT1, such as those disclosed in WO 2022/066835, exhibit transient degradation efficacy due to pH instability, leading to restored GSPT1 expression and tumor cell proliferation after 48 hours, limiting their anticancer effectiveness.

Method used

A novel compound represented by Formula I, with specific substituents on the phenylsulfonamide ring bound to the pomalidomide structure, enhances pH stability, selectivity, and sustained degradation activity against GSPT1, improving anticancer efficacy and safety.

Benefits of technology

The compound achieves sustained and selective GSPT1 degradation, exhibiting excellent anticancer activity against neuroendocrine phenotype cancers like small cell lung cancer and neuroendocrine prostate cancer with reduced cytotoxicity to normal cells, thus having a high therapeutic index.

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Abstract

The invention relates to a GSPT1-degrading compound. Specifically, the invention relates to a compound of formula I, its stereoisomer, hydrate, solvate, or pharmaceutical salt, and a pharmaceutical composition for the treatment of uncontrolled cell proliferation disorders containing this compound. The compound under the invention exhibits high selectivity and sustained degradation activity against GSPT1, excellent pH stability, and low cytotoxicity against normal cells, thus possessing excellent anticancer efficacy and a high therapeutic index. In addition, the compound under the invention may exhibit excellent anticancer activity against cancers with neuroendocrine phenotypes, such as small cell lung cancer, neuroendocrine lung cancer, and neuroendocrine prostate cancer.
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