KRAS inhibitors

JP2024510207A5Active Publication Date: 2025-03-25BRISTOL MYERS SQUIBB CO
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Patent Information

Application Number
JP2023555534
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2021-12-13
Filing Date
2022-03-14
Publication Date
2025-03-25
Estimated Expiration
2042-03-14

AI Technical Summary

Technical Problem

Current attempts to develop inhibitors for the KRAS G12D mutation, a common mutation in tumors and cancers, have been hindered by the difficulty in binding to the KRAS protein due to competition with GTP in the intracellular binding pocket, particularly because the allosteric site is unknown.

Method used

The development of compounds represented by Formula (I) and (II), which include specific structural components such as aryl or heteroaryl groups, along with various substituents, to effectively inhibit KRAS G12D activity by targeting the KRAS protein.

Benefits of technology

These compounds demonstrate the ability to inhibit KRAS G12D activity, providing a potential therapeutic approach for treating cancers expressing this mutation, including pancreatic ductal adenocarcinoma, colorectal cancer, and non-small cell lung cancer.

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Abstract

The present disclosure relates to KRAS inhibitors, and also provides methods of treating cancer using such compounds.
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