Gamma-aminobutyric acid derivative containing bicyclic bridge ring structure as well as preparation method and application thereof
By developing a bicyclic bridged-ring γ-aminobutyric acid derivative as a BCAT1 inhibitor, the problem of EGFR inhibitor resistance in non-small cell lung cancer has been solved, achieving effective treatment of tumors with high BCAT1 expression, especially EGFR-resistant lung cancer.
Patent Information
- Application Number
- CN202410596075.4
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2024-05-14
- Publication Date
- 2025-11-14
AI Technical Summary
Existing EGFR inhibitors have problems with drug resistance in the treatment of non-small cell lung cancer, and branched-chain amino acid transaminase BCAT1 plays an important role in the invasive growth of tumors, drug resistance and poor prognosis, and there is a lack of effective inhibitors.
A class of γ-aminobutyric acid derivatives containing a bicyclic bridged ring structure were developed as BCAT1 inhibitors. These derivatives were prepared by generating pharmaceutically acceptable salts and compositions for use in the preparation of tumor drugs that treat BCAT1-overexpressing tumors.
This compound significantly inhibits BCAT1 enzyme activity, effectively suppresses the growth of EGFR-resistant tumor cells, has excellent pharmacokinetic properties, is suitable for oral administration, and is applicable to the treatment of cancers with high BCAT1 expression, such as lung cancer, gastric cancer, and prostate cancer.