Inhibitors of idiopathic pulmonary fibrosis, their preparation methods, and applications
By designing compounds targeting the BET protein BD1, the problems of toxicity and side effects of existing BET inhibitors in the treatment of IPF have been solved. A highly selective and low-toxicity BET inhibitor has been developed to effectively inhibit BRD4-BD1, which has significant potential for the treatment of pulmonary fibrosis.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- SICHUAN UNIV
- Filing Date
- 2024-01-15
- Publication Date
- 2026-07-17
AI Technical Summary
Existing BET inhibitors such as JQ1 or CG223 have dose-limiting toxicities and serious side effects when treating idiopathic pulmonary fibrosis (IPF), and there is a need to develop highly selective, low-toxicity BET inhibitors to target BRD4-BD1.
A compound or its pharmaceutically acceptable salt was designed and synthesized that targets the bromine domain BD1 of the BET protein, significantly enhancing the inhibitory activity against BRD4-BD1 and reducing the inhibitory activity against BRD4-BD2, achieving this goal through specific chemical structures such as compounds of formula I and formula II.
The compound exhibits significantly higher inhibitory activity against BRD4-BD1 than against BRD4-BD2, effectively inhibiting the transcription of pulmonary fibrosis-related genes, reducing side effects, and providing an effective treatment for IPF.
Smart Images
Figure CN117902998B_ABST