FXa inhibitor as well as preparation method and application thereof
By introducing pyrrole groups of different amine side chains onto the apixaban core, a novel pyrazolopyridine derivative FXa inhibitor was synthesized, solving the problems of complex synthesis, expensive raw materials, and insufficient safety in the existing technology, and achieving a highly efficient and safe FXa inhibition effect.
Patent Information
- Application Number
- CN202610911508.X
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2026-06-24
- Publication Date
- 2026-07-24
- Estimated Expiration
- 2046-06-24
AI Technical Summary
Existing FXa inhibitors have problems such as complicated synthesis steps, harsh reaction conditions, expensive raw materials and the use of sensitive reagents. They also pose risks of bleeding and individual tolerance differences, and the safety of long-term use needs to be improved.
A series of pyrazole-pyridine derivatives with different amine side chains introduced onto the benzene ring of the apixaban core were designed and synthesized. FXa inhibitors were prepared through steps such as amide condensation, cycloaddition, and Mannich reaction, avoiding the use of sensitive reagents such as trimethylaluminum and simplifying the synthetic route.
An FXa inhibitor with high anticoagulant activity, good pharmacokinetic properties and low bleeding risk was obtained. The synthetic route is simple, the raw materials are inexpensive, the overall yield is high, and a diverse compound library is provided.