Terpene Derivative PAR1 Inhibitor for Low Bleeding Risk Thrombosis Treatment
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Solution Overview
Problem
Current anti-platelet medications for preventing and treating thrombotic diseases often interfere with normal hemostasis, increasing the risk of bleeding, and have complex structures and high production costs, limiting their effectiveness and efficiency.
Innovation Solution
A novel terpene derivative-based PAR1 inhibitor is developed, using andrographolide as a starting material for structural modification, resulting in a compound with a clear target, low bleeding risk, and reduced preparation costs, which can be used to treat thrombotic diseases without affecting normal hemostasis.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional anti-platelet medications (TXA2 or ADP inhibitors) are used to inhibit platelet aggregation, then thrombotic diseases can be prevented and treated, but normal hemostasis is affected and bleeding risk increases
Solution Approach 1:
The patent extracts and targets only the pathological thrombin-mediated platelet activation pathway by specifically inhibiting PAR1 receptors, while leaving the normal hemostatic pathways (TXA2 and ADP) intact. This selective extraction of the pathological mechanism allows anti-thrombotic treatment without compromising normal hemostasis, thereby reducing bleeding risk while maintaining anti-thrombotic efficacy
2Object-affected harmful factors
If Vorapaxar is used as a PAR1 inhibitor to block platelet aggregation, then the risk of accidental bleeding is reduced, but the structure becomes complicated and preparation cost increases
Solution Approach 1:
The patent replaces the complex, expensive Vorapaxar molecule with simpler terpene derivative structures that are cheaper to produce. Although the new compounds have simpler structures, they maintain effective PAR1 inhibition and bleeding risk reduction, achieving the same therapeutic goal with more economical molecular designs
Solution Approach 2:
The patent changes the molecular parameters by using natural terpene derivatives with simpler structures compared to Vorapaxar. By modifying structural parameters (molecular weight, complexity, chiral centers) while maintaining biological activity, the patent achieves reduced preparation cost and simplified structure while preserving the bleeding risk reduction benefit
3Reliability
If Vorapaxar is used to inhibit PAR1, then anti-coagulation activity is improved, but the synthetic route becomes long and preparation cost increases
Solution Approach 1:
The patent utilizes naturally occurring terpene derivatives as starting materials that already possess the necessary structural features for PAR1 inhibition. By leveraging nature's own molecular designs, the patent eliminates the need for complex multi-step synthesis required for Vorapaxar, thereby reducing preparation cost while maintaining anti-coagulation activity
Data Source
AI summary
A novel terpene derivative-based PAR1 inhibitor, a preparation method thereof and a pharmaceutical composition including the same or a salt thereof, as well as a use of the PAR1 inhibitor and the salt thereof in preparation of medicaments for preventing and/or treating thrombotic diseases. The structural formula of the compound is as follows:The compound has the advantages of clear target, novel structure, low bleeding risk, high safety, outstanding active effect, low preparation cost and the like, and has a great application prospect in the preparation of the medicaments for treating the thrombotic diseases.