Broad-Spectrum Anticoagulation Reversal Compound for Bleeding Control
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Solution Overview
Problem
There is a lack of broad-spectrum and high-effective anticoagulation reversal agents to rapidly and effectively reverse the effects of anticoagulant therapy, which can lead to life-threatening bleeding complications.
Innovation Solution
A compound with a specific structure represented by formula I, or its salt or deuterated form, is synthesized through a multi-step process involving xanthine and a halide reaction, followed by amino deprotection and deprotection treatments, and used in combination with pharmaceutically acceptable excipients to form an anticoagulation reversal composition.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If anticoagulant drugs are used to prevent and treat thrombotic diseases, then the incidence of thrombotic events is significantly reduced, but bleeding complications occur which can be life-threatening
Solution Approach 1:
The patent introduces a multifunctional reversal agent as an intermediary substance that can neutralize multiple types of anticoagulant drugs (direct thrombin inhibitors, factor Xa inhibitors, and indirect thrombin inhibitors) through specific molecular interactions. This mediator enables the body to counteract the harmful bleeding effects while preserving the therapeutic anticoagulation benefits
2Reliability
If multiple specific reversal agents are developed for different anticoagulant drugs, then the reversal effect for each specific drug is optimized, but the number of agents increases and broad-spectrum coverage is not achieved
Solution Approach 1:
The patent designs a universal reversal agent with multiple functional groups that can simultaneously interact with different anticoagulant mechanisms. The molecule contains basic amino acid residues (arginine, lysine, histidine) that can bind to various anticoagulant targets, enabling one agent to perform multiple reversal functions across different drug classes
3Ease of manufacture
If conventional reversal agents are used, then the development process is simple and quick, but the reversal efficiency and broad-spectrum coverage are insufficient
Solution Approach 1:
The patent employs composite peptide结构设计, combining multiple amino acid residues with specific functions into a single reversal agent molecule. The composite structure includes basic amino acids for binding anticoagulants, hydrophobic regions for structural stability, and specific spatial arrangements that enhance both reversal efficiency and broad-spectrum activity
Data Source
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AI summary
Provided in the present invention is an anticoagulation reversal agent having a structure as shown in formula I or a salt thereof or a deuterated compound thereof. Experimental results show that the compound provided in the present invention can better inhibit bleeding complications caused by an anticoagulant, for example, the compound can inhibit bleeding complications caused by warfarin, heparin and enoxaparin sodium, and has the characteristics of broad spectrum and high efficiency.