C-linked cyclic P2Y1 antagonists for thrombotic conditions
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Solution Overview
Problem
Current P2Y1 receptor antagonists lack the necessary pharmacological properties for in vivo studies and effective anti-thrombotic activity, highlighting the need for more potent and selective inhibitors to treat thrombotic or thromboembolic disorders.
Innovation Solution
Development of novel C-linked cyclic compounds and their analogues as selective inhibitors of the P2Y1 receptor, which can be used in pharmaceutical compositions to modulate platelet reactivity and treat thrombotic disorders.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current P2Y1 receptor antagonists are used, then platelet activation can be inhibited, but they lack the necessary pharmacological properties for in vivo studies and effective anti-thrombotic activity
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of P2Y1 receptor antagonists through C-linked cyclic compounds with specific substituents (R1-R6a groups, various ring structures). These structural parameter changes enhance both the pharmacological properties and anti-thrombotic activity, resolving the contradiction between reliability and adaptability of the compounds
2Reliability
If more potent and selective P2Y1 inhibitors are developed, then anti-thrombotic activity is improved, but the complexity of compound structure increases
Solution Approach 1:
The patent applies segmentation by dividing the P2Y1 antagonist molecule into distinct functional segments: a C-linked cyclic core structure with specific substituents (R1-R6a groups), aromatic rings (ring A, ring B), and heterocyclic moieties. This segmented approach allows for selective enhancement of anti-thrombotic activity through specific substituent modifications while maintaining the overall molecular framework
Solution Approach 2:
The patent applies local quality by introducing specific functional groups and substituents at particular positions on the molecular structure (e.g., R1-R6a groups at specific ring positions, carbonyl groups, hydroxyl groups). These localized structural modifications enhance receptor selectivity and anti-thrombotic potency without requiring complete redesign of the entire molecule, thus managing complexity
Data Source
AI summary
The present invention provides novel C-linked cyclic compounds and analogues of Formula (I):or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.