Urea Hydantoin Derivatives as Selective FPR2 Modulators
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Solution Overview
Problem
Current pharmaceutical agents targeting the formyl peptide receptor 2 (FPR2) face limitations due to the inherent physicochemical properties of natural ligands like lipoxin A4, leading to side effects and inefficiencies in treating inflammatory disorders, particularly in ocular and dermal conditions, where selective modulation of FPR2 is desired for anti-inflammatory and pro-resolutionary effects.
Innovation Solution
Development of novel urea hydantoin derivatives that act as potent and selective FPR2 modulators, including receptor agonists, antagonists, and partial agonists/antagonists, to treat a wide range of disorders associated with FPR2 modulation, specifically designed to target inflammatory responses in ocular and dermal tissues.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If natural ligands like lipoxin A4 are used to target FPR2, then anti-inflammatory and pro-resolutionary effects are achieved, but side effects occur and inefficiencies arise due to inherent physicochemical properties
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of natural ligands through the development of synthetic urea hydantoin derivatives. These compounds maintain the desired FPR2 modulatory effects while altering physicochemical properties to reduce side effects and improve therapeutic reliability.
2Reliability
If broad-acting anti-inflammatory drugs are used, then inflammatory responses are suppressed, but selectivity is lost leading to reduced safety profiles
Solution Approach 1:
The patent applies local quality by designing compounds with specific molecular structures (urea hydantoin derivatives) that target FPR2 selectively. This localized molecular design enables selective modulation of FPR2 without affecting other receptors, thereby improving safety while maintaining therapeutic effectiveness.
3Productivity
If current pharmaceutical agents are used to treat inflammatory disorders, then some therapeutic benefit is achieved, but inefficiencies occur due to limitations in FPR2 modulation
Solution Approach 1:
The patent applies copying by creating synthetic analogs (urea hydantoin derivatives) that replicate and enhance the beneficial effects of natural ligands. These copied structures optimize FPR2 modulation efficiency while overcoming the limitations of natural ligands, thereby improving therapeutic productivity and reliability.
Data Source
AI summary
The present invention relates to urea hydantoin compounds, processes for preparing them, pharmaceutical compositions containing them, and their use as pharmaceuticals as modulators of the FPR2 receptor, and to methods of treating inflammatory diseases or conditions in a subject in need thereof by administering the compound(s) or pharmaceutical composition to the subject.