NLRP3 Antagonist Compounds for Inflammatory Disease Treatment
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Solution Overview
Problem
Current treatments lack effective modulation of NLRP3 activity, which is implicated in various complex diseases such as type 2 diabetes, Alzheimer's disease, and inflammatory disorders, leading to inadequate management of these conditions.
Innovation Solution
Development of chemical entities, including compounds and their pharmaceutically acceptable salts, hydrates, or cocrystals, that antagonize NLRP3 by inhibiting IL-1β and IL-18 production, either by direct binding or altering NLRP3 distribution, for use in pharmaceutical compositions and treatment methods.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments are used for diseases associated with NLRP3 signaling, then existing therapeutic options are available, but effective modulation of NLRP3 activity is lacking leading to inadequate disease management
Solution Approach 1:
The patent applies parameter changes by developing compounds that specifically modulate NLRP3 activity through chemical structure variations. The compounds of Formula I and its salts introduce new chemical parameters and mechanisms to achieve effective NLRP3 modulation, directly addressing the lack of effective modulation capability in current treatments while maintaining disease management effectiveness.
2Object-affected harmful factors
If NLRP3 activity is increased to treat conditions requiring enhanced inflammatory response, then immune defense may be improved, but pathogenic activation in disorders such as CAPS and metabolic diseases worsens
Solution Approach 1:
The patent applies local quality by designing compounds with specific molecular structures (Formula I) that target NLRP3 activity in a controlled and localized manner. The compounds provide precise modulation at the molecular level, enabling selective inhibition of pathogenic NLRP3 activation in autoimmune and metabolic diseases while preserving necessary immune defense functions.
Solution Approach 2:
The patent applies inversion by switching from approaches that attempt to manage inflammation broadly to those that specifically inhibit NLRP3 activation. The compounds reverse the pathogenic overactivation of NLRP3 in diseases like CAPS and metabolic disorders, transforming the harmful excessive activation into a controlled state while maintaining protective immune functions.
3Object-generated harmful factors
If broad-spectrum anti-inflammatory treatments are used, then general inflammation may be reduced, but specific NLRP3-mediated pathology is not adequately addressed
Solution Approach 1:
The patent applies the intermediary principle by introducing compounds of Formula I as specific mediators that target NLRP3. These compounds act as precise intermediaries between the therapeutic agent and the NLRP3 pathway, providing specific control over NLRP3-mediated inflammation rather than broad-spectrum suppression, thereby achieving both general inflammation reduction and specific pathway control.
Data Source
AI summary
In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.