Novel Formula Ib Compounds for NLRP3 Inflammasome Inhibition
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Solution Overview
Problem
Current treatments for NLRP3-related diseases, such as CAPS, type 2 diabetes, and atherosclerosis, lack compounds with improved pharmacological and physicochemical properties and offer limited potency and specificity in inhibiting the NLRP3 inflammasome.
Innovation Solution
Development of novel organic compounds of formula Ib, which modulate NLRP3 inhibition, including specific substitutions and pharmaceutically acceptable salts, to provide enhanced therapeutic options for NLRP3-related diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments are used for NLRP3-related diseases, then treatment options are available, but potency and specificity in inhibiting the NLRP3 inflammasome are limited
Solution Approach 1:
The patent segments the treatment approach by developing multiple distinct compound series (formula I compounds) with different structural configurations and substitution patterns, each targeting NLRP3 inhibition through slightly different mechanisms, thereby providing both high potency and diverse treatment options
Solution Approach 2:
The patent systematically varies chemical parameters including substituent types (halo, alkyl, cycloalkyl), positions (R1-R4), and molecular structure characteristics to optimize both the potency/specificity of NLRP3 inhibition and to create a library of compounds with improved pharmacological and physicochemical properties
2Reliability
If novel compounds of formula Ib are developed, then pharmacological and physicochemical properties are improved, but compound structure complexity increases
Solution Approach 1:
The patent applies local quality by introducing specific functional groups and substituents at particular positions (R1-R4) on the core molecular structure, allowing optimization of pharmacological properties at specific locations without requiring complete structural redesign, thus balancing improved properties with manageable complexity
Solution Approach 2:
The patent develops a universal core structure (formula I and Ib) that can accommodate multiple different substituent patterns and configurations, creating a platform that provides both improved pharmacological properties across the series and structural coherence that limits overall complexity
Data Source
AI summary
The invention relates to novel compounds having the general formula Ibwherein R1, R2, R3, R4, R5 and Z are as described herein, composition including the compounds and methods of using the compounds.