Substituted Tetrahydroquinolinone Modulators for RORγ and IL-17 Control
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Solution Overview
Problem
There is a need for compounds that modulate RORγ activity to treat diseases mediated by RORγ, such as autoimmune disorders and inflammatory conditions, as existing treatments are inadequate.
Innovation Solution
Development of substituted tetrahydroquinolinone compounds that act as RORγ modulators, specifically targeting RORγ to regulate its activity and reduce IL-17 production.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing treatments are used for RORγ-mediated diseases, then treatment options are limited, but therapeutic effectiveness is inadequate
Solution Approach 1:
The patent applies parameter changes by systematically modifying chemical structures of tetrahydroquinolinone compounds through varying substituents at different positions (R1-R7 groups). This structural parameter optimization enables the development of compounds with improved RORγ modulatory activity, directly addressing the inadequate therapeutic effectiveness of existing treatments while maintaining structural versatility for multiple disease applications
2Reliability
If new RORγ modulator compounds are developed, then therapeutic benefits are improved, but compound structure complexity increases
Solution Approach 1:
The patent employs segmentation by dividing the tetrahydroquinolinone core structure into distinct functional regions with specific substituent positions (R1-R7). Each position can be independently optimized with specific functional groups, allowing systematic improvement of therapeutic benefits while maintaining a manageable modular structure that simplifies synthesis and characterization
Solution Approach 2:
The patent applies local quality by assigning specific functional groups to specific positions on the tetrahydroquinolinone ring system. For example, particular substituents at R2, R6, or R7 positions are optimized to enhance RORγ binding affinity or selectivity, thereby improving therapeutic benefits without requiring complex overall molecular architecture
Data Source
AI summary
The present invention provides substituted tetrahydroquinolinone and related compounds of formula (I), which are therapeutically useful as modulators of Retinoic acid receptor-related orphan receptors (RORs), more particularly as RORγ modulators. These compounds are useful in the treatment and prevention of diseases and/or disorder, in particular their use in diseases and/or disorder mediated by RORγ receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted tetrahydroquinolinone or related compounds of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.