Tricyclic Sulfone RORγ Modulators for IL-17 Regulation

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current therapeutic agents are insufficient in addressing the unmet medical need for treating inflammatory and autoimmune diseases, particularly those involving dysregulated IL-17 production, such as psoriasis, rheumatoid arthritis, inflammatory bowel disease, and multiple sclerosis, where RORγ modulation offers a promising therapeutic benefit.

Innovation Solution

Development of specific compounds that modulate RORγt activity, including those of the formula described, which can be used to diagnose, prevent, or treat various immune and inflammatory disorders by targeting the RORγ receptor pathway.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current therapeutic agents are used, then existing treatment protocols are maintained, but they are insufficient for treating inflammatory and autoimmune diseases involving dysregulated IL-17 production

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidtreatment coverage
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent introduces novel chemical compounds with specific molecular structures (tricyclic sulfones) that represent a parameter change in therapeutic agents. These compounds target RORγt receptors to modulate IL-17 production, providing a new mechanism of action that improves therapeutic efficacy for inflammatory and autoimmune diseases where existing agents are insufficient.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If RORγt modulation is implemented, then therapeutic benefits are achieved in treating autoimmune and inflammatory diseases, but new compound development and validation are required

Engineering Contradiction:
Improvetherapeutic benefitVSAvoidcompound development
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent performs preliminary action by providing a comprehensive framework including novel compound structures, synthetic methods, and preclinical validation data before clinical application. The detailed description of synthesis protocols and characterization methods enables straightforward replication and manufacturing, reducing the barrier to translating RORγt modulation into therapeutic practice.

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentEP3541786B1Tricyclic sulfones as ROR gamma modulators
Publication Date: 2020.08.05 BRISTOL MYERS SQUIBB CO
  • EP3541786B1 patent drawing
  • EP3541786B1 patent drawing
  • EP3541786B1 patent drawing

AI summary

There are described RORγ Gamma modulators of the formula (I), (I) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.