Novel RORγ Modulators for Autoimmune Disease Treatment

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Solution Overview

Problem

Current treatments for autoimmune and inflammatory diseases mediated by RORγ, such as multiple sclerosis, rheumatoid arthritis, psoriasis, and ankylosing spondylitis, are inadequate due to the limited ability to effectively modulate RORγ activity.

Innovation Solution

Development of novel RORγ modulators, specifically compounds according to Formulas I and II, which are designed to treat autoimmune or inflammatory diseases by modulating RORγ activity, including autoimmune or inflammatory diseases like multiple sclerosis, rheumatoid arthritis, psoriasis, and ankylosing spondylitis.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments are used for autoimmune and inflammatory diseases, then existing therapeutic options are available, but the ability to effectively modulate RORγ activity is limited

Engineering Contradiction:
Improveeffectiveness of RORγ modulationVSAvoidability to modulate RORγ activity
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by developing novel chemical compounds with specific molecular structures (Formulas I and II) that have optimized binding affinity and selectivity for RORγ. The compounds feature varying substituent groups (R1-R7) that can be adjusted to fine-tune pharmacological properties, thereby improving the effectiveness and versatility of RORγ modulation compared to existing treatments

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP3148975B1Piperazine derivatives as ROR-gamma modulators
Publication Date: 2018.11.28 GLAXOSMITHKLINE INTPROP DEV LTD
  • EP3148975B1 patent drawing
  • EP3148975B1 patent drawing
  • EP3148975B1 patent drawing

AI summary

Disclosed are novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ.