Cot Modulator Compounds for Targeted Protein Activity Control

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Solution Overview

Problem

Current therapies lack effective agents to modulate the expression or activity of Cot protein, which is involved in inflammatory diseases and cancer, leading to unaddressed conditions such as rheumatoid arthritis, multiple sclerosis, inflammatory bowel disease, diabetes, sepsis, psoriasis, and graft rejection.

Innovation Solution

Development of compounds that modulate the expression or activity of Cot protein, represented by specific chemical structures, for use in pharmaceutical compositions to treat diseases mediated by Cot.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current therapies are used, then existing treatment options are available, but effective modulation of Cot protein expression or activity is lacking

Engineering Contradiction:
Improveeffectiveness of therapyVSAvoidability to modulate Cot protein
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent employs parameter changes by developing small molecule compounds with specific chemical structures (Formula I) that can modulate Cot protein activity. The compounds feature variable substituents (R1-R6, Z1-Z8) that can be optimized to achieve desired therapeutic effects, representing systematic parameter optimization to overcome the lack of effective Cot modulators in current therapies

Inventive Principle:
Principle #35Parameter changes

2Reliability

If Cot protein activity is modulated, then therapeutic benefits for inflammatory diseases and cancer are achieved, but new compound development and pharmaceutical composition formulation are required

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

Solution Approach 1:

The patent segments the therapeutic approach into distinct components: (1) core compound structures of Formula I with defined variable regions, (2) pharmaceutical compositions containing these compounds, and (3) methods of use for treating specific diseases. This segmentation allows systematic development and optimization of each component independently

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent creates universal solutions by developing compounds that can treat multiple Cot-mediated diseases including inflammatory diseases (rheumatoid arthritis, multiple sclerosis, inflammatory bowel disease, psoriasis), metabolic diseases (diabetes), and cancer. The broad-spectrum applicability reduces the need for disease-specific compound development

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentUS20250346609A1Cot modulators and methods of use thereof
Publication Date: 2025.11.13 GILEAD SCIENCES INC
  • US20250346609A1 patent drawing
  • US20250346609A1 patent drawing
  • US20250346609A1 patent drawing

AI summary

The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.