STING Agonist Compounds for Immune Activation

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Solution Overview

Problem

Current treatments for cancer and immune response modulation lack effective STING agonists that can induce robust interferon production and immune activation, limiting their therapeutic potential.

Innovation Solution

Development of novel compounds of Formula (I) with STING agonistic activity, which can be administered to induce immune responses, type I interferon production, and treat cell proliferation disorders, including their use in vaccine compositions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments are used for cancer and immune response modulation, then existing therapeutic approaches are maintained, but effective STING agonists that can induce robust interferon production and immune activation are lacking, limiting therapeutic potential

Engineering Contradiction:
Improvetherapeutic potentialVSAvoidimmune activation capability
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent employs parameter changes by systematically varying chemical structures of STING agonists, including modifications to the core purine ring, substituent groups, and linker regions. These structural parameter changes enable the development of compounds with enhanced STING activation capability and robust interferon production, directly addressing the limitation of current treatments lacking effective STING agonists

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent utilizes composite material principles by creating complex molecular structures that combine multiple functional elements: a purine core, specific substituent groups (such as halo, alkyl, or aryl groups), and linker regions. These composite molecular structures work synergistically to achieve potent STING activation and immune response modulation, enhancing therapeutic potential beyond existing single-component approaches

Inventive Principle:
Principle #40Composite materials

2Reliability

If novel compounds of Formula (I) are developed with STING agonistic activity, then immune responses and type I interferon production are enhanced, but the complexity of compound structure and synthesis increases

Engineering Contradiction:
Improveimmune response inductionVSAvoidcompound structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the STING agonist molecule into distinct functional segments: a core purine structure (segments 1-6), substituent groups (segments 7-12), and linker regions (segments 13-18). This segmentation allows for independent optimization of each component's function while maintaining overall molecular stability and STING binding capability, managing structural complexity through modular design

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent implements universality by designing a core purine structure that serves multiple functions: it provides the foundational scaffold for STING binding, enables attachment of various substituent groups for enhanced activity, and maintains structural stability. This multi-functional core structure reduces overall complexity by consolidating multiple roles into a single molecular element

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

Data Source

PatentUS12054512B2Sting modulator compounds, and methods of making and using
Publication Date: 2024.08.06 TAKEDA PHARMA CO LTD
  • US12054512B2 patent drawing
  • US12054512B2 patent drawing
  • US12054512B2 patent drawing

AI summary

The present disclosure provides STING modulators/agonists, and methods of synthesis and methods for using for the prophylaxis or treatment of cancer and other STING-related diseases.The present disclosure relates to a compound represented by the Formula (I):wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.