TLR7 Agonist Compounds for Selective Immune Activation

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Solution Overview

Problem

Current therapies lack effective compounds that can specifically activate Toll-Like Receptor 7 (TLR7) to enhance immune responses against pathogens and diseases, such as viral infections, inflammatory conditions, and cancers, while minimizing autoimmune responses.

Innovation Solution

Development of compounds with a specific structure, represented by Formula (I), which act as TLR7 agonists, activating the receptor to potentiate immune responses and treat various diseases associated with TLR7 activity, including pharmaceutical compositions for different administration routes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If compounds are developed to activate TLR7, then immune response enhancement is achieved, but risk of autoimmune responses increases

Engineering Contradiction:
Improveimmune response effectivenessVSAvoidautoimmune response risk
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs parameter changes by optimizing the chemical structure of TLR7 agonist compounds (Formula I) to achieve selective activation of TLR7 while minimizing off-target effects. By modifying molecular parameters such as substituent groups (R1-R7) and structural features, the compounds achieve enhanced immune response with reduced autoimmune side effects through precise receptor targeting.

Inventive Principle:
Principle #35Parameter changes

2Adaptability or versatility

If broad-spectrum immune activation is used, then coverage against multiple pathogens is improved, but specificity of response decreases

Engineering Contradiction:
Improvepathogen coverage rangeVSAvoidimmune response specificity
Core Design Contradiction:
Adaptability or versatilityVSMeasurement precision

Solution Approach 1:

The patent achieves universality by designing TLR7 agonist compounds that can recognize and respond to diverse pathogens through a single receptor mechanism. The compounds activate TLR7 to initiate immune responses against various pathogen-associated molecular patterns (PAMPs) including viral RNA, bacterial components, and other pathogens, providing broad-spectrum protection while maintaining response coordination through the specific TLR7 pathway.

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

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The compounds effectively activate TLR7, enhancing immune responses against pathogens and diseases, offering therapeutic benefits for conditions like asthma, psoriasis, cancer, and viral infections while potentially reducing autoimmune inflammation.

Implementation Method 1

Pattern recognition receptors are involved in more than just recognition of pathogens via their PAMPs. Once bound, pattern recognition receptors tend to cluster, recruit other extracellular and intracellular proteins to the complex, and initiate signaling cascades that ultimately impact transcription.

Methodology Applied
Scientific EffectToll-Like Receptor activation:

Data Source

PatentEP3137470B1Compounds and compositions as toll-like receptor 7 agonists
Publication Date: 2021.04.07 NOVARTIS AG
  • EP3137470B1 patent drawing
  • EP3137470B1 patent drawing
  • EP3137470B1 patent drawing

AI summary

The invention provides a compounds of formula (I), immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat diseases or disorders associated with Toll-Like Receptor 7 activity.