STING Modulator Compounds for Selective Immune Activation
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Solution Overview
Problem
Current therapies lack effective compounds that modulate STING activity for treating inflammatory, allergic, autoimmune, infectious diseases, and cancer, particularly prostate cancer, lung cancer, breast cancer, head and neck cancer, and melanoma, as existing treatments do not adequately address the immune response and type I interferon regulation.
Innovation Solution
Development of compounds of formula (I) that act as STING agonists or modulators, facilitating their use as medicaments to activate or inhibit STING pathways, thereby treating various diseases by regulating immune responses.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If STING agonists are developed to activate immune responses for cancer treatment, then anti-tumor immunity is improved, but unwanted immune activation and inflammation may occur
Solution Approach 1:
The patent applies local quality by designing STING agonists with specific molecular structures (formula I) that enable selective activation of STING in tumor microenvironments. The compounds are configured to activate STING locally at tumor sites while minimizing systemic immune activation, thereby improving anti-tumor immunity without causing unwanted inflammation throughout the body.
Solution Approach 2:
The patent utilizes parameter changes by modifying the chemical structure of STING agonists through systematic variation of molecular parameters (formula I substituents and configurations). This allows optimization of the agonists' activity, selectivity, and pharmacokinetic properties to achieve effective tumor immunity while controlling harmful immune activation effects.
2Reliability
If STING is activated to produce type I interferons for immune response, then immunity against infections and cancer is improved, but autoimmune reactions may be triggered
Solution Approach 1:
The patent applies local quality by designing STING agonists that selectively activate the immune response in specific tumor microenvironments rather than systemically. This localized activation generates type I interferons and anti-tumor immunity at cancer sites while avoiding widespread immune activation that could trigger autoimmune reactions.
Solution Approach 2:
The patent uses STING agonists as intermediary substances that bridge the gap between detecting tumor presence and generating protective immunity. These compounds act as controlled mediators that activate STING signaling only when and where needed, preventing direct harmful effects while achieving the desired immune response.
3Reliability
If synthetic STING agonists are used to treat cancer, then treatment efficacy is improved, but compound complexity and development difficulty increase
Solution Approach 1:
The patent applies segmentation by dividing the complex task of cancer treatment into a modular approach: first identifying the STING pathway as the target, then developing a series of related compounds (formula I) that share common structural features. This segmentation allows systematic optimization of individual compound properties while maintaining overall treatment efficacy.
Solution Approach 2:
The patent applies universality by designing a family of STING agonists (formula I) that share common structural motifs and mechanisms of action. This universal approach allows a single structural framework to address multiple cancer types and treatment scenarios, reducing the need for entirely new compound developments for each application.
Data Source
AI summary
The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.