STING Modulator Compounds for Type I Interferon Activation
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Solution Overview
Problem
There is a need for compounds that can modulate the activity of STING, particularly as agonists, to treat diseases such as inflammatory, allergic, autoimmune, infectious, and cancerous conditions, as existing treatments are inadequate in effectively activating or inhibiting type I interferon production.
Innovation Solution
Development of compounds of formula (I) that act as STING agonists or modulators, capable of activating STING to induce type I interferon production for therapeutic benefits in diseases like cancer, autoimmune diseases, and infectious diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing treatments are used to activate or inhibit type I interferon production, then disease treatment is attempted, but the treatments are inadequate in effectively activating or inhibiting type I interferon production
Solution Approach 1:
The patent employs parameter changes by modifying the chemical structure of STING agonist compounds (formula I) to optimize their biological activity. By systematically varying molecular parameters such as substituent groups R1-R6, X1-X2, and core structure features, the invention achieves compounds with enhanced ability to activate STING and induce type I interferon production, directly addressing the inadequacy of existing treatments
Solution Approach 2:
The patent introduces compound (I) as an intermediary substance that mediates between the administered drug and the STING pathway. These compounds act as synthetic agonists that bind to and activate STING, serving as intermediaries to trigger the desired immune response and type I interferon production, thereby overcoming the limitations of direct or existing indirect modulation approaches
2Reliability
If STING is activated to promote type I IFN and TNFα release for immunity-mediated anti-tumor response, then anti-tumor immunity is enhanced, but the complexity of achieving specific activation in tumor microenvironment increases
Solution Approach 1:
The patent applies local quality by designing compounds that preferentially activate STING in the tumor microenvironment. The chemical structure of compound (I) is optimized to interact with STING in the specific physiological context of tumor-resident dendritic cells, enabling localized immune activation without requiring complex delivery systems or conditional activation mechanisms
Solution Approach 2:
The patent employs self-service by utilizing the endogenous STING pathway and associated signaling molecules (cGAS, cGAMP, IRF3, NFkB) to achieve anti-tumor immunity. The compound (I) activates the existing immune infrastructure, allowing the body's own immune system to perform the anti-tumor function without requiring external complex systems or continuous external intervention
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.