Macrocyclic STING Agonists for Immune Activation
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Solution Overview
Problem
Current therapies for cancer and infectious diseases lack effective activation of the STING pathway, which is crucial for inducing antitumor and antiviral immune responses, as existing STING agonists have limitations in specificity and efficacy.
Innovation Solution
Development of macrocyclic compounds represented by general Formula (I) and its tautomeric forms, stereoisomers, and pharmaceutically acceptable salts, which act as STING modulators to activate the STING pathway, thereby promoting immune responses against cancer and infectious diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing STING agonists are used, then STING pathway activation is achieved, but specificity and efficacy are limited
Solution Approach 1:
The patent employs parameter changes by modifying the chemical structure of STING agonists through macrocyclic compound design (Formula I), adjusting molecular parameters such as ring size, substituent groups (R1-R6), and structural constraints to achieve both high efficacy and specificity in STING pathway activation
Solution Approach 2:
The invention creates composite molecular structures combining macrocyclic frameworks with specific functional groups and substituent patterns, forming a composite agonist structure that simultaneously enhances binding affinity (efficacy) and selectivity (specificity) for the STING protein
2Reliability
If current cancer therapies are used, then treatment is provided, but effective activation of STING pathway is not achieved
Solution Approach 1:
The macrocyclic compounds act as intermediary agents that bridge the gap between current cancer therapies and STING pathway activation, serving as a mediating substance that triggers the STING pathway to produce the desired immune response enhancement
Solution Approach 2:
The patent applies preliminary action by pre-activating the STING pathway using the macrocyclic agonist before administering cancer therapy, thereby preparing the immune system in advance to mount a more effective antitumor response
Data Source
AI summary
Disclosed are the macrocyclic compounds having the general Formula (I) and their tautomeric forms, stereoisomers, pharmaceutically acceptable salts, and their combination with suitable medicament, corresponding processes for the synthesis and pharmaceutical compositions and uses of compounds disclosed herein.