Cyclic Di-Nucleotide STING Agonists for Interferon Potency
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Solution Overview
Problem
There is a need for new agents that can induce potent type I interferon production, which is crucial for antiviral and anti-cancer therapies, as existing compounds may not be sufficient in activating the STING pathway effectively to stimulate a strong immune response.
Innovation Solution
Development of novel cyclic di-nucleotide compounds that act as STING agonists, activating the STING pathway to induce type I interferon production, which can be used in pharmaceutical compositions alone or in combination with other therapeutic agents for immune response induction and cancer treatment.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing compounds are used to activate the STING pathway, then some immune response is generated, but the type I interferon production is not potent enough for effective antiviral and anti-cancer therapy
Solution Approach 1:
The patent modifies the chemical structure of cyclic di-nucleotide compounds by changing parameters such as the sugar moiety (ribose vs. arabino configuration), nucleobase composition (2'-3' linkages), and substituent groups to optimize STING pathway activation and type I interferon production potency for therapeutic applications
Solution Approach 2:
The invention creates composite cyclic di-nucleotide structures combining specific nucleoside units with modified sugar rings and nucleobases to form novel compounds that exhibit enhanced STING agonist activity and therapeutic effectiveness compared to natural cyclic dinucleotides
Data Source
AI summary
A class of polycyclic compounds of general formula (II), of general formula (II'), or of general formula (II"), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3a, R4, R4a, R5, R6, R6a, R7, R7a, R8, and R8a are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.