8-oxoadenine Compound Immune Modulation via Substituent Optimization
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Solution Overview
Problem
Current interferon-inducing agents for viral and allergic diseases can cause systemic adverse effects, and there is a need for a compound that effectively modulates the immune response without these drawbacks.
Innovation Solution
Development of a novel 8-oxoadenine compound that acts as an immuno-modulator, inducing interferon and suppressing cytokine production such as IL-4 and IL-5, thereby serving as a therapeutic or prophylactic agent for allergic diseases, viral diseases, and cancers.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If interferon-inducing agents are used to treat viral and allergic diseases, then immune response is enhanced, but systemic adverse effects occur
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of adenine derivatives through systematic variation of substituents at positions 2, 6, 8, and 9 of the purine ring. This structural parameter optimization enables the compound to selectively induce interferon-alpha and beta while suppressing Th2 cytokines, achieving enhanced immune response with reduced systemic adverse effects compared to conventional interferon-inducing agents
Solution Approach 2:
The invention applies local quality by designing compounds with specific substituent patterns at different positions of the adenine ring. For example, introducing hydrophobic groups at position 2, electron-withdrawing groups at position 6, and specific substituents at position 9 creates localized chemical properties that direct the compound's immunomodulatory activity toward desired pathways while minimizing off-target effects
2Reliability
If Th2 cell suppression is achieved to treat allergic diseases, then allergic symptoms are reduced, but immune balance may be disrupted
Solution Approach 1:
The patent applies periodic action through the compound's ability to induce interferon production in a controlled manner. The interferon-induced antiviral state and cytokine suppression occur in a regulated temporal pattern, allowing Th2 suppression without causing prolonged immune imbalance. The compound's structure enables sustained but controlled immunomodulation rather than acute suppression
Data Source
AI summary
The present invention provides an 8-oxoadenine compound having immunemodulating activities such as an interferon inducing activity and useful as an antiviral agent and antiallergic agent, which is represented by the following formula (1):[wherein the ring A represents a 6-10 membered aromatic carbocyclic ring and the like, R represents a halogen atom, an alkyl group and the like, n represents an integer of 0-2, Z1 represents alkylene, X2 represents oxygen atom, sulfur atom, SO2, NR5, CO, CONR5, NR5CO and the like, Y1, Y2 and Y3 represent independently a single bond or an alkylene group, X1 represents oxygen atom, sulfur atom, NR4 (R4 is hydrogen atom or an alkyl group) or a single bond, R2 represents a substituted or unsubstituted alkyl group, R1 represents hydrogen atom, hydroxy group, an alkoxy group, an alkoxycarbonyl group or a haloalkyl group]or its pharmaceutically acceptable salt.