Antiviral Antisense Oligonucleotide Targeting Conserved SARS-CoV-2 RNA

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Solution Overview

Problem

There is no established treatment method for SARS-CoV-2, SARS-CoV-1, and MERS-CoV, which belong to the genus Betacoronavirus, and existing antiviral agents have not been clinically demonstrated to be effective against these viruses.

Innovation Solution

An antisense oligonucleotide targeting specific regions of the genomic RNA of SARS-CoV-2, SARS-CoV-1, and MERS-CoV, comprising 15 to 30 nucleotides complementary to conserved sequences in regions such as the 5' UTR, nsp regions, and 3' UTR, with a gapmer structure and modified nucleotides, is used to inhibit viral replication.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing antiviral agents are used for SARS-CoV-2, then treatment is attempted, but clinical effectiveness is not demonstrated

Engineering Contradiction:
Improveclinical effectivenessVSAvoidestablished treatment method
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent changes the molecular parameters of the antiviral agent by designing antisense oligonucleotides with specific length (15-30 nucleotides), complementarity to conserved regions, and modified nucleotides (gapmer structure with 2'-OMe or 2'-O-MOE groups), transforming ineffective existing agents into potentially effective new agents targeting Betacoronaviruses

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a universal antiviral approach by designing oligonucleotides that target conserved regions across multiple Betacoronavirus species (SARS-CoV-2, SARS-CoV-1, MERS-CoV), enabling a single therapeutic strategy to address multiple viral threats simultaneously

Inventive Principle:
Principle #6Universality (Multi-functionality)

2Reliability

If existing antiviral agents are used for SARS-CoV-1 and MERS-CoV, then treatment is attempted, but no established treatment method exists

Engineering Contradiction:
Improveantiviral effectVSAvoidtreatment coverage
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent develops a universal therapeutic approach by designing antisense oligonucleotides that target conserved regions common to multiple Betacoronavirus species, enabling the same molecular mechanism to potentially treat SARS-CoV-2, SARS-CoV-1, and MERS-CoV with appropriate sequence variations

Inventive Principle:
Principle #6Universality (Multi-functionality)

Solution Approach 2:

The patent adapts the oligonucleotide parameters (sequence, length, modification pattern) to match the specific target virus while maintaining the core gapmer structure and targeting strategy, allowing flexibility across different viral targets

Inventive Principle:
Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The antisense oligonucleotide exhibits a high viral growth inhibitory effect with minimal adverse reactions, capable of targeting multiple Betacoronaviruses, including SARS-related coronaviruses, by specifically binding to conserved regions in their genomic RNA, thereby reducing viral infectivity.

Implementation Method 1

consisting of 15 to 30 nucleotides complementary to a nucleic acid comprising at least 10 consecutive bases in at least one target region

Methodology Applied
Scientific EffectComplementary base pairing:

Data Source

PatentUS20250011786A1Antiviral antisense oligonucleotide
Publication Date: 2025.01.09 NIPPON SHINYAKU CO LTD
  • US20250011786A1 patent drawing

AI summary

The present specification provides an antisense oligonucleotide or a pharmaceutically acceptable salt or hydrate thereof targeting a particular region in genomic RNA of SARS-CoV-2, a pharmaceutical composition comprising the antisense oligonucleotide or the pharmaceutically acceptable salt or hydrate thereof, etc.