Adamantane Derivatives Inhibiting Filovirus Entry

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Solution Overview

Problem

Current antiviral therapies lack effective solutions for inhibiting the infection of filoviruses, such as Ebola and Marburg, which cause severe hemorrhagic fevers with high mortality rates.

Innovation Solution

The use of compounds represented by Structural Formula I, or their pharmaceutically acceptable salts, which are administered to inhibit filovirus infection by targeting the cell entry process mediated by filovirus glycoproteins.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current antiviral therapies are used, then treatment of other enveloped viruses is possible, but effective inhibition of filovirus infection is lacking

Engineering Contradiction:
Improveeffectiveness of antiviral therapyVSAvoidbroad-spectrum antiviral activity
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent develops adamantane derivative compounds that function as broad-spectrum antivirals effective against multiple enveloped virus families including Filoviridae, Coronaviridae, Flaviviridae, and others. These compounds target conserved viral entry mechanisms shared across different enveloped viruses, enabling a single therapeutic agent to address multiple viral threats simultaneously.

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

Solution Approach 2:

The invention modifies the chemical structure of adamantane derivatives by varying substituents at different positions (R1-R10 groups) to optimize antiviral activity. By changing molecular parameters such as hydrophobicity, steric bulk, and electronic properties, the compounds achieve enhanced potency and selectivity against filoviruses while maintaining broad-spectrum activity.

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If compounds targeting filovirus glycoproteins are developed, then filovirus infection is inhibited, but lack of effective antiviral solutions for high mortality rates persists

Engineering Contradiction:
Improvefilovirus infection and replicationVSAvoidmortality rate from filovirus infection
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The adamantane derivative compounds intervene at the very initial stage of viral infection by blocking glycoprotein-mediated cell entry. By preventing virus attachment and fusion with host cells before replication begins, these compounds stop the infection cascade early, reducing viral load and preventing the progression to severe disease and high mortality.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The compounds act as molecular intermediaries that interfere with the interaction between filovirus glycoproteins and host cell receptors. The adamantane core structure with specific substituents serves as a steric and chemical barrier, blocking the glycoprotein's ability to mediate membrane fusion without requiring direct contact with vulnerable viral components.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS12240857B2Adamantane derivatives for the treatment of filovirus infection
Publication Date: 2025.03.04 ARISAN THERAPEUTICS INC
  • US12240857B2 patent drawing
  • US12240857B2 patent drawing
  • US12240857B2 patent drawing

AI summary

Compounds of structural Formula I were developed for the treatment of infections by filoviruses including Ebolavirus and Marburgvirus, wherein, R1, R2, R3, X and Y are defined in the specification.