Formula I Compounds for RSV Treatment and Prophylaxis

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Solution Overview

Problem

Current treatments for Respiratory Syncytial Virus (RSV) infections lack effective and safe options, with existing antiviral drugs and antibodies showing limited efficacy and significant side effects, highlighting the need for new therapeutic approaches.

Innovation Solution

Development of novel chemical compounds of a new chemical class that inhibit RSV, specifically represented by compounds of formula (I), which are designed for use in pharmaceuticals to treat and prevent RSV disease.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing antiviral drugs (e.g., ribavirin) are used for RSV treatment, then some antiviral effect is achieved, but side effects and limited efficacy occur

Engineering Contradiction:
Improveantiviral efficacyVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the chemical structure of existing antiviral compounds by changing molecular parameters (introducing specific functional groups, modifying carbon chains, adjusting molecular weight) to achieve better efficacy and safety profile. The compounds of formula (I) represent systematic structural optimization of antiviral agents.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite molecular structures combining different functional groups and chemical moieties in a single molecule. The compounds integrate multiple pharmacological activities into unified molecular entities, achieving synergistic effects that improve antiviral performance while reducing side effects.

Inventive Principle:
Principle #40Composite materials

2Reliability

If monoclonal antibodies (e.g., palivizumab) are used for RSV prophylaxis, then hospitalization rate reduction is achieved, but treatment of established infection is not effective

Engineering Contradiction:
Improveprophylaxis efficacyVSAvoidtreatment effectiveness
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent develops small molecule compounds that can function effectively in both prophylaxis and treatment scenarios. The compounds of formula (I) are designed with broad spectrum activity against RSV, making them versatile for different clinical stages and patient populations, unlike antibodies that are primarily prophylactic.

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

Solution Approach 2:

The invention replaces the antibody-based immune system approach with direct-acting viral inhibitors. Instead of relying on the host immune system mediated by antibodies, the small molecule compounds directly interfere with viral replication mechanisms, providing effective treatment for established infections.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

3Reliability

If more potent antiviral compounds are developed, then efficacy is improved, but safety and tolerability may be compromised

Engineering Contradiction:
Improveantiviral potencyVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces specific functional groups and molecular features at particular locations within the compound structure to achieve selective antiviral activity. The compounds are designed to target specific viral proteins or replication pathways, concentrating the antiviral effect where needed while minimizing off-target effects and toxicity.

Inventive Principle:
Principle #3Local quality

Data Source

PatentUSRE49481E1Compounds for the treatment and prophylaxis of respiratory syncytial virus disease
Publication Date: 2023.04.04 F HOFFMANN LA ROCHE INC
  • USRE49481E1 patent drawing
  • USRE49481E1 patent drawing
  • USRE49481E1 patent drawing

AI summary

A compound of formula (I)as well as pharmaceutically acceptable salt thereof, wherein R1 to R10, A, Q, X and Y are as defined in the specification and claims, and their use as a pharmaceutical for the treatment or prophylaxis of respiratory syncytial virus disease.