HIV Therapeutic Compounds Resolving Viral Resistance

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Solution Overview

Problem

Current antiretroviral therapies for HIV-1 infections face challenges with the emergence of drug-resistant HIV strains, necessitating the development of new antiretroviral agents.

Innovation Solution

A compound of Formula (I) and its pharmaceutically acceptable salts, which are designed to treat HIV infections, either alone or in combination with other therapeutic agents such as HIV protease inhibitors or reverse transcriptase inhibitors, are provided. The compound has a specific structural configuration that includes variously substituted rings and functional groups, allowing for potential efficacy against HIV.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If highly active antiretroviral therapies (HAART) are used to treat HIV-1 infections, then viral load is reduced and disease progression is delayed, but HIV strains resistant to current therapies emerge

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidviral resistance
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of antiretroviral compounds through various substituents (Z1, Z2, Z3, Z4 groups) and ring configurations (rings A and B) to create new compounds with altered properties that can effectively target resistant HIV strains while maintaining therapeutic efficacy

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by combining multiple structural elements (heteroaryl rings, carbocyclic rings, heterocyclic rings, and various functional groups) into complex molecular structures that provide both antiviral activity and resistance to viral mutations, creating a multi-faceted approach to combating HIV resistance

Inventive Principle:
Principle #40Composite materials

2Reliability

If new antiretroviral agents are developed to overcome resistance, then efficacy against resistant strains may improve, but treatment complexity and development time increase

Engineering Contradiction:
Improveefficacy against resistant strainsVSAvoidcompound structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the complex antiretroviral compound into distinct modular components (ring A, ring B, and various substituent positions) that can be independently varied and optimized, allowing systematic development of new agents against resistant strains without requiring complete redesign of the entire molecular structure

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs universality by designing a core molecular framework with multiple possible substituent configurations that can serve multiple therapeutic functions, potentially addressing different resistant strains with variations of the same base structure, thereby reducing overall treatment complexity

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

Data Source

PatentUS10202353B2Therapeutic compounds
Publication Date: 2019.02.12 GILEAD SCIENCES INC
  • US10202353B2 patent drawing
  • US10202353B2 patent drawing
  • US10202353B2 patent drawing

AI summary

Compounds of Formula I, or salts thereof, are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, intermediates useful for preparing compounds of Formula I and therapeutic, methods for treating a Retroviridae viral infection, in particular infection caused by the HIV virus.