Bicyclic Compounds Targeting cccDNA for HBV and HDV Control

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Solution Overview

Problem

Current treatments for hepatitis B and D viruses are inadequate, as they only suppress virus replication without curing the infection, and there is no cure or vaccine for hepatitis D, leading to significant health risks and complications.

Innovation Solution

Development of bicyclic compounds or their pharmaceutically acceptable salts that can inhibit the replication of hepatitis B and D viruses, potentially offering a cure by directly targeting and disrupting the viral lifecycle.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current approved drugs are used to treat HBV, then virus replication is suppressed, but the infection is not cured and the virus can re-emerge

Engineering Contradiction:
Improvecure rateVSAvoidvirus re-emergence
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent extracts and targets the covalently closed circular DNA (cccDNA) form of HBV, which is the persistent viral reservoir that causes re-emergence. By specifically eliminating cccDNA through compounds of Formula (I), the invention addresses the root cause of viral re-emergence rather than just suppressing replication temporarily.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent employs preliminary action by targeting and eliminating cccDNA before the virus can re-emerge and cause disease. The compounds prevent the formation of new cccDNA and promote the degradation of existing cccDNA, thereby preemptively removing the source of potential viral re-emergence.

Inventive Principle:
Principle #10Preliminary action

2Reliability

If current approved drugs are used to treat HBV, then virus replication is slowed down, but there is no cure and liver disease progression continues

Engineering Contradiction:
Improvecure rateVSAvoidliver disease progression
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts and targets the cccDNA form of HBV, which is the persistent viral reservoir that causes re-emergence. By specifically eliminating cccDNA through compounds of Formula (I), the invention addresses the root cause of viral re-emergence rather than just suppressing replication temporarily.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the therapeutic parameter from merely suppressing viral replication to actively eliminating the persistent cccDNA form. This parameter change enables the transition from chronic suppression to potential cure, thereby stopping liver disease progression.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If there is no cure or vaccine for hepatitis D, then transmission and complications remain significant, but treatment options are limited

Engineering Contradiction:
Improveinfection controlVSAvoidtreatment options
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent provides multi-functionality by developing compounds that can treat both HBV and HDV infections. The compounds of Formula (I) target common viral mechanisms shared by both hepatitis B and D viruses, enabling a single treatment approach to address both infections and their associated complications.

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

Data Source

PatentUS12384779B2Bicyclic compounds
Publication Date: 2025.08.12 ALIGOS THERAPEUTICS INC
  • US12384779B2 patent drawing
  • US12384779B2 patent drawing
  • US12384779B2 patent drawing

AI summary

Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.