SSAO/VAP-1 Inhibitor Compounds for NASH and Chronic Pain
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Solution Overview
Problem
Current treatments for nonalcoholic steatohepatitis (NASH) and chronic pain lack efficacy, and existing drugs for pain management have adverse effects, while there is a need for effective SSAO/VAP-1 inhibitors to address liver inflammation, fibrosis, and associated disorders.
Innovation Solution
Development of compounds of Formula (I) or (I′) and their pharmaceutically acceptable forms to inhibit SSAO/VAP-1, administered for treating SSAO-mediated disorders, including liver diseases, NASH, and chronic pain.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current standard of care (diet control and lifestyle changes) is used for NASH treatment, then treatment simplicity is maintained, but therapeutic efficacy is insufficient once liver cell injury and inflammation are evident
Solution Approach 1:
The patent introduces a novel pharmacological parameter (SSAO/VAP-1 inhibition) to change the therapeutic approach from lifestyle modifications to targeted enzyme inhibition, thereby improving efficacy for patients with established liver injury and inflammation
2Reliability
If NSAIDs and opioids are used for chronic pain management, then pain relief is achieved, but adverse effects and abuse potential increase
Solution Approach 1:
The patent uses SSAO/VAP-1 inhibition as an intermediary mechanism to achieve pain relief through a different pathway than traditional NSAIDs and opioids, thereby providing effective analgesia without the associated adverse effects and abuse potential
Solution Approach 2:
The patent changes the pharmacological parameter from COX inhibition or opioid receptor activation to SSAO/VAP-1 inhibition, providing a novel mechanism for pain management that avoids the harmful effects of current therapies
3Reliability
If SSAO/VAP-1 inhibition is used to treat liver diseases, then liver inflammation and fibrosis are reduced, but novel therapeutic agents are required
Solution Approach 1:
The patent segments the therapeutic approach by targeting specific SSAO/VAP-1 inhibitor compounds with defined chemical structures (Formula I and Formula I'), allowing for systematic development and optimization of therapeutic agents
Solution Approach 2:
The patent defines specific chemical parameters and structural features for SSAO/VAP-1 inhibitors, enabling the development of novel therapeutic agents with optimized efficacy and safety profiles for treating liver diseases
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 compounds provide therapeutic benefits in reducing liver inflammation, fibrosis, and pain, offering a novel pharmacological strategy with improved safety and efficacy compared to existing treatments.
Implementation Method 1
SSAO/VAP-1 has amine oxidase enzymatic activity. SSAO catalyzes oxidative deamination of primary amines and produces aldehyde, hydrogen peroxide and ammonium.
Data Source
AI summary
The application relates to a compound of Formula (I′) or (I):or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of Formula (I′) or (I), and a method of treating or preventing a disease in which SSAO plays a role.