ALCAT1 Inhibitor Compounds for Mitochondrial Dysfunction Control

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Solution Overview

Problem

There is a need for compounds that can inhibit ALCAT1 activity to treat aging and age-related diseases such as type 2 diabetes, diabetic complications, cardiovascular diseases, neurodegenerative diseases, and other disorders associated with mitochondrial dysfunction.

Innovation Solution

Development of compounds according to formula (I) that inhibit ALCAT1 activity, which are administered in a pharmaceutical composition to target and down-regulate ALCAT1, thereby mitigating mitochondrial dysfunction and related diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If ALCAT1 is overexpressed, then cardiolipin remodeling is enhanced, but mitochondrial dysfunction and oxidative stress increase

Engineering Contradiction:
Improvecardiolipin remodeling activityVSAvoidoxidative stress
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by developing compounds that modify ALCAT1 activity through specific chemical interactions. The inhibitors change the enzymatic parameters of ALCAT1, reducing its catalytic activity toward cardiolipin remodeling, thereby decreasing oxidative stress while maintaining beneficial metabolic functions.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces chemical compounds as intermediary substances that mediate between ALCAT1 and its substrate (cardiolipin). These compounds act as inhibitors, interfering with the enzyme-substrate interaction to reduce harmful cardiolipin remodeling while preserving other physiological functions.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Object-affected harmful factors

If ALCAT1 is inhibited, then oxidative stress is reduced, but mitochondrial fusion may be impaired

Engineering Contradiction:
Improveoxidative stressVSAvoidmitochondrial fusion
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent employs parameter changes by carefully controlling the degree and specificity of ALCAT1 inhibition. The compounds are designed to modulate enzymatic activity parameters to achieve selective inhibition of harmful cardiolipin remodeling while preserving essential mitochondrial fusion functions through MFN2.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent applies local quality by achieving selective inhibition of specific ALCAT1 functions. The inhibitors are designed to target specific substrate interactions (cardiolipin remodeling) while leaving other ALCAT1-dependent processes (such as mitochondrial fusion support) unaffected, thereby maintaining local functional differentiation.

Inventive Principle:
Principle #3Local quality

3Reliability

If ALCAT1 is inhibited, then mitochondrial fragmentation is prevented, but DHA content in cardiolipin may increase

Engineering Contradiction:
Improvemitochondrial network stabilityVSAvoidDHA content in cardiolipin
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent introduces chemical compounds as intermediary substances that mediate the interaction between ALCAT1 and cardiolipin. These inhibitors specifically block the enzymatic conversion that increases DHA content, thereby preventing mitochondrial fragmentation while controlling lipid composition changes.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent converts the potential harmful effect of increased DHA content (which can lead to lipid peroxidation) into a beneficial outcome by selectively inhibiting ALCAT1. The inhibition prevents excessive DHA incorporation while maintaining adequate levels for mitochondrial function, thereby transforming a potential harm into a protective effect.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

Data Source

PatentUS12630541B2Compounds useful as inhibitors of ALCAT 1
Publication Date: 2026.05.19 PERENNA PHARMACEUTICALS INC
  • US12630541B2 patent drawing
  • US12630541B2 patent drawing
  • US12630541B2 patent drawing

AI summary

Inhibitors of ALCAT1 are described having the general formula: (I). These compounds offer a treatment for aging and age-related diseases.