Trans-4-hydroxycyclohexyl Mitofusin Activators for Neurodegenerative Disease

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Solution Overview

Problem

Current treatments for neurodegenerative diseases and mitochondrial-associated disorders lack effective methods to enhance mitochondrial fusion and subcellular transport, leading to impaired neuronal function and progression of diseases like Charcot-Marie-Tooth disease, Alzheimer's, and Parkinson's.

Innovation Solution

Development of novel trans-4-hydroxycyclohexyl stereoisomers of mitofusin activators that stimulate mitochondrial fusion and subcellular transport, promoting neuronal repair and regeneration by activating mitofusin-1 and mitofusin-2, thereby addressing mitochondrial dysfunction and dysmotility.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments are used for neurodegenerative diseases, then current therapeutic approaches are maintained, but mitochondrial fusion and subcellular transport remain impaired

Engineering Contradiction:

Improvemitochondrial fusion functionVSAvoidneuronal repair capability

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent employs parameter changes by modifying the chemical structure of mitofusin activators through stereoisomer selection (trans-4-hydroxycyclohexyl configuration) to enhance mitochondrial fusion activity and neuronal repair capabilities, directly addressing the impairment in mitochondrial function caused by conventional treatments

Inventive Principle:

Principle #35Parameter changes

2Productivity

If mitofusin activators are developed to stimulate mitochondrial fusion, then neuronal repair is enhanced, but functional potency and pharmacokinetic properties must be optimized

Engineering Contradiction:

Improveneuronal repair rateVSAvoidstereoisomer purity

Core Design Contradiction:

ProductivityVSManufacturing precision

Solution Approach 1:

The patent applies local quality by focusing on the specific trans-4-hydroxycyclohexyl stereoisomer configuration to achieve enhanced functional potency and optimized pharmacokinetic properties, ensuring that the therapeutic effect is concentrated in the most effective molecular form while maintaining manufacturability

Inventive Principle:

Principle #3Local quality

Data Source

PatentUS20250099404A1Trans-4-hydroxycyclohexyl phenyl amide mitofusin activators and methods of use thereof

Publication Date: 2025.03.27 DORN GERALD W II DR

AI summary

Compounds and compositions including stereoisomers of 6-phenylhexanamide derivative small molecule mitofusin activators are described. In particular, mitofusin activators comprising derivatives of (trans-4-hydroxycyclohexyl)-6-phenylhexanamide, which are useful for treating diseases or disorders associated with a mitochondria-associated disease, disorder, or condition such as diseases or disorders associated with mitofusin-1 (MFN1) and/or mitofusin-2 (MFN2), or mitochondrial dysfunction, are described. Methods of treatment and pharmaceutical formulations are also described.