Hydroxysteroids Stimulate Mitochondrial Biogenesis

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Solution Overview

Problem

Current treatments for chronic mitochondrial dysfunction and toxicity lack effective prophylactic and therapeutic options, particularly for conditions associated with mitochondrial biogenesis and organ degeneration, such as neuromuscular diseases, diabetes, and heart failure, where existing drugs can cause mitochondrial toxicity and organ degeneration.

Innovation Solution

Development of novel hydroxysteroids, specifically 11β-hydroxypregnenolone and 11β-hydroxyprogesterone, which stimulate mitochondrial biogenesis and activate AMP kinase, thereby enhancing mitochondrial function and reducing oxidative stress and metabolic disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing drugs are administered to treat mitochondrial dysfunction, then some therapeutic effect is achieved, but mitochondrial toxicity and organ degeneration occur

Engineering Contradiction:

Improvetherapeutic effectVSAvoidmitochondrial toxicity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies this principle by developing compounds that specifically target and protect mitochondrial function while converting the harmful effect of mitochondrial dysfunction into a beneficial therapeutic outcome. The hydroxysteroid compounds selectively enhance mitochondrial biogenesis and protect against mitochondrial toxicity, transforming the pathological state into a therapeutic opportunity.

Inventive Principle:

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

Solution Approach 2:

The patent uses AMP-activated protein kinase (AMPK) as an intermediary mediator. The hydroxysteroid compounds activate AMPK, which then serves as a signaling hub to coordinate multiple downstream effects including mitochondrial biogenesis, metabolic regulation, and protection against mitochondrial toxicity, thereby achieving therapeutic effects through a controlled intermediary pathway.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Use of energy by moving object

If mitochondrial function is stimulated to treat dysfunction, then energy production improves, but oxidative stress and cell injury may increase

Engineering Contradiction:

Improveenergy productionVSAvoidoxidative stress

Core Design Contradiction:

Use of energy by moving objectVSObject-generated harmful factors

Solution Approach 1:

The patent applies preliminary action by pre-activating AMPK before mitochondrial biogenesis is fully induced. This preliminary activation of AMPK prepares the cellular environment, upregulates protective mechanisms, and establishes antioxidant defenses in advance, preventing oxidative stress from developing during the mitochondrial stimulation process.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent implements beforehand cushioning by inducing mitochondrial biogenesis in a controlled, gradual manner through AMPK activation. This slow induction allows the cell to adapt and build protective mechanisms concurrently, cushioning against the potential harmful effects of rapid mitochondrial proliferation and associated oxidative stress.

Inventive Principle:

Principle #11Beforehand cushioning (Prior cushioning)

Data Source

PatentUS11542298B2Hydroxysteroid compounds, their intermediates, process of preparation, composition and uses thereof

Publication Date: 2023.01.03 EPIRIUM BIO INC

AI summary

The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds.