Crystalline Salt Forms of Boc-D-Arg-DMT-Lys(Boc)-Phe-NH2 for Mitochondrial Targeting

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Solution Overview

Problem

Current antioxidants struggle to effectively target the electron transport chain (ETC) in mitochondria, leading to inadequate protection against oxidative damage and inefficient ATP production, which contributes to various diseases.

Innovation Solution

Development of various crystalline salt forms of Boc-D-Arg-DMT-Lys(Boc)-Phe-NH2, which can modulate the physicochemical properties of the compound, including its ability to target the ETC and restore normal oxidative phosphorylation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If natural antioxidants are used to protect cells from oxidative damage, then some protection is provided, but they cannot reach the ETC in sufficient concentrations and may reduce ROS to unhealthy levels

Engineering Contradiction:

Improveprotection effectivenessVSAvoiddelivery to target

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent modifies the chemical structure of antioxidants by conjugating them to mitochondrial targeting sequences (MTS) and cell-penetrating peptides (CPP), changing the physical-chemical parameters of the molecule to enable active targeting and accumulation at the ETC while maintaining antioxidant activity

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent uses mitochondrial targeting sequences and cell-penetrating peptides as intermediary carriers that guide the antioxidant to the mitochondrial ETC, solving the delivery problem by introducing a mediating structure that facilitates targeted transport

Inventive Principle:

Principle #24Intermediary (Mediator)

2Object-affected harmful factors

If antioxidants are used to reduce ROS levels, then oxidative damage is reduced, but ROS may be reduced to unhealthy levels and mitochondrial imbalance is not corrected

Engineering Contradiction:

Improveoxidative damageVSAvoidmitochondrial function restoration

Core Design Contradiction:

Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent creates antioxidants with localized action by attaching mitochondrial targeting sequences that direct the molecule specifically to the ETC, ensuring the antioxidant effect is concentrated at the mitochondrial level rather than systemically, thus correcting local mitochondrial imbalance without disrupting overall ROS homeostasis

Inventive Principle:

Principle #3Local quality

3Stability of the object's composition

If crystalline salt forms are developed for Boc-D-Arg-DMT-Lys(Boc)-Phe-NH2, then solubility and stability are improved, but manufacturing complexity increases

Engineering Contradiction:

Improvecompound stabilityVSAvoidmanufacturing process

Core Design Contradiction:

Stability of the object's compositionVSEase of manufacture

Solution Approach 1:

The patent changes the physical state and chemical form of the compound by developing various crystalline salt forms, which improves solubility and stability parameters while providing defined manufacturing protocols for each salt form

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20250188122A1Crystalline salt forms of boc-d-arg-DMT-lys-(BOC)-phe-NH2

Publication Date: 2025.06.12 STEALTH BIOTHERAPEUTICS INC

AI summary

Disclosed are various crystalline salt forms of Boc-D-Arg-DMT-Lys(Boc)-Phe-NH2.