Azobenzene Derivatives for Deep-Tissue Ionizing-Radiation Activation

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Solution Overview

Problem

Current photosensitive systems for therapeutic applications are limited to depths of a few hundred micrometers below the body surface due to the intrinsic limitations of UV, visible, or near-infrared radiation penetration, and activation by ionizing radiation requires high doses that are not clinically viable.

Innovation Solution

Development of a molecular energy converter combined with a photosensitive switch, utilizing azobenzene moieties, activated by highly penetrating ionizing radiation at moderate doses, allowing deep tissue activation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Illumination intensity

If UV, visible or near infrared radiation is used to activate photosensitive systems, then the activation mechanism works effectively, but the penetration depth into tissues is limited to a few hundred micrometers

Engineering Contradiction:
Improveradiation penetration depthVSAvoidactivation efficacy
Core Design Contradiction:
Illumination intensityVSReliability

Solution Approach 1:

The patent introduces an intermediary substance (compound of formula I containing a metal atom and an azo group) that acts as a mediator between ionizing radiation and the photosensitive system. This intermediary absorbs ionizing radiation and converts it to visible light, which then activates the photosensitive system. This resolves the contradiction by enabling deep tissue penetration through ionizing radiation while maintaining effective photosensitive activation through the visible light conversion process.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Illumination intensity

If ionizing radiation is used to activate compounds, then deep tissue penetration is achieved, but extremely high doses are required which are not clinically viable

Engineering Contradiction:
Improveradiation penetration depthVSAvoidradiation dose
Core Design Contradiction:
Illumination intensityVSUse of energy by moving object

Solution Approach 1:

The patent changes the energy conversion parameters by introducing a compound with specific structural features (formula I with metal atom and azo group) that optimizes the conversion efficiency from ionizing radiation to visible light. This parameter change enables effective activation at clinically viable doses (e.g., 2-10 Gy) rather than the extremely high doses previously required, while maintaining deep tissue penetration capability.

Inventive Principle:
Principle #35Parameter changes

3Illumination intensity

If invasive electrodes or optical fibres are used to activate photosensitive systems at depth, then activation can be achieved, but the treatment becomes invasive and complex

Engineering Contradiction:
Improvedeep tissue activationVSAvoidtreatment system complexity
Core Design Contradiction:
Illumination intensityVSDevice complexity

Solution Approach 1:

The patent extracts the activation function from invasive devices (electrodes or optical fibres) and transfers it to a molecular-level mechanism. The compound of formula I itself becomes the activation device at the molecular level, eliminating the need for invasive physical delivery systems. This resolves the contradiction by achieving deep tissue activation through a non-invasive approach while maintaining treatment effectiveness.

Inventive Principle:
Principle #2Taking out (Extraction)

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

Enables activation of therapeutic compounds in deep tissues without depth restriction, facilitating real-time control and modulation of therapeutic actions, suitable for clinical applications.

Implementation Method 1

a molecular energy converter (metal chelate) is combined with a photosensitive switch (an azobenzene moiety) to give a photosensitive system that can be activated by highly penetrating light

Methodology Applied
Scientific EffectPhotoisomerization: Photochromism

Implementation Method 2

Ionizing radiation can be used to effectively reach deep tissue, where the high energy of the radiation will be converted locally to specifically activate redox/photosensitive therapeutic systems

Methodology Applied
Scientific EffectEnergy conversion:

Data Source

PatentUS12414991B2Azobenzene derivatives, process for their preparation and their use for therapeutic treatment associated with ionizing radiations
Publication Date: 2025.09.16 UNIV PARIS SACLAY
  • US12414991B2 patent drawing
  • US12414991B2 patent drawing
  • US12414991B2 patent drawing

AI summary

The present invention relates to new ionizing radiation-activatable derivatives, their preparation process and their therapeutic uses.