Progesterone Phosphate Derivatives for Rapid Aqueous Delivery

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Solution Overview

Problem

Current treatments for traumatic brain injury (TBI) and stroke are inadequate in improving outcomes due to the delayed administration of progesterone, which is insoluble in aqueous-based formulations and requires complex preparation, and have limited plasma half-life, leading to secondary neuronal damage and inflammation.

Innovation Solution

Development of progesterone phosphate derivatives and pharmaceutical compositions that can be easily and rapidly administered, providing neuroprotective effects by reducing inflammation and edema, and enhancing functional recovery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If progesterone is administered in conventional formulations, then neuroprotective effects are achieved, but administration is delayed and preparation is complex

Engineering Contradiction:

Improveneuroprotective effectVSAvoidadministration delay

Core Design Contradiction:

ReliabilityVSLoss of time

Solution Approach 1:

The patent converts progesterone from its conventional insoluble form into water-soluble phosphate ester derivatives, fundamentally changing the solubility parameter to enable rapid dissolution and administration in aqueous formulations, thereby eliminating preparation complexity and administration delays

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent introduces phosphate ester groups as intermediary chemical modifications to progesterone, creating derivatized compounds that serve as effective intermediaries between the original neuroprotective agent and the aqueous administration system, enabling rapid delivery without sacrificing therapeutic efficacy

Inventive Principle:

Principle #24Intermediary (Mediator)

2Reliability

If progesterone is administered in conventional formulations, then neuroprotective effects are achieved, but plasma half-life is limited

Engineering Contradiction:

Improveneuroprotective effectVSAvoidplasma half-life

Core Design Contradiction:

ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent modifies the chemical parameters of progesterone by introducing phosphate ester groups, which alter the pharmacokinetic properties including plasma half-life, enabling sustained circulation and prolonged neuroprotective action while maintaining the core therapeutic mechanism

Inventive Principle:

Principle #35Parameter changes

3Productivity

If progesterone phosphate derivatives are developed, then rapid and sustained neuroprotective effects are achieved, but compound complexity increases

Engineering Contradiction:

Improvefunctional recovery rateVSAvoidcompound structure

Core Design Contradiction:

ProductivityVSDevice complexity

Solution Approach 1:

The patent segments the development process into systematic phases: identifying key structural modifications (phosphate esterification at specific positions), optimizing individual derivatives, and evaluating their pharmacokinetic and pharmacodynamic properties separately before clinical application, thereby managing complexity through structured segmentation

Inventive Principle:

Principle #1Segmentation

Data Source

PatentUS12415829B2Progesterone phosphate analogs and uses related thereto

Publication Date: 2025.09.16 EMORY UNIVERSITY

AI summary

This disclosure relates to progesterone phosphate derivatives and uses related thereto. In certain embodiments, the disclosure relates to compounds disclosed herein and uses for managing inflammation such as those resulting from traumatic brain injury or stroke.