Steroid Analogues with Polar Groups for CNS Injury Treatment

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Solution Overview

Problem

Current pharmacological agents are ineffective in consistently improving outcomes after traumatic brain injury (TBI) or stroke, and progesterone, while neuroprotective, suffers from poor solubility and potential side effects.

Innovation Solution

Development of novel steroid analogues functionalized with polar groups at the C3 and C20 positions, such as amino acid substituents, to enhance water solubility and bioavailability for the treatment of CNS injuries.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If progesterone is used as a neuroprotective agent, then neuroprotection efficacy is improved, but water solubility deteriorates

Engineering Contradiction:

Improveneuroprotection efficacyVSAvoidwater solubility

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The patent modifies the chemical structure of progesterone by introducing polar functional groups at specific positions (C3 and C20) to change its physical properties. This structural modification increases water solubility while maintaining the core neuroprotective activity, resolving the contradiction between efficacy and solubility.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention creates composite steroid molecules that combine the neuroprotective steroid core with hydrophilic functional groups (such as amino acids, carbohydrates, or polar substituents). This composite structure integrates both lipophilic neuroprotective properties and hydrophilic solubility characteristics.

Inventive Principle:

Principle #40Composite materials

2Reliability

If progesterone is administered to achieve neuroprotection, then treatment effectiveness is improved, but side effects increase

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent introduces specific functional groups at particular positions (C3 and C20) of the steroid molecule to modify local chemical properties. This localized modification enhances water solubility and reduces non-specific interactions that cause side effects, while preserving the neuroprotective function at the target site.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

By changing the chemical parameters of progesterone (introducing polar groups), the patent alters the drug's pharmacokinetic profile to reduce toxicity and side effects while maintaining therapeutic efficacy.

Inventive Principle:

Principle #35Parameter changes

3Quantity of substance

If steroid analogues with polar groups are developed, then water solubility is improved, but drug complexity increases

Engineering Contradiction:

Improvewater solubilityVSAvoiddrug structure complexity

Core Design Contradiction:

Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent systematically modifies steroid structures by introducing specific types of polar groups (amino acids, carbohydrates, hydroxyl groups) at defined positions. This structured approach to parameter change achieves solubility improvement while maintaining reasonable structural complexity for pharmaceutical development.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS10716795B2Steroid analogues for neuroprotection

Publication Date: 2020.07.21 EMORY UNIVERSITY

AI summary

Provided are steroid analogues functionalized with polar substituents at the C3 and/or C20 positions of the steroid ring system that exhibit improved water solubility. Also provided are pharmaceutical compositions comprising the steroid analogues and methods using the novel steroid analogues for the treatment and prevention of neurodegeneration in a patient following injury to the central nervous system.