LXR Modulator Compounds for Dermal Barrier Repair

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Solution Overview

Problem

Current treatments for dermal diseases and conditions such as skin aging, psoriasis, and skin cancer lack effective modulation of liver X receptor (LXR) activation, which is crucial for maintaining the dermal barrier and reducing inflammation.

Innovation Solution

Development of compounds of Formula E and V, which are LXR modulators, for topical application to stimulate epidermal differentiation, lipid production, and reduce inflammation, thereby improving the dermal barrier function and treating various skin conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If LXR activation is used to treat dermal diseases, then inflammation is reduced and dermal barrier function is improved, but current treatments lack effective LXR modulation

Engineering Contradiction:
Improvedermal barrier functionVSAvoidLXR modulation capability
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies molecular parameters by designing compounds with specific structural features (Formula E and V) that optimize LXR binding affinity and modulatory activity, transforming existing treatments into effective LXR modulators

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces LXR as an intermediary target between existing treatments and dermal disease outcomes, where LXR modulators mediate the therapeutic effect by regulating inflammation and barrier function through LXR activation

Inventive Principle:
Principle #24Intermediary (Mediator)

2Productivity

If LXR modulators are developed for topical application, then epidermal differentiation and lipid production are stimulated, but compound structure complexity increases

Engineering Contradiction:
Improveepidermal differentiationVSAvoidcompound structure
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent applies local quality by introducing specific functional groups and substituents at particular positions in the molecular structure (as defined in Formula E and V) to achieve LXR modulatory activity while maintaining overall structural manageability

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent segments the complex molecular structure into defined components (Formula E and V with specific R groups and structural elements) that can be independently optimized and combined to achieve desired LXR modulatory effects

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP2820013B9Liver x receptor (LXR) modulators for the treatment of dermal diseases, disorders and conditions
Publication Date: 2019.01.09 RALEXAR THERAPEUTICS INC
  • EP2820013B9 patent drawingFigure 1
  • EP2820013B9 patent drawingFigure 2
  • EP2820013B9 patent drawing

AI summary

Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of dermal diseases, disorders or conditions. Also described herein are pharmaceutical compositions containg such compounds.