Phenyl Acetamide IL-17A Modulators for Oral Inflammatory Treatment

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Solution Overview

Problem

Current treatments for inflammatory diseases, such as psoriasis and ankylosing spondylitis, either require costly biologics that are not orally absorbable or small molecule modulators that lack efficacy.

Innovation Solution

Development of a compound represented by Formula (I) or its pharmaceutically acceptable salt, which is a potent small molecule IL-17A modulator for oral administration, designed to treat inflammatory diseases by modulating IL-17A activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If biologic treatments (Secukinumab and Ixekizumab) are used to modulate IL-17A, then treatment efficacy is improved, but cost of entry increases and oral absorption is lost

Engineering Contradiction:

Improvetreatment efficacyVSAvoidoral absorption

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent replaces the mechanical/injection-based biologic treatment system with a chemically-based small molecule system that can be orally administered. The small molecule compounds of Formula (I) substitute for the biologic agents, achieving IL-17A modulation through chemical interaction rather than protein-based mechanisms, thereby enabling oral absorption while maintaining therapeutic efficacy.

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

2Ease of operation

If small molecule modulators are used for oral administration, then cost of entry is reduced and oral absorption is enabled, but treatment efficacy decreases

Engineering Contradiction:

Improveoral administrationVSAvoidtreatment efficacy

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent optimizes the molecular parameters of the small molecule compounds to enhance their binding affinity and potency toward IL-17A. By carefully adjusting structural parameters in Formula (I) including the heterocycle A, linker B, and substituents R1-R6, the compounds achieve improved efficacy while maintaining oral bioavailability, thus resolving the trade-off between ease of administration and treatment effectiveness.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If biologic treatments are used, then treatment efficacy is improved, but cost of entry increases

Engineering Contradiction:

Improvetreatment efficacyVSAvoidcost of entry

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent employs small molecule compounds that are chemically synthesized rather than biologically manufactured, resulting in lower production costs. These small molecules can be produced through established chemical synthesis methods, making them more cost-effective than biologic treatments while providing sustained therapeutic effect through appropriate dosing regimens.

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

Data Source

PatentUS20240376056A1Phenyl acetamide based il-17a modulators and uses thereof

Publication Date: 2024.11.14 DICE ALPHA INC

AI summary

The disclosure herein provides phenyl acetamide based compounds of Formula (I), (I-a), (II), and pharmaceutical compositions thereof, for the modulation of IL-17A, useful in the treatment of inflammatory conditions such as psoriasis.