KS-513 Compound Targeting Inflammatory Pathways for COPD Therapy

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Solution Overview

Problem

Current treatments for allergic diseases, inflammatory diseases, asthma, and chronic obstructive pulmonary disease (COPD) lack specific and effective therapies, with existing anti-inflammatory therapies primarily developed for asthma being non-specific and ineffective for COPD, which has a distinct pathological mechanism.

Innovation Solution

A novel compound (KS513) isolated from Pseudolysimachion rotundum var. subintegrum is developed, which exhibits potent anti-inflammatory, anti-allergy, and anti-COPD activity by inhibiting pro-inflammatory enzymes and cytokines, offering a specific treatment for these conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing anti-inflammatory therapies developed for asthma are used, then asthma symptoms may be relieved, but they are non-specific and ineffective for COPD which has a distinct pathological mechanism

Engineering Contradiction:

Improveeffectiveness of therapyVSAvoidspecificity to disease type

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent segments the anti-inflammatory therapy by identifying and targeting specific molecular pathways (iNOS, COX-2, TNF-α, IL-6) that are distinct in COPD compared to asthma. This allows development of therapies tailored to COPD's unique pathological mechanisms rather than using generic anti-inflammatory agents

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The invention applies local quality by focusing on specific inflammatory mediators and enzymes (iNOS, COX-2, TNF-α, IL-6) that are characteristically elevated in COPD. The therapy is designed to selectively inhibit these specific targets in the COPD context, providing disease-specific treatment rather than broad-spectrum anti-inflammatory action

Inventive Principle:

Principle #3Local quality

2Object-affected harmful factors

If broad-spectrum anti-inflammatory agents are used, then general inflammation may be reduced, but they lack the specific efficacy needed for COPD's distinct pathological mechanism

Engineering Contradiction:

Improveinflammation reductionVSAvoiddisease-specific efficacy

Core Design Contradiction:

Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent applies parameter changes by specifically targeting the inhibition of iNOS and COX-2 enzymes along with their downstream cytokines (TNF-α, IL-6) in COPD. This selective parameter-based approach changes the therapeutic strategy from broad anti-inflammatory action to targeted inhibition of specific molecular parameters that are pathologically elevated in COPD

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentEP3310799B1A novel compound (KS 513) isolated from pseudolysimachion rotundum VAR. subintegrum and the composition comprising the same as an active ingredient for preventing or treating allergy disease, inflammatory disease, asthma or chronic obstructive pulmonary disease

Publication Date: 2020.08.26 YUNGJIN PHARMACEUTICAL CO LTD

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AI summary

The present invention relates to a novel (1aS,1bS,2S,4S,5aR,6S,6aS)-1a-(hydroxymethyl)-4-methoxy-2-(((2S,3R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)octahydrooxireno[2',3':4,5]cyclopenta[1,2-c]pyran-6-yl 4-hydroxybenzoate} (KS-513), the isomer thereof, the pharmaceutically acceptable salt or solvates thereof, a composition comprising the same as an active ingredient for preventing or treating allergic disease, inflammatory disease, asthma or chronic obstructive pulmonary disease (COPD) and the use thereof.