Isoprenyl Compounds Modulating G-Protein Signaling for Anti-Inflammatory Therapy

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Solution Overview

Problem

Traditional anti-inflammatory drugs, such as corticosteroids and NSAIDs, used to treat inflammatory diseases often cause significant side effects, and there is a need for compounds that can effectively inhibit inflammation without these adverse effects.

Innovation Solution

Development of specific isoprenyl compounds, structurally related to N-acetyl-S-farnesyl-L-cysteine, which modulate G-protein signaling cascades and inflammatory pathways, inhibiting pro-inflammatory cytokines and oxidative burst responses, thereby reducing inflammation without the side effects of traditional drugs.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional anti-inflammatory drugs (corticosteroids and NSAIDs) are used to treat inflammatory diseases, then inflammation is effectively inhibited, but significant side effects occur (appetite and weight gain, excess sweating, high blood pressure, nausea, vomiting, diarrhea)

Engineering Contradiction:
Improveinflammation inhibition effectivenessVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent modifies the chemical structure of known anti-inflammatory compounds by changing parameters such as the hydrocarbon chain length (C2-C6), substitution groups (halogen, phenyl, heteroaryl rings), and functional groups (-O-, -S-, -NH-, -C(O)-, -CF2-). These parameter changes in molecular structure aim to maintain anti-inflammatory effectiveness while reducing the generation of harmful side effects associated with traditional drugs

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite molecular structures combining farnesyl or geranyl groups with amino acids (cysteine, homocysteine, penicillamine) and various substituent groups. This composite approach produces new compounds that retain the beneficial anti-inflammatory properties while attempting to eliminate the adverse effects of conventional single-structure drugs

Inventive Principle:
Principle #40Composite materials

2Object-generated harmful factors

If new isoprenyl compounds are developed to reduce side effects, then side effect profile is improved, but the compounds must still maintain effective anti-inflammatory activity

Engineering Contradiction:
Improveside effectsVSAvoidinflammation inhibition effectiveness
Core Design Contradiction:
Object-generated harmful factorsVSReliability

Solution Approach 1:

The patent systematically varies molecular parameters including the bivalent hydrocarbon chain L (C2-C6), substitution patterns (halogen, phenyl, heteroaryl), and functional groups to optimize the balance between side effect reduction and maintaining effective anti-inflammatory activity. Specific modifications include replacing methylene units with -O-, -S-, -NH-, or -C(O)- groups

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The compounds act as intermediary substances that modulate G-protein signaling cascades and inflammatory pathways. By interfering with these signaling pathways, the compounds mediate the reduction of pro-inflammatory cytokines and oxidative burst responses, achieving anti-inflammatory effects without triggering the harmful side effects of traditional drugs

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentEP3330252B1Isoprenyl compounds and methods thereof
Publication Date: 2020.02.12 SIGNUM BIOSCIENCES INC
  • EP3330252B1 patent drawingFigure 1
  • EP3330252B1 patent drawingFigure 1
  • EP3330252B1 patent drawingFigure 2

AI summary

Among other things, the present invention provides novel isoprenyl compounds capable of effectively modulating inflammatory responses and pharmaceutical, cosmetic, cosmeceutical and topical compositions comprising these isoprenyl compounds. Antiinflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with inflammation. Proinflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with suppression of inflammatory responses. Thus, the present invention also provides methods useful in the treatment or prevention of diseases or conditions associated with inflammation as well as methods useful in the treatment or prevention of diseases or conditions associated with suppression of inflammatory responses.