Alkylamido Compounds Modulating PPAR and EGF Receptors

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Solution Overview

Problem

Current treatments for diseases associated with PPAR and EGF receptors, such as cancer and inflammatory conditions, lack effective therapeutic agents that specifically modulate these receptors to induce desired cellular responses like apoptosis and anti-inflammatory activity.

Innovation Solution

Development of compounds represented by formulas I and II, which are specific to PPAR and EGF receptors, and their use in pharmaceutical compositions to administer therapeutically effective amounts to treat conditions like cancer and inflammatory diseases, including colorectal cancer and Crohn's disease.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments are used for diseases associated with PPAR and EGF receptors, then existing therapeutic options are available, but effective modulation of these receptors to induce desired cellular responses is lacking

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidreceptor modulation capability
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by systematically varying molecular structures of compounds (changing chemical parameters) to optimize their ability to modulate PPAR and EGF receptors. The compounds feature variable substituents (R1-R6, X, Y, Z) that can be adjusted to tune receptor binding affinity and biological activity, thereby improving therapeutic effectiveness while maintaining receptor modulation capability

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite molecular structures combining multiple functional groups and structural elements (aromatic rings, alkyl chains, amide groups, heteroatoms) within single compounds. These composite structures enable simultaneous interaction with multiple receptor targets (PPARα, PPARγ, EGF receptors), providing both therapeutic effectiveness and versatile receptor modulation in a unified molecular entity

Inventive Principle:
Principle #40Composite materials

2Object-generated harmful factors

If molecules that modulate PPAR and EGF receptors are developed, then therapeutic benefits in treating cancer and inflammatory conditions are achieved, but specific therapeutic agents that induce desired cellular responses are still lacking

Engineering Contradiction:
Improvecellular proliferation and inflammationVSAvoidapoptosis induction and anti-inflammatory activity
Core Design Contradiction:
Object-generated harmful factorsVSReliability

Solution Approach 1:

The patent applies preliminary anti-action by designing compounds that preemptively block pathological cellular processes. The molecules are structured to prevent excessive cellular proliferation and inflammatory responses before they progress to disease states. The compounds achieve this by预先 binding to and modulating PPAR and EGF receptors, thereby preventing the harmful effects of uncontrolled cell growth and inflammation while reliably inducing apoptosis in tumor cells and reducing inflammatory activity

Inventive Principle:
Principle #9Preliminary anti-action

3Adaptability or versatility

If compounds specific to PPAR and EGF receptors are developed, then receptor modulation is achieved, but pharmaceutical compositions with therapeutically effective amounts need to be formulated

Engineering Contradiction:
Improvereceptor specificityVSAvoidpharmaceutical formulation
Core Design Contradiction:
Adaptability or versatilityVSEase of manufacture

Solution Approach 1:

The patent applies universality by designing compounds that can serve multiple functions simultaneously: they act as PPAR modulators, EGF receptor modulators, anti-cancer agents, and anti-inflammatory agents. This multi-functionality reduces the need for separate formulations for different indications, simplifying pharmaceutical manufacturing while maintaining high receptor specificity. The same compound can be formulated into various dosage forms (tablets, capsules, injections) for different therapeutic applications

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentEP3744398A1Alkylamido compounds and uses thereof
Publication Date: 2020.12.02 NOGRA PHARMA LTD
  • EP3744398A1 patent drawingFigure 1~2
  • EP3744398A1 patent drawingFigure 3~4
  • EP3744398A1 patent drawingFigure 5

AI summary

Disclosed herein are compounds that may be specific to PPAR and/or EGF receptors, and methods of making and using same.