Triazole Ghrelin Receptor Agonists With High Binding Specificity

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current treatments for diseases mediated by the ghrelin receptor lack compounds that bind with high specificity, leading to inefficiencies and potential side effects.

Innovation Solution

Development of triazole-based compounds that strongly bind to the ghrelin receptor, serving as agonists to modulate its activity and treat associated diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional compounds are used for treating diseases mediated by the ghrelin receptor, then treatment can be provided, but the compounds lack high binding specificity leading to inefficiencies and side effects

Engineering Contradiction:
Improvebinding specificityVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure parameters of ghrelin receptor ligands. Specifically, it uses triazole ring structures with various substituents (R1-H, R2-OH, R3-H, R4-alkyl groups with 1-15 carbons) to optimize binding affinity and specificity. The systematic variation of molecular parameters (functional groups, chain lengths, positions) enables high-specificity binding to the ghrelin receptor while reducing off-target effects and side effects.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If conventional compounds are used for treating diseases mediated by the ghrelin receptor, then treatment can be provided, but binding force is insufficient leading to treatment inefficiency

Engineering Contradiction:
Improvebinding forceVSAvoidtreatment efficiency
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent employs composite material principles by designing complex triazole-based molecular structures that combine multiple functional elements. The compounds feature a central triazole ring (1H-1,2,3-triazol-4-yl) composite structure with various alkyl substituents (C1-C15 straight or branched chain alkyl groups) and hydroxyl groups. This composite molecular architecture enables strong, specific binding to the ghrelin receptor, significantly improving binding force and consequently treatment efficiency for diseases such as obesity, gastrointestinal disorders, and cardiovascular conditions.

Inventive Principle:
Principle #40Composite materials

Data Source

PatentUS12570617B2Use of triazole compound as ghrelin receptor agonist
Publication Date: 2026.03.10 KYUNGPOOK NAT UNIV IND ACADEMIC COOP FOUND
  • US12570617B2 patent drawing
  • US12570617B2 patent drawing
  • US12570617B2 patent drawing

AI summary

The present invention relates to a use of a triazole compound as a ghrelin receptor agonist and, more specifically, to a composition for preventing or treating diseases mediated by the ghrelin receptor, the composition being of a triazole compound which strongly binds to the ghrelin receptor with very high specificity. The compound provided by the present invention exhibits a strong binding force to the ghrelin receptor with very high specificity, and thus may be very usefully employed for preventing or developing a therapeutic agent for diseases mediated by the ghrelin receptor.