Dipeptidyl Ketoamide Compounds Reduce Adipose Triglyceride Accumulation

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Solution Overview

Problem

Current treatments for obesity and obesity-related conditions, such as lipid storage disease and hyperlipemia, are inadequate due to side effects from existing drugs, and there is a need for more effective methods to control weight gain and reduce triglyceride accumulation in adipose tissue.

Innovation Solution

The use of dipeptidyl ketoamide compounds, specifically compounds of formula (I) and (II), which reduce adipogenesis and triglyceride deposition in adipocytes, thereby preventing triglyceride accumulation in adipose tissue, offering a potential treatment for obesity and related conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing drugs are used to treat obesity and obesity-related conditions, then weight control and triglyceride reduction are achieved, but adverse side effects occur

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidadverse side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by developing new chemical compounds with modified molecular structures (dipeptidyl ketoamide compounds with specific formula I and II) that change the pharmacological parameters of the treatment. This structural modification aims to achieve the desired therapeutic effect while altering the side effect profile compared to existing drugs.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by creating complex dipeptidyl ketoamide compounds that combine multiple functional groups and structural elements (including ketoamide moieties, specific amino acid derivatives, and various substituent patterns) to achieve both efficacy and reduced toxicity.

Inventive Principle:
Principle #40Composite materials

2Reliability

If more effective methods are developed to control weight gain and reduce triglyceride accumulation, then treatment efficacy is improved, but treatment complexity may increase

Engineering Contradiction:
Improvetreatment efficacyVSAvoidtreatment complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies the extraction principle by isolating and optimizing the key pharmacophore elements responsible for anti-obesity activity. The dipeptidyl ketoamide structure represents an extracted and refined active component that targets specific pathways (such as adipogenesis and triglyceride metabolism) to achieve efficacy with potentially simpler pharmacological action compared to multi-target drugs.

Inventive Principle:
Principle #2Taking out (Extraction)

3Quantity of substance

If dipeptidyl ketoamide compounds are used to reduce adipogenesis and triglyceride deposition, then triglyceride accumulation is reduced, but the mechanism of action requires precise molecular targeting

Engineering Contradiction:
Improvetriglyceride accumulationVSAvoidmolecular targeting precision
Core Design Contradiction:
Quantity of substanceVSManufacturing precision

Solution Approach 1:

The patent applies local quality by designing compounds with specific local structural features (such as the ketoamide group at specific positions, particular amino acid residues, and defined stereochemistry) that enable precise interaction with target molecules in adipose tissue. This localized structural optimization ensures specific binding to targets involved in adipogenesis and triglyceride metabolism.

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS10294269B2Dipeptidyl ketoamide compounds and their use for the treatment and/or prevention of fat accumulation
Publication Date: 2019.05.21 LANDSTEINER GENMED SL
  • US10294269B2 patent drawing
  • US10294269B2 patent drawing
  • US10294269B2 patent drawing

AI summary

The present invention relates to the use of dipeptidyl ketoamide compounds for preventing accumulation of triglycerides in adipose tissue or for reducing the amount of triglycerides in adipose tissue in a subject in need thereof and to novel dipeptidyl ketoamide compounds.