Substituted Triazole Compounds for Uric Acid Control

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Solution Overview

Problem

Current treatments for conditions associated with abnormal uric acid levels, such as gout and hyperuricaemia, are inadequate in effectively managing uric acid levels and associated symptoms.

Innovation Solution

Administration of specific compounds, including those of formulas (I), (II), and (III), or their metabolites, pharmaceutically acceptable salts, solvates, polymorphs, esters, tautomers, or prodrugs, to decrease uric acid levels, increase excretion, or both, thereby treating conditions like gout, hyperuricaemia, and related disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for gout and hyperuricaemia are used, then some symptom management is achieved, but uric acid levels are not effectively controlled

Engineering Contradiction:
Improveuric acid level controlVSAvoidabnormal uric acid levels
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of existing uric acid lowering compounds. Specifically, it introduces substituted naphthalenyl and heteroaryl groups at the 4-position of the triazole ring, creating new derivatives with potentially improved pharmacological properties. This structural modification approach aims to enhance the reliability of uric acid level control while maintaining the core mechanism of action.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials principles by combining different chemical moieties into single molecular structures. The compounds feature fused ring systems (naphthalenyl, heteroaryl) integrated with triazole cores and additional functional groups, creating complex composite molecular architectures that may simultaneously target multiple aspects of uric acid metabolism and provide enhanced therapeutic effects.

Inventive Principle:
Principle #40Composite materials

2Object-generated harmful factors

If uric acid levels are decreased through medication, then hyperuricaemia symptoms are alleviated, but treatment complexity increases

Engineering Contradiction:
Improvehyperuricaemia symptomsVSAvoidtreatment regimen
Core Design Contradiction:
Object-generated harmful factorsVSDevice complexity

Solution Approach 1:

The patent applies universality by designing compounds that may perform multiple functions simultaneously. The substituted triazole compounds are intended to lower uric acid levels while also addressing associated inflammatory responses and potentially preventing tophi formation. This multi-functional approach aims to reduce treatment complexity by consolidating multiple therapeutic effects into single agents.

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

Solution Approach 2:

The patent uses intermediary principles by introducing specific chemical substituents (naphthalenyl, heteroaryl groups) that act as mediators between the core triazole structure and biological targets. These intermediary groups may enhance drug-receptor interactions, improve pharmacokinetic properties, and facilitate more effective uric acid lowering with reduced side effects, thereby simplifying the overall treatment approach.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS10183012B2Compounds and compositions and methods of use
Publication Date: 2019.01.22 ARDEA BIOSCIENCES INC
  • US10183012B2 patent drawing
  • US10183012B2 patent drawing
  • US10183012B2 patent drawing

AI summary

Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.