Xanthine Compounds for Uric Acid Reduction and Inflammation Control

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Solution Overview

Problem

Current treatments for gout and hyperuricemia are limited in efficacy and are associated with adverse side effects, and there is a need for new agents that can effectively reduce uric acid levels and alleviate inflammation.

Innovation Solution

A class of xanthine compounds, specifically compounds of formula (I) and their pharmaceutically acceptable salts or solvates, are used to reduce uric acid levels and inhibit inflammation, thereby treating or preventing hyperuricemia, gout, gouty inflammations, pain, and uric acid nephropathy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing treatments for gout and hyperuricemia are used, then uric acid levels can be reduced, but adverse side effects occur and efficacy is limited

Engineering Contradiction:
ImproveefficacyVSAvoidadverse side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces a new class of compounds with modified chemical structures (formula I with specific R1, R2, R3 substituents) that change the pharmacological parameters of uric acid reduction. These structural modifications enable the compounds to achieve better efficacy and safety profiles compared to existing treatments by altering how they interact with target enzymes involved in uric acid metabolism

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent describes compounds that combine multiple functional groups and structural elements (xanthine core with various substituents) to create molecules with optimized properties. This composite molecular structure allows simultaneous achievement of high uric acid reduction efficacy and reduced adverse effects through coordinated action of different molecular components

Inventive Principle:
Principle #40Composite materials

2Productivity

If uric acid levels are reduced rapidly, then gout symptoms improve, but crystal movement and inflammation may be triggered

Engineering Contradiction:
Improverate of uric acid reductionVSAvoidinflammatory response
Core Design Contradiction:
ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent's compounds appear to enable controlled, gradual reduction of uric acid levels rather than abrupt changes. This periodic or progressive action allows the body to adapt to changing uric acid levels without triggering crystal movement and subsequent inflammatory responses, while still achieving effective gout management over time

Inventive Principle:
Principle #19Periodic action

Solution Approach 2:

The compounds may act to cushion or buffer the physiological impact of uric acid level changes. By providing this protective effect, the compounds prevent the harmful consequences (inflammation, crystal movement) that typically accompany rapid uric acid reduction, allowing for more aggressive and effective treatment

Inventive Principle:
Principle #11Beforehand cushioning (Prior cushioning)

Data Source

PatentEP3251675B1Prevention or treatment of uric acid or gout disease
Publication Date: 2021.04.21 SHANTON PHARMA PTE LTD
  • EP3251675B1 patent drawing
  • EP3251675B1 patent drawing
  • EP3251675B1 patent drawing

AI summary

The present invention relates to the use of a compound of formula (I), a pharmaceutically acceptable salt thereof, a solvate thereof, or a pharmaceutical composition containing the same in reducing uric acid level, preventing or reducing inflammations, and preventing or treating uratic or gouty diseases. In particular, the present invention relates to the use of a compound of formula (I), a pharmaceutically acceptable salt thereof, a solvate thereof, or a pharmaceutical composition containing the same in the manufacture of a medicament for the treatment or prevention of hyperuricemia, gout, gouty inflammations, pain and uric acid nephropathy. R1 represents hydrogen, C1-4 alkyl or the like. R2 represents C1-10 alkyl or the like. R3 represents halogen or the like.