1,3-Dioxane Carboxylic Acids for Metabolic Disorder Treatment

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Solution Overview

Problem

Current treatments for hyperlipidemia, diabetes, and obesity often come with side effects such as hypoglycemia, liver toxicity, and tumor-inducing potential, necessitating a safer and more effective drug that can manage insulin resistance and hyperlipidemia without severe adverse effects.

Innovation Solution

Development of novel substituted 1,3-dioxane carboxylic acids and their derivatives, which act as hypocholesterolemic, hypolipidemic, and antihyperglycemic agents, potentially offering additional weight-lowering effects and improved treatment outcomes for Syndrome X, atherosclerosis, and related metabolic disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for hyperlipidemia and diabetes are used, then blood glucose and lipid levels are lowered, but severe side effects such as hypoglycemia, liver toxicity, and tumor-inducing potential occur

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

Solution Approach 1:

The patent applies parameter changes by developing novel substituted 1,3-dioxane carboxylic acid derivatives with modified chemical structures and properties. These compounds represent a new class of PPAR agonists with altered molecular parameters that achieve therapeutic effects while reducing adverse reactions compared to existing drugs

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention employs composite material principles by creating dual PPAR alpha and gamma agonists that combine the beneficial effects of both receptor activations. This composite approach allows simultaneous improvement of lipid metabolism and glucose control with enhanced safety profile

Inventive Principle:
Principle #40Composite materials

2Reliability

If higher dosages are used to achieve better treatment outcomes, then metabolic parameters are improved, but side effects increase

Engineering Contradiction:
Improvetreatment efficacyVSAvoidadverse reactions
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent utilizes parameter changes by optimizing the chemical structure of 1,3-dioxane carboxylic acid derivatives to achieve high potency at lower dosages. The modified molecular parameters enable effective PPAR activation with reduced drug concentrations, thereby improving efficacy while minimizing dose-dependent side effects

Inventive Principle:
Principle #35Parameter changes

3Reliability

If conventional drug therapies are administered, then insulin resistance and hyperlipidemia are managed, but liver toxicity and tumor-inducing potential arise

Engineering Contradiction:
Improvemetabolic controlVSAvoidhepatic and oncogenic risks
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies the extraction principle by isolating and optimizing specific molecular features of PPAR agonists that provide metabolic benefits while removing or minimizing structural elements associated with hepatotoxicity and tumorigenicity. This selective extraction creates safer therapeutic agents

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention employs short-acting or reversible binding characteristics in the 1,3-dioxane derivatives, allowing controlled PPAR activation that can be quickly terminated if adverse effects occur, providing a safety mechanism against cumulative toxicity

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Data Source

PatentEP1989192B11,3-dioxane carboxylic acids
Publication Date: 2009.07.22 ZYDUS LIFESCIENCES LTD
  • EP1989192B1 patent drawing
  • EP1989192B1 patent drawing
  • EP1989192B1 patent drawing

AI summary

The present invention relates to novel 1,3-dioxane carboxylic acids of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.