Formula I Compounds for Insulin Resistance and Metabolic Disorders

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Solution Overview

Problem

Current treatments for diabetes and insulin resistance syndrome are inadequate due to side effects and lack of effective oral therapeutic agents, and there is a need for safer and more effective treatments for fatty liver disease.

Innovation Solution

A biologically active compound of Formula I is used to treat insulin resistance syndrome, diabetes, cachexia, hyperlipidemia, fatty liver disease, obesity, atherosclerosis, or arteriosclerosis, administered in a pharmaceutical composition with a pharmaceutically acceptable carrier, demonstrating activity in animal models of diabetes and insulin resistance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing diabetes treatments (insulin releasers, biguanides, insulin sensitizers) are used, then glycemic control is improved, but side effects increase (hypoglycemia, liver toxicity, weight gain)

Engineering Contradiction:
Improveglycemic controlVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by developing a novel chemical compound structure (Formula I) with specific molecular characteristics that differ from existing diabetes medications. The compound features a core structure with variable substituents (R1-R6, R8-R15) that can be modified to optimize therapeutic efficacy while minimizing side effects. This structural parameter change enables improved glycemic control through a different mechanism of action that avoids the harmful effects of current treatments.

Inventive Principle:
Principle #35Parameter changes

2Ease of operation

If orally active therapeutic agents are developed, then treatment convenience is improved, but safety and efficacy are compromised

Engineering Contradiction:
Improveoral administrationVSAvoidsafety and efficacy
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent employs composite material principles by creating a complex molecular structure that combines multiple functional groups and substituents in a specific arrangement. The compound of Formula I integrates various chemical moieties that work synergistically to achieve both oral bioavailability and therapeutic efficacy. This composite structural approach allows the molecule to undergo appropriate metabolic processing while maintaining effectiveness in treating insulin resistance and related conditions.

Inventive Principle:
Principle #40Composite materials

3Reliability

If insulin sensitizers (thiazolidinedione derivatives) are used, then peripheral insulin responsiveness is improved, but adverse effects increase (weight gain, edema, liver toxicity)

Engineering Contradiction:
Improveinsulin responsivenessVSAvoidweight gain, edema, liver toxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies copying principles by designing a new chemical scaffold that replicates the desired pharmacological effect of insulin sensitizers without copying their harmful side effect profile. The compound of Formula I represents a novel structural copy that achieves peripheral insulin sensitization through a different molecular architecture, thereby avoiding the weight gain, edema, and liver toxicity associated with thiazolidinedione derivatives while maintaining the beneficial effect of improved insulin responsiveness.

Inventive Principle:
Principle #26Copying

Data Source

PatentUS7906675B2Compounds for the treatment of metabolic disorders
Publication Date: 2011.03.15 PHARMA CINQ LLC
  • US7906675B2 patent drawing
  • US7906675B2 patent drawing
  • US7906675B2 patent drawing

AI summary

A biologically active agent, wherein the agent is a compound of the formula:Wherein A, R5, R9, X, Q and n, m, q are defined herein below.