Pyrimidine Piperidine Compound for Glucose Metabolism Modulation

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Solution Overview

Problem

Current treatments for diabetes and obesity-related disorders, such as Type I and Type II diabetes, often fail to accurately normalize blood glucose levels and are associated with risks like hypoglycemia, and existing therapies do not effectively address insulin resistance and β-cell dysfunction.

Innovation Solution

The compound 4-[5-methyl-6-(2-methyl-pyridin-3-yloxy)-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester acts as a selective agonist for the RUP3 receptor, modulating glucose metabolism by enhancing insulin secretion and improving insulin sensitivity, thereby reducing blood glucose levels and promoting weight management.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If current treatments for diabetes are used, then blood glucose levels can be reduced, but hypoglycemia risk increases and insulin resistance is not effectively addressed

Engineering Contradiction:
Improveblood glucose normalization accuracyVSAvoidhypoglycemia risk
Core Design Contradiction:
Measurement precisionVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by developing a novel chemical compound with a specific molecular structure (Formula I) that modifies the pharmacological parameters of glucose metabolism. The compound achieves better blood glucose control by altering the interaction between insulin and cellular receptors, thereby improving normalization accuracy while reducing hypoglycemia risk through optimized molecular properties.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention employs a composite molecular structure combining multiple functional groups (aromatic rings, heterocyclic moieties, and substituent patterns) that work synergistically. This composite structure enables the compound to simultaneously address multiple pathological mechanisms including insulin resistance and glucose homeostasis, while maintaining a safer therapeutic profile with reduced hypoglycemia risk.

Inventive Principle:
Principle #40Composite materials

2Reliability

If existing therapies are used, then some glucose control is achieved, but insulin resistance and β-cell dysfunction are not effectively addressed

Engineering Contradiction:
Improveinsulin resistance treatment efficacyVSAvoidmulti-mechanism action capability
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent implements universality by designing a multi-functional compound that simultaneously addresses insulin resistance, enhances β-cell function, and improves glucose metabolism. The molecular structure of Formula I is engineered to interact with multiple targets in the insulin signaling pathway, providing comprehensive treatment for diabetic pathophysiology rather than addressing single mechanisms.

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

Solution Approach 2:

The compound structure is segmented into distinct functional regions including aromatic rings, heterocyclic cores, and variable substituent groups (R1-R6). These segments can be independently optimized to target different aspects of insulin resistance and β-cell dysfunction, allowing the molecule to perform multiple therapeutic functions simultaneously with high reliability.

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP1931654B1Modulators of metabolism and the treatment of disorders related thereto
Publication Date: 2009.04.22 ARENA PHARMACEUTICALS INC
  • EP1931654B1 patent drawing
  • EP1931654B1 patent drawing
  • EP1931654B1 patent drawing

AI summary

The present invention relates to 4-[5-methyl-6-(2-methyl-pyridin-3-yloxy)-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester, pharmaceutically acceptable salts, solvates and hydrates thereof that are modulators of glucose metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.