GPR119 Modulators for Glucose-Dependent Insulin Release
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current treatments for diabetes and obesity lack effective glucose-dependent insulin release mechanisms and often induce hypoglycemia, while existing therapies for metabolic disorders are not fully effective in addressing interconnected disease states.
Innovation Solution
Development of compounds that modulate GPR119 activity to stimulate insulin release and regulate metabolic processes, including the use of GPR119 agonists to enhance glucose signaling, promote β-cell proliferation, and reduce hunger, thereby treating diabetes and obesity-related disorders.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If current treatments for diabetes and obesity are used, then insulin release is stimulated, but hypoglycemia is induced
Solution Approach 1:
The patent applies parameter changes by developing GPR119 modulators with specific molecular structures (formula I compounds) that alter the physiological parameters of glucose signaling and insulin release. These compounds change the binding affinity and activation characteristics of the GPR119 receptor, enabling insulin secretion that is tightly coupled to glucose levels rather than causing indiscriminate hypoglycemia. The structural modifications in the compound formulas allow for selective activation that maintains glucose-dependent insulin release.
2Reliability
If existing therapies for metabolic disorders are used, then some symptoms are treated, but interconnected disease states are not fully addressed
Solution Approach 1:
The patent applies universality by developing GPR119 modulators that simultaneously address multiple metabolic disorders through a single therapeutic mechanism. Since GPR119 is expressed in pancreatic beta cells, adipose tissue, and the brain, activating this single receptor pathway produces multi-effect outcomes: improving insulin secretion, regulating lipid metabolism, controlling appetite, and enhancing beta-cell survival. This multi-functional approach treats interconnected disease states including type 2 diabetes, obesity, and dyslipidemia concurrently.
3Use of energy by moving object
If GPR119 agonists are used to stimulate insulin release, then glucose signaling is enhanced, but the risk of hypoglycemia increases
Solution Approach 1:
The patent applies feedback mechanisms by designing GPR119 modulators that enhance glucose signaling in a glucose-dependent manner. The compounds activate GPR119 receptors on pancreatic beta cells, which then amplify the physiological response to elevated blood glucose levels. This creates a feedback loop where insulin release is stimulated only when glucose levels are high, and ceases when glucose returns to normal, preventing hypoglycemia. The feedback control is inherent in the glucose-sensing mechanism that the GPR119 agonists enhance.
Data Source
AI summary
The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.