GPR119 Modulators for Glucose-Dependent Insulin Secretion

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Solution Overview

Problem

Current therapies for treating diabetes and obesity, particularly Type II diabetes, are inadequate as they either fail to normalize blood glucose levels or carry risks of hypoglycemia, and there is a need for glucose-dependent action mechanisms that effectively modulate GPR119 activity to manage metabolic disorders.

Innovation Solution

Development of novel compounds that modulate GPR119 activity, specifically represented by compounds of Formula I, which are used in pharmaceutical compositions to treat diseases associated with GPR119, including diabetes and obesity, by enhancing insulin secretion and regulating metabolic pathways.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If current therapies for treating diabetes and obesity are used, then blood glucose levels may be reduced, but hypoglycemia risk increases and glucose-dependent action is lacking

Engineering Contradiction:
Improveblood glucose level controlVSAvoidhypoglycemia risk
Core Design Contradiction:
Measurement precisionVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by developing GPR119 modulators that alter the physiological response parameters - specifically inducing glucose-dependent insulin secretion where insulin release occurs only in the presence of glucose, thereby maintaining safe blood glucose levels without causing hypoglycemia. This changes the fundamental parameter of glucose responsiveness in the therapeutic mechanism.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If conventional diabetes treatments are administered, then insulin secretion may be stimulated, but the action is not glucose-dependent leading to unsafe glucose reduction

Engineering Contradiction:
Improveinsulin secretion efficiencyVSAvoidglucose-dependent action
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent implements feedback control through GPR119 modulation, where the insulin secretion response is feedback-regulated by glucose levels. The modulator activates GPR119 receptors that sense glucose presence, creating a feedback loop that stimulates insulin secretion only when glucose is elevated, ensuring reliable glucose-dependent action and preventing hypoglycemia.

Inventive Principle:
Principle #23Feedback

Data Source

PatentEP2134704B1Compounds and compositions as modulators of GPR119 activity
Publication Date: 2010.09.22 IRM
  • EP2134704B1 patent drawing
  • EP2134704B1 patent drawing
  • EP2134704B1 patent drawing

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.