Bicyclic Heterocycle Derivatives GPR119 Modulation

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Solution Overview

Problem

Current small molecule modulators for GPR119 receptor have limitations in efficacy and safety for treating metabolic disorders and obesity-related conditions, necessitating the development of improved compounds.

Innovation Solution

Development of Bicyclic Heterocycle Derivatives, specifically compounds of Formula (I), which are designed to modulate GPR119 receptors, offering enhanced therapeutic effects for obesity, diabetes, and cardiovascular diseases by administering effective amounts of these derivatives or their pharmaceutically acceptable salts, solvates, esters, or prodrugs.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current small molecule modulators are used for GPR119 receptor, then the treatment can be administered, but the efficacy and safety are limited

Engineering Contradiction:

Improveefficacy and safetyVSAvoidtherapeutic effectiveness for metabolic disorders

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by systematically modifying the chemical structure of small molecule modulators through varying substituents (R1-R8), ring systems (J, K, L), and molecular weight parameters to optimize both efficacy and safety profiles for GPR119 receptor treatment

Inventive Principle:

Principle #35Parameter changes

2Reliability

If existing GPR119 modulators are used, then metabolic disorders can be treated, but the therapeutic effects are insufficient

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidlimitations in efficacy

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent employs composite materials by creating bicyclic heterocycle derivatives that combine multiple structural elements (aromatic rings, heteroatoms, substituent groups) to achieve enhanced therapeutic effects and overcome the limitations of existing single-structure modulators

Inventive Principle:

Principle #40Composite materials

Data Source

PatentUS8410122B2Bicyclic heterocycle derivatives and methods of use thereof

Publication Date: 2013.04.02 MERCK SHARP & DOHME LLC

AI summary

The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.