Four-Cycle Carboxylic Acid Derivatives as GLP-1 Receptor Modulators
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Solution Overview
Problem
Current treatments for diabetes, particularly type I and type II, lack effective modulators or potentiators of the glucagon-like peptide 1 (GLP-1) receptor, which are essential for managing blood glucose levels and preserving pancreatic beta cells.
Innovation Solution
Development of compounds with specific structures, such as those represented by Formula I-R and I-S, that act as potentiators or modulators of the GLP-1 receptor, including pharmaceutical compositions and methods for their synthesis and use in treating metabolic disorders like diabetes.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current diabetes treatments are used, then existing therapeutic options are available, but effective GLP-1 receptor modulators or potentiators are lacking
Solution Approach 1:
The patent segments the GLP-1 receptor modulation function into distinct compound classes (Formula I-R and I-S) with specific structural features, allowing for targeted development of modulators with different properties and mechanisms of action
Solution Approach 2:
The patent systematically varies chemical parameters (substituents R1-R7, ring structures A-C, linkers L1-L3) to create a library of compounds with optimized binding affinity, selectivity, and pharmacological properties for GLP-1 receptor modulation
2Adaptability or versatility
If non-peptide GLP-1 receptor modulator compounds are developed, then new therapeutic agents are created, but synthesis complexity increases
Solution Approach 1:
The patent divides the complex molecule into modular components (core structure with rings A-B, substituent groups R1-R7, and optional linkers L1-L3), allowing independent optimization and simplified synthesis of each module before assembly
Solution Approach 2:
The patent provides systematic guidance for modifying chemical parameters (different ring sizes for A-B, various substituent types for R1-R7, optional linkers L1-L3) to achieve desired pharmacological properties while maintaining synthetic feasibility
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
These compounds effectively activate or potentiate the GLP-1 receptor, providing therapeutic benefits for conditions such as type I and type II diabetes, gestational diabetes, obesity, and metabolic disorders by enhancing glucose-stimulated insulin secretion and preserving pancreatic beta cells.
Implementation Method 1
These compounds effectively activate or potentiate the GLP-1 receptor, providing therapeutic benefits for conditions such as type I and type II diabetes, gestational diabetes, obesity, and metabolic disorders by enhancing glucose-stimulated insulin secretion
Data Source
AI summary
The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where"﹋" represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.