Multi-Fused Ring GLP-1 Agonists for Oral Diabetes Treatment
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Solution Overview
Problem
Current GLP-1 analogs for treating diabetes require subcutaneous injection, leading to poor patient compliance due to inconvenience, necessitating the development of non-polypeptide small-molecule agonists that can target the GLP-1 receptor effectively.
Innovation Solution
Development of a compound with a polycyclic fused ring structure, its stereoisomers, or pharmaceutically acceptable salts, designed to act as GLP-1 receptor agonists, potentially offering an oral administration option for diabetes and obesity treatment.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If GLP-1 analogs are administered via subcutaneous injection, then therapeutic efficacy is improved, but patient compliance deteriorates due to inconvenience
Solution Approach 1:
The patent changes the fundamental parameter of molecular structure from polypeptide to small molecule, enabling a transition from injection to oral administration. This structural parameter change allows the compound to achieve both oral bioavailability and GLP-1 receptor agonist activity, resolving the contradiction between therapeutic efficacy and ease of administration
2Ease of operation
If non-polypeptide small-molecule agonists are developed, then ease of operation is improved by enabling oral administration, but reliability may deteriorate due to uncertain receptor binding efficacy
Solution Approach 1:
The patent applies local quality by introducing specific functional groups and structural features at key positions of the small molecule structure. The multi-fused ring structure with specific substituents creates localized interaction zones that mimic the binding characteristics of natural GLP-1, ensuring high receptor binding efficacy while maintaining oral administration capability
Solution Approach 2:
The patent employs composite structural design by combining multiple ring systems (benzene, pyridine, pyrimidine rings) with various substituents to create a composite small molecule structure. This composite approach integrates multiple functional elements that collectively achieve both oral bioavailability and potent GLP-1 receptor agonist activity
Data Source
AI summary
The present invention is in the field of pharmaceutical chemistry, and relates to a compound containing a multi-fused ring structure, specifically to a compound of formula (I), a stereoisomer or pharmaceutically acceptable salt thereof, a preparation method therefor, or a pharmaceutical composition thereof, and a use thereof in the preparation of a drug for treating diabetes or obesity-related diseases.