Glucagon-like peptide 1 receptor agonists

Orally administered benzimidazole derivatives represented by Formula I address the need for GLP-1R agonists with a favorable toxicology and pharmacokinetic profile, enhancing insulin secretion and treating type II diabetes mellitus effectively.

AU2023377707B2Pending Publication Date: 2026-07-23ELI LILLY & CO
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Patent Information

Application Number
AU2023377707
Authority / Receiving Office
AU · AU
Patent Type
Applications
Current Assignee / Owner
Priority Date
2022-11-11
Filing Date
2023-11-06
Publication Date
2026-07-23

AI Technical Summary

Technical Problem

There is a need for alternative glucagon-like peptide-1 receptor (GLP-1R) agonists that can be orally administered, with a favorable toxicology profile and pharmacokinetic profile supporting once daily dosing, to treat type II diabetes mellitus, as existing injectable agents are inconvenient and can cause irritation.

Method used

Development of compounds represented by Formula I, including various substituted benzimidazole derivatives, which can be orally administered, providing effective GLP-1R agonism with a favorable toxicology and pharmacokinetic profile.

Benefits of technology

The compounds effectively enhance insulin secretion and treat type II diabetes mellitus, offering a convenient oral administration option with a favorable safety and efficacy profile, suitable for once daily dosing.

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Abstract

In an embodiment, the present invention provides a compound of the formula: or a pharmaceutically acceptable salt thereof, and methods of using this compound for treating type II diabetes mellitus.
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Citation Information

Patent Citations

  • GLP-1 receptor agonist and application thereof in medicine

    CN114763352A

  • GLP-1 receptor agonist

    WO2021112538A1

  • Macrocyclic glucagon-like peptide 1 receptor agonists

    WO2022246019A1