Heterocyclic GLP-1 agonists
Inventors
Meng, Qinghua • Lei, Hui • Zhang, Haizhen • Lin, Xichen • Jennings, Andrew
Assignees
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Publication Number
US-12528781-B2
Publication Date
2026-01-20
Expiration Date
Abstract
This disclosure relates to GLP-1 agonists of Formula I: including pharmaceutically acceptable salts and solvates thereof, and pharmaceutical compositions including the same.
Core Innovation
The disclosure concerns heterocyclic GLP-1 receptor agonists of Formula I, compound subgenera Formulae (I-A5)–(I-A8) and Formula (I-B2), and related scaffolds with carboxylic-acid or bioisostere groups. These chemical entities feature piperidine-linked pyridine, benzodioxole, or aromatic cores with varied imidazole, triazole, oxadiazole, or tetrazole motifs, alongside acrylic-acid and propanoic-acid side chains. The structures encompass diverse N-substituents comprising heteroaryl, aryl, cyclic ether, sulfone, and fluorinated moieties.
The described series encompasses structural variants, stereoisomers, and specific enumerated compounds, with claim 1 covering selected compounds and their pharmaceutically acceptable salts or solvates. The compounds demonstrate GLP-1 receptor agonist activity in cAMP-stimulation assays, with representative EC50 values, LC-MS data, and NMR spectra reported. Because abstract, summary, and background sections are largely omitted from the provided content, the specific technical problem addressed by the invention is not explicitly described in patent.
Claims Coverage
The claims identify independent claims comprising three inventive features across claim 1 and claims 4, 5, 7, 8, 10, 11, 13, 14, 16, 17, 19, and 20.
Selected compounds and their pharmaceutically acceptable salts or solvates
Claim 1 recites a compound selected from an enumerated or depicted group, or a pharmaceutically acceptable salt or solvate thereof, including substituted imidazole-, triazole-, or pyridine-containing scaffolds.
Compounds and their pharmaceutically acceptable salts
Claims 4, 7, 10, 13, 16, and 19 recite a compound defined by a structure in the claim, or a pharmaceutically acceptable salt thereof, wherein the structures are not rendered in the provided excerpts.
Compounds with unrendered structures
Claims 5, 8, 11, 14, 17, and 20 recite a compound, but the provided claim excerpts terminate before identifying the compound or rendering its chemical structure.
The independent claims cover specified compounds and additional compounds defined by structures absent from the provided claim excerpts, together with pharmaceutically acceptable salts and solvates.
Stated Advantages
The disclosed therapeutic effects include reduced glucose and glucagon and increased insulin.
Documented Applications
A pharmaceutical composition comprising a claim 1 compound, its pharmaceutically acceptable salt or solvate, and a pharmaceutically acceptable excipient.
Therapeutic use for the treatment of GLP-1-associated conditions, including type 2 diabetes mellitus and obesity, via oral administration and combination therapy.
Co-administration with anti-emetic agents and patient-identification criteria involving type 2 diabetes mellitus, HbA1c, fasting or non-fasting plasma glucose, and BMI.
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