Heterocyclic GLP-1 agonists
Inventors
Meng, Qinghua • Jennings, Andrew • Lei, Hui • Lin, Xichen
Assignees
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Publication Number
US-12552791-B2
Publication Date
2026-02-17
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 invention discloses heterocyclic compounds of Formula I, or pharmaceutically acceptable salts or solvates thereof, which function as GLP-1 agonists. The claim defines structural alternatives for core atoms, linkers L1 and L2, and Rings A, B, and C. Specific structural elements include a carboxylic acid group at T1, a methylene group at L1, a bond at L2, and a phenyl Ring C. Disclosed examples characterize imidazo[4,5-b]pyridine-5-carboxylic acid and benzimidazole-6-carboxylic acid embodiments.
The disclosure encompasses subformulae IB through IE, stereochemical variants, and pharmaceutical compositions comprising a pharmaceutically acceptable excipient. Disclosed therapeutic applications address GLP-1-associated conditions, type 2 diabetes mellitus, obesity, and metabolic disorders through oral administration or combination therapy. Reported treatments involve the modulation of glucose, insulin, glucagon, and body weight. The technical problem addressed by the invention is not explicitly described in patent.
Claims Coverage
The provided claim information identifies one independent claim directed to compounds of Formula I, presenting one inventive feature.
Formula I compounds and pharmaceutically acceptable forms
Claim 1 covers a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, defining structural alternatives for core atoms, linkers L1 and L2, and Rings A, B, and C. The claim specifies T1 as C(=O)OH, L1 as CH2, L2 as a bond, Ring C as phenyl, and permitted ring heteroatoms, alkyl groups, halogens, and substituents.
The independent claim encompasses the defined Formula I compound genus and its pharmaceutically acceptable salts or solvates, while dependent claims relate to pharmaceutical compositions, oral administration, and methods for treating type 2 diabetes mellitus, obesity, and GLP-1-associated conditions.
Stated Advantages
The patent content identifies potential reductions in glucose, HbA1c, glucagon, and BMI.
The nonhuman-primate pharmacokinetic embodiments report improved oral exposure and bioavailability versus REF1.
In a nonhuman-primate glucose tolerance test, exemplary compounds induce robust insulin secretion and significantly enhance glucose clearance.
Documented Applications
Pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable excipient.
Treatment of type 2 diabetes mellitus, obesity, GLP-1-associated diseases and conditions, and associated metabolic disorders.
Therapeutic methods involving insulin or glucose modulation.
Oral administration and combination therapy options for the treatment of type 2 diabetes mellitus and associated conditions.
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