Tris(hydroxymethyl)aminomethane salts of a small-molecule glp1r agonist and pharmaceutical compositions and uses thereof

摘要

The disclosure relates to tris(hydroxymethyl)aminomethane salts of a small-molecule GLP1R agonist (S)-3-(4’-cyano-biphenyl-4-yl)-2-{ [(3R,7S)-3-[4-(3,4-dichloro-benzyloxy)-phenyl]-1-methyl-2-oxo-6-((S)-1-phenyl-propyl)-2,3,5,6,7,8-hexahydro-1H-4-oxa-1,6-diaza-anthracene-7-carbonyl]-amino} -propionic acid. The disclosure further provides solid compositions comprising tris(hydroxymethyl)aminomethane salts of the small-molecule GLP1R agonist and their use for treating type 1 diabetes, type 2 diabetes, or obesity. Solid formulations further comprising an evaporation residue and a binder, such as hydroxy propyl methyl cellulose acetate succinate (HPMCAS), are also provided.