Imidazobenzazepine derivatives as DGAT-1 inhibitors and their preparation and use for the treatment of diabetes and obesity

Abstract

The invention relates to imidazobenzazepine derivs. of formula I, which are diacylglycerol acyltransferase 1 (DGAT-1) inhibitors and which are useful in the treatment of diabetes and obesity. Compds. of formula I wherein R1 is H, F, Cl, CF3, etc.; R2 is H and Me; R3 is H and Me; provided that at least one of R2 and R3 is H; A is (CH2)1-3; and pharmaceutically acceptable salts thereof, are claimed. Example compd. II was prepd. by amidation of 1-[(4-chlorobenzoyl)amino]cyclopropanecarboxylic acid with (4R)-5,6-dihydro-4H-imidazo[1,2-a][1]benzazepin-4-amine. All the invention compds. were evaluated for their DGAT-1 inhibitory activity. From the assay, it was detd. that compd. II exhibited an IC50 value of 89.0±0.98 nM.