αvβ3 antagonists based on a central benzoic acid scaffold

A series of novel, highly potent α v β 3 antagonists based on a benzoic acid scaffold and containing an acylguanidine as an Arg-mimetic and sulfonamide side chains is described. The compounds are selective against the fibrinogen receptor α I I b β 3 and they are capable of inhibiting bone resorption in vivo in a TPTX model of osteoporosis. Therefore the compounds are promising drug substances for the treatment of osteoporosis.