Preparation of N- oxohexahydrofuropyrrole amino acid amides as cathepsin K inhibitors.

Abstract

Title compds. [I; 1 of R1, R2 = halo, the other = H, halo; R3 = (fluoro)alkyl; R4 = H; R3R4C = (substituted) spirocycloalkyl, heterocyclyl; R5 = H, Me; E = CO, SOm, NR5SOm, NR5CO, CO2; R6 = stable (substituted) mono- or bicyclic carbocyclyl, heterocyclyl; m = 0-2], were prepd. Thus, title compd. (II) (multistep prepn. given) inhibited cathepsin K with Ki = 5.3 nM. [on SciFinder(R)]