HETEROARYL SUCCINAMIDES AND THEIR USE AS METALLOPROTEINASE INHIBITORS

摘要

Heteroaryl succinamide derivatives of formula (I), and their salts, solvates and prodrugs, are new. X = single bond or optionally unsaturated 1-6C chain where one or more C may be replaced by O or S and one or more H may be replaced by F; Y = single bond, CH(OH) or C(O); R1 = H, alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R2 = as R1 or C(O)R10; R10 = as R1 or O-aryl, O-alkyl or NR11R12; R11 = as R1 or O-alkyl; R12 = as R1; or NR11R12 = heteroaryl or heterocycloalkyl; R3 = as R1 or NR11R12 or OR11; or R2+R3 with attached atoms = cycloalkyl or heterocycloalkyl; R4 = H or any suitable organic moiety; R5 = C(O)NHOH, C(O)OR13, SH, N(OH)CHO, SC(O)R14, P(O)(OH)R15 or P(O)(OH)OR13; R13 = H, alkyl or aryl; R14 = alkyl or aryl; R15 = aryl; and Het = 5 membered heteroaryl including 1-3 O, S and/or N.