Tripeptidyl peptidase inhibitors

摘要

The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds. wherein n is an integer 0 or 1; X represents O; S; or -(CR⁴R⁵)_m- wherein m is an integer 1 or 2; R⁴ and R⁵ are each independently from each other hydrogen or C_1-4alkyl; R¹ is C_1-6alkylcarbonyl optionally substituted with hydroxy; C_1-6alkyloxycarbonyl; aminoC_1-6alkylcarbonyl wherein the C_1-6alkyl group is optionally substituted with C_3-6cycloalkyl; mono- and di(C_1-4alkyl)aminoC_1-6alkylcarbonyl; aminocarbonyl substituted with aryl; C_1-6alkylcarbonyloxyC_1-6alkylcarbonyl; C_1-6alkyloxycarbonylaminoC_1-6alkylcarbonyl wherein the amino group is optionally substituted with C_1-4alkyl; an amino acid; C_1-6alkyl substituted with amino; or arylcarbonyl; R² is an optionally substituted 5-membered heterocycle, or R² is optionally substituted benzimidazole; R³ is a bivalent radical -CH₂CH₂- optionally substituted with halo or phenylmethyl; or R³ is a bivalent radical of formula