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 --(CR.sup.4R.sup.5).sub.m-- wherein m is an
integer 1 or 2; R.sup.4 and R.sup.5 are each independently from each
other hydrogen or C.sub.1-4alkyl; R.sup.1 is C.sub.1-6alkylcarbonyl
optionally substituted with hydroxy; C.sub.1-6alkyloxycarbonyl;
aminoC.sub.1-6alkylcarbonyl wherein the C.sub.1-6alkyl group is
optionally substituted with C.sub.3-6cycloalkyl; mono- and
di(C.sub.1-4alkyl)aminoC.sub.1-6alkylcarbonyl; aminocarbonyl substituted
with aryl; C.sub.1-6alkylcarbonyloxyC.sub.1-6alkylcarbonyl;
C.sub.1-6alkyloxycarbonylaminoC.sub.1-6alkylcarbonyl wherein the amino
group is optionally substituted with C.sub.1-4alkyl; an amino acid;
C.sub.1-6alkyl substituted with amino; or arylcarbonyl; R.sup.2 is an
optionally substituted 5-membered heterocycle, or R.sup.2 is optionally
substituted benzimidazole; R.sup.3 is a bivalent radical
--CH.sub.2CH.sub.2-- optionally substituted with halo or phenylmethyl; or
R.sup.3 is a bivalent radical of formula