Tripeptidyl peptidase inhibitors

Details Tripeptidyl peptidase inhibitors Tripeptidyl peptidase inhibitors

2006-10-24

2006-10-24

Shameem, Golam M. M. (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C514S310000, C546S143000, C546S144000

Reexamination Certificate

active

07125891

ABSTRACT:
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; R4and R5are each independently from each other hydrogen or C1-4alkyl; R1is C1-6alkylcarbonyl optionally substituted with hydroxy; C1-6alkyloxycarbonyl; aminoC1-6alkylcarbonyl wherein the C1-6alkyl group is optionally substituted with C3-6cycloalkyl; mono- and di(C1-4alkyl)aminoC1-6alkylcarbonyl; aminocarbonyl substituted with aryl; C1-6alkylcarbonyloxyC1-6alkylcarbonyl; C1-6alkyloxycarbonylaminoC1-6alkylcarbonyl wherein the amino group is optionally substituted with C1-4alkyl; an amino acid; C1-6alkyl substituted with amino; or arylcarbonyl; R2is an optionally substituted 5-membered heterocycle, or R2is optionally substituted benzimidazole; R3is a bivalent radical —CH2CH2— optionally substituted with halo or phenylmethyl; or R3is a bivalent radical of formula

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