Invention Grant
US07947713B2 Tripeptidyl peptidase inhibitors 有权
三肽基肽酶抑制剂

Tripeptidyl peptidase inhibitors
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; R4 and R5 are each independently from each other hydrogen or C1-4alkyl; R1 is 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; 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.
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