Tripeptidyl peptidase inhibitors

Details Tripeptidyl peptidase inhibitors Tripeptidyl peptidase inhibitors

C - Chemistry, Metallurgy

07

D

C07D 403/04 (2006.01) A61K 31/4184 (2006.01) A61K 31/422 (2006.01) A61K 31/47 (2006.01) C07D 217/26 (2006.01) C07D 401/04 (2006.01) C07D 413/04 (2006.01)

Patent

CA 2422617

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. (I) 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 (II).

La présente invention concerne de nouveaux composés de formule (I) qui sont des inhibiteurs d'une tripeptidyl peptidase membranaire responsable de l'inactivation de neuropeptides endogènes tels que les cholécystokinines (CCK); des procédés de préparation de ces composés, des compositions pharmaceutiques renfermant lesdits composés. Dans la formule (I), n représente un entier tel que 0 ou 1; X représente O; S; ou -(CR?4¿R?5¿)¿m?- où m est un entier tel que 1 ou 2; R?4¿ et R?5¿ représentent chacun indépendamment de l'autre hydrogène ou alkyle C¿1-4; R?1¿ représente alkylcarbonyle C¿1-6? facultativement substitué par hydroxy; alkyloxycarbonyle C¿1-6?; amino alkylcarbonyle C¿1-6 ? dans lequel le groupe alkyle C¿1-6? est facultativement substitué par cycloalkyle C¿3-6?; mono- et di(alkyle C¿1-4?)amino alkylcarbonyle C¿1-6?; aminocarbonyle substitué par aryle; alkylcarbonyloxy C¿1-6? alkylcarbonyle C¿1-6?; alkyloxycarbonylamino C¿1-6? alkylcarbonyle C¿1-6? dans lequel le groupe amino est facultativement substitué par alkyle C¿1-4?; un acide aminé; alkyle C¿1-6? substitué par amino; ou arylcarbonyle; R?2¿ représente un hétérocycle à 5 chaînons facultativement substitué, ou R?2¿ représente benzimidazole facultativement substitué; R?3¿ représente un radical bivalent -CH¿2?CH¿2?- facultativement substitué par halo ou phénylméthyle; ou R?3¿ représente un radical bivalent de formule (II). Formules (I) et (II)

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