Tripeptidyl peptidase inhibitors

45m4 5 1-41 1-61-61-61-63-61-41-61-61-61-61-61-41-62 2 3 223 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 furt...

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Bibliographische Detailangaben
Hauptverfasser: Breslin, Henry Joseph, De Winter, Hans Louis Jos, Kukla, Michael Joseph
Format: Patent
Sprache:eng
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Zusammenfassung:45m4 5 1-41 1-61-61-61-63-61-41-61-61-61-61-61-41-62 2 3 223 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 -(CRR)- wherein m is an integer 1 or 2; Rand Rare each independently from each other hydrogen or Calkyl; Ris Calkylcarbonyl optionally substituted with hydroxy; Calkyloxycarbonyl; aminoCalkylcarbonyl wherein the Calkyl group is optionally substituted with Ccycloalkyl; mono- and di(Calkyl)aminoCalkylcarbonyl; aminocarbonyl substituted with aryl; CalkylcarbonyloxyCalkylcarbonyl; CalkyloxycarbonylaminoCalkylcarbonyl wherein the amino group is optionally substituted with Calkyl; an amino acid; Calkyl substituted with amino; or arylcarbonyl; Ris an optionally substituted 5-membered heterocycle, or Ris optionally substituted benzimidazole; Ris a bivalent radical -CHCH- optionally substituted with halo or phenylmethyl; or Ris a bivalent radical of formula