Tripeptidyl peptidase inhibitors

US7125891B2 · kind B2 · utility

Assignee

• Janssen Pharmaceutica NA · BE

Inventors

• Henry J. Breslin · Lansdale, US
• Hans Louis Jos De Winter · Schilde, BE
• Michael Joseph Kukla · Masontown, US

Key dates

• Filing date: Oct 24, 2001
• Grant date: Oct 24, 2006
• Expiry date: Aug 28, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D417/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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 substit…