N-substituted peptidyl nitriles as cysteine cathepsin inhibitors

US6812237B2 · kind B2 · utility

Assignee

• Novartis AG · CH

Inventors

• Scott D. Cowen · Readington, US
• Paul Greenspan · New Providence, US
• Leslie Wighton McQuire · Hackettstown, US
• Ruben Tommasi · Whitehouse Station, US
• John H. van Duzer · Phillipsburg, US

Key dates

• Filing date: Nov 7, 2002
• Grant date: Nov 2, 2004
• Expiry date: Nov 16, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds of the formula (I), wherein R1 is aryl or biaryl; R2 is aryl-lower alkyl, biaryl-lower alkyl, benzo-fused cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7-alkyl in which C2-C7-alkyl is interrupted by Y; Y is O, S, SO, SO2, CO or NR6; R3 is hydrogen or lower alkyl; or R2 and R3 combined are C2-C7-alkylene or C2-C7-alkylene interrupted by Y; R4 is hydrogen or lower alkyl; R5 is hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, biaryl-lower alkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7-alkyl in which C2-C7-alkyl is interrupted by Y; R6 is hydrogen, lower alkyl or aryl-lower alkyl; and pharmaceutically acceptable salts thereof, which are useful as cysteine cathepsin inhibitors