Heterocyclic aspartyl protease inhibitors

US8178513B2 · kind B2 · utility

Assignees

• SCHERING CORPORATION · US
• Pharmacopeia Drug Discovery, Inc. · US

Inventors

• Zhaoning Zhu · Plainsboro, US
• Brian McKittrick · New Vernon, US
• Zhong-Yue Sun · Sayreville, US
• Yuanzan C. Ye · New Brunswick, US
• Johannes H. Voigt · Cranford, US
• Corey Strickland · Bound Brook, US
• Elizabeth M. Smith · Verona, US
• Andrew Stamford · Madison, US
• William J. Greenlee · Teaneck, US
• Robert Mazzola · Stewartsville, US
• John P. Caldwell · Ringwood, US
• Jared N. Cumming · Garwood, US
• Lingyan Wang · East Brunswick Township, US
• Yusheng Wu · New York, US
• Ulrich Iserloh · Hoboken, US
• Tao Guo
• Thuy X. H. Le · Monmouth Junction, US
• Kurt W. Saionz · Cranford, US
• Suresh D. Babu · Pennington, US
• Rachael C. Hunter · Princeton, US

Key dates

• Filing date: Jun 8, 2009
• Grant date: May 15, 2012
• Expiry date: Jan 9, 2030

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02A50/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed are compounds of the formula Ior a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W, U, X, R1, R2, R3, and R4 are as defined herein, and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of using such compounds to inhibit aspartyl protease and to treat a variety of disease or disorders, including cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist