Cyclic amine BACE-1 inhibitors having a benzamide substituent

US8623867B2 · kind B2 · utility

Assignees

• Merck Sharp & Dohme LLC · US
• Pharmacopeia Drug Discovery, Inc. · US

Inventors

• Jared N. Cumming · Garwood, US
• Ulrich Iserloh · Hoboken, US
• Andrew Stamford · Madison, US
• Corey Strickland · Bound Brook, US
• Johannes H. Voight · Cranford, US
• Yusheng Wu · New York, US
• Ying Huang · Berkeley Heights, US
• Yan Xia · Edison, US
• Samuel Chackalamannil · Califon, US
• Tao Guo
• Douglas W. Hobbs · Yardley, US
• Thuy X. H. Le · Monmouth Junction, US
• Jeffrey H. Lowrie · Pennington, US
• Kurt W. Saionz · Cranford, US
• Suresh D. Babu · Pennington, US

Key dates

• Filing date: Sep 11, 2012
• Grant date: Jan 7, 2014
• Expiry date: Sep 11, 2032

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/06
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Disclosed are compounds of the formulaor a pharmaceutically acceptable salt or solvate thereof, whereinR1 isR is —C(O)—N(R27)(R28) orand the remaining variables are as defined in the specification.Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.