Isophthalates as beta-secretase inhibitors

US7981913B2 · kind B2 · utility

Assignee

• Bristol-Myers Squibb Company · US

Inventors

• Lorin A. Thompson, III · Higganum, US
• Kenneth M. Boy · Durham, US
• Jianliang Shi · Furlong, US
• John E. Macor · Guilford, US

Key dates

• Filing date: May 14, 2010
• Grant date: Jul 19, 2011
• Expiry date: May 14, 2030

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

There is provided a series of substituted isophthalates of formula (I)or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.