Substituted tetrahydroisoquinolines as β-secretase inhibitors

US7902218B2 · 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
• Andrew C. Good · Wallingford, US
• Lawrence R. Marcin · Bethany, US

Key dates

• Filing date: Dec 6, 2007
• Grant date: Mar 8, 2011
• Expiry date: Aug 24, 2029

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof,wherein R, R8 and R9 are as defined herein, their pharmaceutical compositions and methods of use. These 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.