N-aryl pyrrolidine derivatives as beta-secretase inhibitors

US7408071B2 · kind B2 · utility

Assignee

• Bristol-Myers Squibb Company · US

Inventors

• Kenneth M. Boy · Durham, US
• Shirong Zhu · Cheshire, US
• John E. Macor · Guilford, US
• Shuhao Shi · Madison, US
• Samuel Gerritz · Guilford, US

Key dates

• Filing date: Mar 29, 2007
• Grant date: Aug 5, 2008
• Expiry date: Apr 9, 2027

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D209/52
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

There is provided a series of substituted N-aryl pyrrolidine derivatives of Formula (I)or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R5′, R6, R7, and p 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.