Diaryl ether derivatives as notch sparing gamma secretase inhibitors

US8871796B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• William Colby Brown · Cleveland Heights, US
• Jason D. Brubaker · Cambridge, US
• Christian Fischer · Natick, US
• Richard W. Heidebrecht · Somerville, US
• John Hendrix · Charlottesville, US
• Elizabeth H. Kelley · Cambridge, US
• Rachel N. MacCoss · Brookline, US
• Joey L. Methot · Westwood, US
• Thomas Miller · Brookline, US
• Karin M. Otte · Natick, US
• Phieng Siliphaivanh · Newton, US
• Thomas S. Reger · Lansdale, US
• Peter D. Williams · Harleysville, US
• Catherine M. Wiscount · Allentown, US

Key dates

• Filing date: Oct 5, 2010
• Grant date: Oct 28, 2014
• Expiry date: Oct 14, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D491/113
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.