Inhibitors of beta-secretase

US9018391B2 · kind B2 · utility

Assignees

• Boehringer Ingelheim International GmbH · DE
• Vitae Pharmaceuticals, LLC · US

Inventors

• Yuri Bukhtiyarov · Boothwyn, US
• Salvacion Cacatian · Conshohocken, US
• Lawrence Wayne Dillard · Yardley, US
• Klaus Fuchs · Ingelheim am Rhein, DE
• Lanqi Jia · Horsham, US
• Deepak S. Lala · North Wales, US
• Angel Morales-Ramos · Blue Bell, US
• Suresh B. Singh · Kendall Park, US
• Shankar Venkatraman · Lansdale, US
• Zhenrong Xu · Forest Park, US
• Jing Yuan · Lansdale, US
• Yi Zhao · Blue Bell, US
• Yajun Zheng · Hockessin, US
• Cornelia Dorner-Ciossek · Ingelheim am Rhein, DE
• Ulrike Gross · Ingelheim am Rhein, DE
• Niklas Heine · Eberhardzell, DE
• Achim Sauer · Ravensburg, DE

Key dates

• Filing date: Aug 27, 2013
• Grant date: Apr 28, 2015
• Expiry date: Aug 27, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2603/97
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.