Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors

US8569521B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Theodros Asberom · West Orange, US
• Thomas Bara · Linden, US
• Chad E. Bennett · Metuchen, US
• Duane A. Burnett · Wayland, US
• Mary Anne Caplen · Sayreville, US
• John W. Clader · Cranford, US
• David James Cole · Springfield, US
• Martin S. Domalski · Verona, US
• Hubert Josien · Hoboken, US
• Chad Knutson · Garwood, US
• Hongmei Li · Hackettstown, US
• Mark D. McBriar · Clinton, US
• Dmitri Pissarnitski · Scotch Plains, US
• Li Qiang · Edison, US
• Murali Rajagopalan · Edison, US
• Thavalakulamgara K. Sasikumar · Westfield, US
• Jing Su · Scotch Plains, US
• Haiqun Tang · Montgomery, US
• Wen-Lian Wu · Edison, US
• Ruo Xu · Watchung, US
• Zhiqiang Zhao · Scotch Plains, US

Key dates

• Filing date: Oct 6, 2011
• Grant date: Oct 29, 2013
• Expiry date: Oct 6, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2602/12
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

This invention discloses novel gamma secretase inhibitors of the formula:R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.