CETP inhibitors

US8735435B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Amjad Ali · Freehold, US
• Joann M. Napolitano · Woodbridge, US
• Qiaolin Deng · Edison, US
• Zhijian Lu · Clinton, US
• Peter J. Sinclair · Highland Park, US
• Gayle E. Hallett · Smethwick, GB
• Christopher F. Thompson · Arlington, US
• Nazia Quraishi · Bethesda, US
• Cameron Smith · Lawrenceville, US

Key dates

• Filing date: Nov 25, 2009
• Grant date: May 27, 2014
• Expiry date: Dec 21, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D263/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis:In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.