1B20 PCSK9 antagonists

US8957194B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Jon H. Condra · Abington, US
• Rose M. Cubbon · Fanwood, US
• Holly A. Hammond · Telford, US
• Timothy McCabe · Doylestown, US
• Shilpa Pandit · Edison, US
• Laurence B. Peterson · Westfield, US
• Joseph C. Santoro · Montgomery, US
• Ayesha Sitlani · Metuchen, US
• Dana D. Wood · Collegeville, US
• Henryk Mach · Somerset, US
• Heidi Joanne Pixley · Glenside, US
• Sonia M. Gregory · Blue Bell, US
• Jeffrey T. Blue · Telford, US
• Kevin Caili Wang · Lansdale, US
• Peizhi Luo · Arcadia, US
• Denise K. Nawrocki · Annandale, US
• Pingyu Zhong · Blue Bell, US
• Feng Dong · Lansdale, US
• Yan Li · Tianjin, CN

Key dates

• Filing date: May 8, 2012
• Grant date: Feb 17, 2015
• Expiry date: May 8, 2032

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K2317/92
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.