AX132 PCSK9 antagonists

US8877900B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Peter Peizhi Luo · San Mateo, US
• Kevin Caili Wangr · Lansdale, US
• Pingyu Zhong · Blue Bell, US
• Mark Hsieh · San Francisco, US
• Yan Li · Tianjin, CN
• Xinwei Wang · Dunstable, US
• Feng Dong · Lansdale, US
• Andrei Golosov · Cambridge, US
• Yan Ni · Westfield, US
• Weirong Wang · New Brunswick, US
• Laurence B. Peterson · Westfield, US
• Rose M. Cubbon · Fanwood, US
• Sujata Sharma · Eagleville, US
• Jon H. Condra · Abington, US
• Jun Lu · East Longmeadow, US
• Gopalakrishnan Parthasarathy · Fryeburg, US
• Stephen Soisson · Fryeburg, US
• Noel Byrne · Doylestown, US

Key dates

• Filing date: Oct 29, 2010
• Grant date: Nov 4, 2014
• Expiry date: Oct 29, 2030

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K2319/00
• 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.