PCSK9 antagonist compounds

US11427616B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Harold B. Wood · Westfield, US
• Hubert Josien · Hoboken, US
• Thomas J. Tucker · North Wales, US
• Angela Dawn Kerekes · Plainfield, US
• Ling Tong · Hackettstown, US
• Abbas M. Walji · Lansdale, US
• Anilkumar G. Nair · Edison, US
• Fa-Xiang Ding · Staten Island, US
• Elisabetta Bianchi · Pomezia, IT
• Danila Branca · Pomezia, IT
• Chengwei Wu · Ambler, US
• Yusheng Xiong · Newtown, US
• Sookhee Nicole Ha · Pequest, US
• Jian Liu · Xi'an, CN
• Sobhana Babu Boga · Scotch Plains, US

Key dates

• Filing date: Jun 20, 2019
• Grant date: Aug 30, 2022
• Expiry date: Feb 4, 2040

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed are compounds of Formula I, or a salt thereof: where A, B, D, X, R1, R2 and R8 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.