PCSK9 antagonists bicyclo-compounds

US11306125B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Yusheng Xiong · Newtown, US
• Thomas J. Tucker · North Wales, US
• Chengwei Wu · Ambler, US
• Elisabetta Bianchi · Pomezia, IT
• Danila Branca · Pomezia, IT
• Angela Dawn Kerekes · Plainfield, US
• Abbas M. Walji · Lansdale, US
• Hubert Josien · Hoboken, US
• Fa-Xiang Ding · Staten Island, US
• Hyewon Youm · Berkeley Heights, US
• Alessia Santoprete · Pomezia, IT
• Raffaele Ingenito · Pomezia, IT

Key dates

• Filing date: Jun 20, 2019
• Grant date: Apr 19, 2022
• Expiry date: Jun 20, 2039

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 cyclic polypeptide of Formula I: Formula I where A, B, E, R4, 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