Cyclic polypeptides for PCSK9 inhibition

US12012468B2 · kind B2 · utility

Assignees

• Merck Sharp & Dohme LLC · US
• RA PHARMACEUTICALS, INC. · US

Inventors

• Alonso Ricardo · Cambridge, US
• Thomas J. Tucker · North Wales, US
• Nicolas Cedric Boyer · Somerville, US
• Joseph R. Stringer · Madison, US
• Derek M. LaPlaca · Somerville, US
• Angela Dawn Kerekes · Plainfield, US
• Chengwei Wu · Ambler, US
• Sookhee Nicole Ha · Pequest, US
• Hyewon Youm · Berkeley Heights, US
• Mark W. Embrey · North Wales, US
• Elisabetta Bianchi · Pomezia, IT
• Danila Branca · Pomezia, IT
• Raffaele Ingenito · Pomezia, IT
• Willy Costantini · Pomezia, IT
• Alessia Santoprete · Pomezia, IT
• Roberto Costante · Silvi, IT
• Immacolata Conte · Roma, IT
• Stefania Colarusso · Roma, IT
• Eric J. Gilbert · Scotch Plains, US
• Aurash Shahripour · Rahway, US
• Yusheng Xiong · Newtown, US

Key dates

• Filing date: Sep 27, 2022
• Grant date: Jun 18, 2024
• Expiry date: Sep 27, 2042

Classification

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

Abstract

Provided herein are cyclic polypeptide compounds that can, e.g., bind specifically to human proprotein convertase subtilisin/kexin type 9 (PCSK9) and optionally also inhibit interaction between human PCSK9 and human low density lipoprotein receptor (LDLR), and pharmaceutical compositions comprising one or more of these compounds. Also provided are methods of reducing LDL cholesterol level in a subject in need thereof that include administering to the subject one or more of the cyclic polypeptide compounds or a pharmaceutical composition provided herein.