Cyclic tetramer compounds as proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors for the treatment of metabolic disorders

US11026993B2 · kind B2 · utility

Assignee

• Novartis AG · CH

Inventors

• Karin Briner · Indianapolis, US
• Brian Addison DECHRISTOPHER · Mountain View, US
• Alec Nathanson Flyer · Cambridge, US
• Andrei Golosov · Cambridge, US
• Philipp Grosche · Inzlingen, DE
• Eugene Yuejin Liu · Lexington, US
• Justin Yik Ching Mao · North Reading, US
• Lauren G. Monovich · Summit, US
• Tajesh Jayprakash Patel · Medford, US
• Carina Cristina Sanchez · Somerville, US
• Liansheng SU · Cambridge, US
• Lihua Yang · Nanhu, CN
• Rui Zheng · Arlington, US

Key dates

• Filing date: Nov 26, 2019
• Grant date: Jun 8, 2021
• Expiry date: Nov 26, 2039

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K5/126
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R1, R1, R1, R1, R1, R1, R1, R1, R1, X1, X2, and X3 are described herein.