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

• Main Authors: LIU ERIC YOUNG, SANCHEZ CARINA CRISTINA, DECHRISTOPHER BRIAN ADDISON, PATEL TAJESH JAYPRAKASH, YANG LIHUA, FLYER ALEC NATHANSON, ZHENG RUI, MONOVICH LAUREN GILCHRIST, SU LIANSHENG, MAO JUSTIN YIK CHING, GROSCHE PHILIPP, BRINER KARIN, GOLOSOV ANDREI ALEXANDROVICH
• Format: Patent
• Language: Chinese; English
• Published: 23.07.2021
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

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. 本披露涉及有用于治疗胆固醇脂质代谢以及PCSK9起作用的其他疾病的PCSK9抑制剂，所述PCSK9抑制剂具有式(I)：或其药学上可接受的盐、水合物、溶剂化物、前药、立体异构体、N-氧化物或互变异构体，其中R1、R1、R1、R1、R1、R1、R1、R1、R1、X1、X2、和X3在本文中描述。