CYCLIC PENTAMER COMPOUNDS AS PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDER

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 X1, R1...

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Hauptverfasser: LIU ERIC YOUNG, SANCHEZ CARINA CRISTINA, DECHRISTOPHER BRIAN ADDISON, GUMP CHRISTOPHER, PATEL TAJESH JAYPRAKASH, HARRISON TYLER, FLYER ALEC NATHANSON, ZHENG RUI, MONOVICH LAUREN GILCHRIST, SU LIANSHENG, MAO JUSTIN YIK CHING, FRIEDMAN AHARON, GROSCHE PHILIPP, LIU QUINGKUN, YANG LIN, BECKER CHRISTOPHER, GOLOSOV ANDREI ALEXANDROVICH
Format: Patent
Sprache:chi ; eng
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Zusammenfassung: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 X1, R1, R2, R3, R4, R5, R6, R6', R7, R7', R8, R9, R9', R10, R11, R12, and n are described herein. 本披露涉及有用于治疗胆固醇脂质代谢以及其中PCSK9起作用的其他疾病的PCSK9抑制剂,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,所述PCSK9抑制剂具有式(I),其中X1、R1、R2、R3、R4、R5、R6、R6'、R7、R7'、R8、R9、R9'、R10、R11、R12、和n描述于本文。