Medical application of compounds with PCSK9 inhibitory activity

The invention discloses a medical application of a compound with PCSK9 inhibitory activity. The compound as shown in formulas I-IV, or a composition of a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate and a pharmaceutically acceptable carrier has the PCSK9 inhibitory activit...

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Hauptverfasser: SUN HONGBIN, DAI LIANG, YUAN HAOLIANG, SUN HENGZHI, WEN XIAOAN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a medical application of a compound with PCSK9 inhibitory activity. The compound as shown in formulas I-IV, or a composition of a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate and a pharmaceutically acceptable carrier has the PCSK9 inhibitory activity. The compound represented by the compound shown in the formula IV can be directly combined with PCSK9 protein, so that protein-protein interaction of PCSK9 and LDLR is inhibited, LDL uptake of liver cells is increased, and therefore the compound can be used for preparing drugs for preventing or treating hyperlipidemia and related metabolic diseases. 本发明公开了一类具有PCSK9抑制活性的化合物的医药用途,本发明如下式Ⅰ-Ⅳ所示的化合物、或其立体异构体、互变异构体、药学上可接受的盐、溶剂化物、与药学上可接受的载体的组合物具有PCSK9抑制活性。本发明公开的如式Ⅳ化合物为代表的化合物,可以直接与PCSK9蛋白结合,从而抑制PCSK9与LDLR的蛋白-蛋白相互作用,增加肝细胞对LDL的摄取,因此可用于制备预防或治疗高血脂症及相关代谢性疾病的药物。