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PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) INHIBITOR AND PHARMACEUTICAL USE THEREFOR

机译:ProProtein转化酶枯草杆菌蛋白酶/ kexin型9(PCSK9)抑制剂和药物用途

摘要

The present invention addresses the problem of providing a low-molecular-weight compound having inhibitory activity against the function of proprotein convertase subtilisin/kexin type 9 (PCSK9). One aspect of the present invention relates to a compound represented by formula (I) (in the formula, n, R1, R2, R3, R4, R5, and R6 are as defined in the specification or in the claims), a pharmaceutically acceptable salt thereof, or a PCSK9 inhibitor containing a pharmaceutically acceptable solvate thereof as an active ingredient. Another aspect of the present invention relates to a drug that contains the PCSK9 inhibitor of the one aspect of the present invention as an active ingredient and that is for use in preventing or treating one or more symptoms, diseases, or disorders relating to PCSK9 function and selected from the group consisting of hypercholesterolemia, familial hypersterolemia, hyperlipidemia, arteriosclerosis, fatty liver, obesity, pancreatic beta cell failure, cholesteryl ester storage disease, Wolman disease, Niemann-Pick disease type C, symptoms in Hodgkin's lymphoma survivors, Tangier disease, Kawasaki disease, sitosterolemia, juvenile idiopathic arthritis, familial hypercholesterolemia, diabetes, symptoms in kidney transplant patients, and symptoms in heart transplant patients.
机译:本发明解决了提供具有抑制活性的低分子量化合物,其针对Proprotein转化酶枯草杆菌蛋白酶/ kexin型9(PCSK9)的功能。本发明的一个方面涉及由式(I)表示的化合物(在式中,在N,R 1 ,R 2 ,R 3 ,R 4 ,R 5 ,和R 6 如说明书或权利要求所述),其药学上可接受的盐或含有其药学上可接受的溶剂化物作为活性成分的PCSK9抑制剂。本发明的另一方面涉及一种药物,其含有本发明的一个方面的PCSK9抑制剂作为活性成分,其用于预防或治疗与PCSK9功能有关的一种或多种症状,疾病或病症选自高胆固醇血症,家族性疗效血症,高脂血症,动脉硬化,脂肪肝,肥胖,胰腺β细胞衰竭,胆囊酯储存疾病,Woldman病,Niemann-Pick疾病类型C,霍奇金淋巴瘤幸存者的症状,唐切尔疾病,川崎疾病,睾酮血症,青少年特发性关节炎,家族性高胆固醇血症,糖尿病,肾移植患者症状,以及心脏移植患者的症状。

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