Nitrogen-containing heterocyclic derivative inhibitor as well as preparation method and application thereof

CN120019043AActive Publication Date: 2025-05-16SHANGHAI HANSOH BIOMEDICAL CO LTD +1
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Patent Information

Application Number
CN202380071542.5
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2023-08-10
Filing Date
2023-10-13
Publication Date
2025-05-16
Estimated Expiration
2043-10-13

AI Technical Summary

Technical Problem

Most existing PCSK9 inhibitors are injectable, which has high production costs and high prices. Furthermore, statins have limited effectiveness in lowering low-density lipoprotein cholesterol (LDL-C) and cannot meet the treatment needs of patients with familial hypercholesterolemia.

Method used

To develop a nitrogen-containing heterocyclic PCSK9 small molecule inhibitor of general formula (I) that reduces LDL-C levels via oral administration, binds to the low-density lipoprotein receptor (LDLR) on the surface of hepatocytes to block the action of PCSK9, and optimizes cholesterol homeostasis.

Benefits of technology

This invention provides an orally administered PCSK9 small molecule inhibitor that significantly reduces LDL-C levels, overcomes the side effects of statins, and is suitable for patients with familial hypercholesterolemia, reducing cardiovascular risk.

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Abstract

The invention discloses a nitrogen-containing heterocyclic derivative inhibitor and a preparation method and application thereof. Specifically, the invention relates to a compound as shown in a general formula (I), a preparation method thereof, a pharmaceutical composition containing the compound, and application of the compound as an inhibitor in treatment of cardiovascular and cerebrovascular diseases and the like, and substituents in the general formula (I) are as defined in the specification. # imgabs0 #
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