Novel thienopyridine compounds and use thereof in medicine

Abstract

The invention relates to novel thienopyridine compounds or pharmaceutically acceptable salts of the novel thienopyridine compounds, medicine compositions comprising the thienopyridine compounds as active ingredients, and an application of the novel thienopyridine compounds or pharmaceutically acceptable salts of the novel thienopyridine compounds to the preparation of an antiplatelet drug. Het is trimethylpyrazinyl, pyrazinyl, pyridyl, thienyl, or indolyl; R1 is H or cyclopropylethanone; R2 is H or acetoxyl.

Description

technical field [0001] The present invention relates to novel thienopyridine compounds or pharmaceutically acceptable salts thereof, pharmaceutical compositions containing these compounds as active ingredients, and the use of said thienopyridine compounds or pharmaceutically acceptable salts for preparing anti-inflammatory drugs. Application of platelet drugs. [0002] [0003] Wherein, Het is trimethylpyrazinyl, pyrazinyl, pyridyl, thienyl, indolyl; R 1 Is H or cyclopropanyl; R 2 is H or acetoxy. Background technique [0004] Thrombotic disease is a common disease, often manifested as myocardial infarction, ischemic cerebral infarction, and venous thromboembolism. The mortality rate and disability rate of thromboembolic diseases are high. Arteriovenous thrombosis is the leading cause of cardiovascular disease morbidity and death, and it is also one of the leading causes of death in cancer patients; 6.5 million people worldwide are affected by deep vein thrombosis ever...

AI Technical Summary

Problems solved by technology

Clopidogrel, the second-generation thienopyridine ADP P2Y12 receptor antagonist, is currently the standard treatment drug for anti-platelet aggregation; After the two-step metabolism of cytochrome P450, the active metabolite can be obtained, and the obtained active metabolite irreversibly binds to the P2Y12 receptor, which leads to the effect of clopidogrel for up to 4-5 days and increases the risk of massive bleeding. risk

Prasugrel is a third-generation thienopyridine ADP P2Y12 receptor antagonist. In its metabolic activation process, only one step depends on liver cytochrome P450, and the cyclopropylmethanone group in the molecular structure replaces the original clopidogrel Gray partially hydrolyzes the inactive ester group, so its ability to inhibit platelet aggregation is stronger and more effective; however, it is accompanied by a significant increase in the risk of bleeding and will run at a high level for a long time

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