A cis 4-(5,6-diphenylpyrazin-2-ylamino)cyclohexyloxyacetic acid compound, its preparation method and application
By synthesizing cis-4-(5,6-diphenylpyrazine-2-amino)cyclohexyloxyacetic acid, the problems of short half-life and poor stability of existing PGI2 drugs have been solved, achieving drug efficacy with high selectivity and low side effects, and making it suitable for the treatment of a variety of diseases.
CN120004812BActive Publication Date: 2025-11-18SICHUAN UNIVERSITY OF SCIENCE AND ENGINEERING
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Patent Information
- Application Number
- CN202510166914.3
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Priority Date
- 2024-11-21
- Filing Date
- 2025-02-14
- Publication Date
- 2025-11-18
- Estimated Expiration
- 2045-02-14
AI Technical Summary
Technical Problem
Existing PGI2 drugs have short half-lives, poor chemical stability, and significant side effects, resulting in poor efficacy and inability to effectively treat a variety of diseases.
Method used
A compound of cis-4-(5,6-diphenylpyrazine-2-amino)cyclohexyloxyacetic acid was synthesized, and an IP receptor agonist with good chemical stability, high selectivity, and few side effects was prepared through specific reaction steps.
Benefits of technology
The prepared compound exhibits excellent antiplatelet aggregation activity and, as an antithrombotic and vasodilating drug, demonstrates high bioavailability and long half-life pharmacokinetic parameters, making it suitable for the treatment of various diseases.
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Abstract
The present application relates to a kind of cis 4-(5,6-diphenylpyrazin-2-aminyl) cyclohexyloxy acetic acid compound and its synthesis method and application, belong to the technical field of drug synthesis.The cis 4-(5,6-diphenylpyrazin-2-aminyl) cyclohexyloxy acetic acid compound has simple molecular structure, simple synthesis path and low production cost.Through in vitro platelet aggregation inhibition activity test, it is found that the synthesized compound shows excellent anti-platelet aggregation effect.In addition, in rat pharmacokinetic study, it is found that the compound shows excellent pharmacokinetic characteristics, has high bioavailability and longer half-life, can effectively improve its activity as antithrombotic drug, and shows excellent prevention and treatment effect in antithrombotic, vasodilator and anti-pulmonary arterial hypertension etc..
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