PAR-1 (protease-activated receptor-1) antagonists for treating thrombotic diseases, as well as preparation and application thereof

A technology of reagents and alkaline conditions, applied in the field of PAR-1 antagonists containing an exocyclic imine structure and the preparation thereof, can solve the problems of high bleeding risk and the like, and achieve the effect of small bleeding risk
CN102442965AActive Publication Date: 2012-05-09TIANJIN INSTITUTE OF PHARMA RESEARCH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
TIANJIN INSTITUTE OF PHARMA RESEARCH
Publication Date
2012-05-09

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Abstract

The invention relates to PAR-1 (protease-activated receptor-1) antagonists for treating thrombotic diseases, as well as a preparation and application thereof. The antagonists are compounds shown in formula (I) or pharmaceutically acceptable salts thereof, wherein R<1> is C1-C3 alkyl, R<2> is H, F or Cl, R<3> is C1-C3 alkyl, and X is O, S, C(CH3)2, CH2CH2, CH=CH or NCH3. The invention also provides a preparation method of the compounds, a medicinal composition containing the compounds, and application of the compounds. The compounds provided by the invention can prevent and / or treat thrombotic diseases.
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Description

Technical field

[0001] The present invention belongs to the technical field of medicine. Specifically, the present invention relates to a PAR-1 antagonist containing an exocyclic imine structure for treating thrombotic diseases, and a preparation method and application thereof. Background technique

[0002] Protease Activated Acceptor-1 (PAR-1) is a new target of antiplatelet antithrombotic drugs discovered recently. Protease activated receptor 1 is also called thrombin receptor. After thrombin is activated by coagulation chain, it acts on platelets through PAR-1 receptor to activate platelets, causing platelet aggregation to cause thrombus and coagulation. Thrombosis caused by PAR-1 is rich in platelet components, which is the main cause of arterial thrombosis. PAR-1 antagonists can block thrombin from activating platelets, thereby blocking arterial thrombosis, and can be used to treat Acute Coronary Syndrome. There have been several PAR-1 inhibitors in clinical studies (Chack...

Claims

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