Substituted oxopyridine derivatives and use thereof in the treatment of cardiovascular disorders
By inhibiting serine protease FXIa and plasma kallikrein through substituted oxopyridine derivatives, the bleeding risk and side effects of existing anticoagulants in the treatment of thromboembolic diseases are solved, and effective treatment of cardiovascular and ophthalmic diseases is achieved. Prevention and treatment.
CN108164513AInactive Publication Date: 2018-06-15BAYER PHARMA AG
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Patent Information
- Application Number
- CN201711458259.0
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2013-10-30
- Filing Date
- 2014-03-27
- Publication Date
- 2018-06-15
- Estimated Expiration
- Not applicable · inactive patent
AI Technical Summary
Technical Problem
Existing anticoagulants have bleeding risks, high variable bioavailability and other side effects when treating and preventing thromboembolic disorders, and are difficult to effectively prevent the alternating increase in thrombosis and inflammation.
Method used
Provided is a substituted oxopyridine derivative, which regulates blood coagulation cascade and platelet aggregation by inhibiting serine protease FXIa and plasma kallikrein, and is used for the treatment and prevention of cardiovascular and ophthalmic diseases.
Benefits of technology
Effectively inhibits thrombosis and inflammation, reduces vascular permeability, reduces the risk of thromboembolic complications, while reducing the risk of bleeding, providing a wider range of treatments.
✦ Generated by Eureka AI based on patent content.
Abstract
The invention provides substituted oxopyridine derivatives of the formula (1) as shown in the discription, where R1 represents a group of the formula, * is the point of attachment to the oxopyridine ring, R6 represents bromine, chlorine, fluorine, methyl, difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy or trifluoromethoxy, and R7 represents bromine, chlorine, fluorine, cyano, nitro, hydroxy, methyl, difluoromethyl, trifluoromethyl, methoxy, ethoxy, difluoromethoxy, trifluoromethoxy, ethynyl, 3,3,3-trifluoroprop-1-yn-1-yl or cyclopropyl. The invention also relates to processes for preparation of substituted oxopyridine derivatives, and also to their use for preparing medicaments for the treatment and / or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
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