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Novel Antithrombotic Agent White Powders Pharmaceutical Raw Materials Rivaroxaban CAS 366789-02-8
Product Name: Rivaroxaban
Synonyms: 5-Chloro-N-[[(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-5-oxazolidinyl]methyl]-2-thiophenecarboxamide;BAY 59-7939;Rivaroxaban;5-Chloro-N-(((5S)-2-oxo-3-(4-(3-oxomorpholin-4-yl)phenyl)-1,3-oxazolidin-5-yl)methyl)thiophene-2-carboxamide;2-Thiophenecarboxamide, 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-5-oxazolidinyl]methyl];Xarelto;(S)-5-chloro-N-((2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl)thiophene-2-carboxamide;Rivaroxaban (BAY59-7939)
Product Categories: Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;API;Inhibitor;Rivaroxaban;Pharmaceutical raw materials;Inhibitors
Melting point 228-229°C
Storage temp. Refrigerator
Chemical Properties : White Solid
Usage : anti-coagulant, Factor X inhibitor
Usage : A novel antithrombotic agent. A highly potent and selective, direct FXa inhibitor .
Antithrombotic drugs Rivaroxaban and dabigatran etexilate are currently the most promising antithrombotic drugs, and compared to traditional antithrombotic drugs heparin, essential difference is that it does not require participation of antithrombin Ⅲ, directly antagonizes the free and bound Xa factor. And heparin needs to have antithrombin Ⅲ and can play a role, and is invalid to the prothrombin complex of Xa factor. Two new oral anticoagulants are praised as as a major step forward of anticoagulant therapy and potentially fatal thrombosis prevention in the medical field, will become a new milestone in the development of cardiovascular drugs .
Rivaroxaban was associated research and development success by the German Bayer and USA Johnson & Johnson. In October 2008, get approved for listing in Canada and the EU, trade name is Xarelto. Rivaroxaban is the world's first oral direct Xa factor inhibitor, can be high selectively, competitively inhibit free and bound Xa factor and activity of prothrombin, in a dose - dependent manner prolonged activated partial thromboplastin time board (PT) and prothrombin time (aPTT), thus prolonging the clotting time, reducing thrombin formation. Having characteristics of high bioavailability, a wide spectrum of disease treatment, dose effect relationship is stable, convenient oral administration, low bleeding risk .
Rivaroxaban also is drug for prevention and treatment of venous thrombosis. Clinically for the prevention of forming patients with deep vein thrombosis (DVT) and pulmonary embolism (PE) after hip joint and knee replacement surgery. It can also be used to prevent stroke and non-CNS systemic embolism in patients with non-valvular atrial fibrillation, reduce the risk of recurrent coronary syndrome, and so on.
Dabigatran is a new antithrombotic drugs with a variety of characteristics developed by a German company Boehringer Ingelheim. In April 2008 , first listed in Germany and the UK, Trade name was Pradaxa. This is listed first oral anticoagulant drug following warfarin in the past 50 years, is another milestone in the field of anticoagulant therapy and potentially fatal thrombosis prevention.
Dabigatran is a new synthetic direct thrombin inhibitor, is a prodrug for oral administration, belongs to the thrombin inhibitors of non-peptides. After oral gastrointestinal absorption, it is converted to have a direct anticoagulant activity of dabigatran etexilate in vivo. Drug binds to the fibrin-specific binding sites of thrombin, preventing fibrinogen from cleaving into fibrin, thereby blocking the final step of the coagulation cascade network and thrombosis .
Rivaroxaban, sold under the brand name Xarelto among others, is a blood thinner which is taken by mouth. It was initially developed by Bayer. In the United States, it is marketed by Janssen Pharmaceutica. It is the first available active direct factor Xa inhibitor which is taken by mouth. The maximum inhibition of factor Xa occurs four hours after a dose. The effects last approximately 8–12 hours, but factor Xa activity does not return to normal within 24 hours, so once-daily dosing is possible.
In those with non-valvular atrial fibrillation it appears to be as effective as warfarin in preventing nonhemorrhagic strokes and embolic events. Rivaroxaban is associated with lower rates of serious and fatal bleeding events than warfarin though rivaroxaban is associated with higher rates of bleeding in the gastrointestinal tract .
In July 2012, the UK´s National Institute for Health and Clinical Excellence recommended rivaroxaban to prevent and treat venous thromboembolism .
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