758685-72-2Relevant academic research and scientific papers
Preparation method of edoxaban and intermediate thereof
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Paragraph 0032-0035, (2021/06/12)
The invention relates to a preparation method of edoxaban and an intermediate thereof. A compound 1, a compound 2 and a compound 5 which are taken as initial raw materials are subjected to an ammonolysis reaction, a deprotection reaction, a carboxylation reaction and a condensation reaction to generate edoxaban. Compared with the prior art, the preparation method is higher in operability and safety during amplified production, and the obtained product is high in yield and purity.
Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors
Xing, Junhao,Yang, Lingyun,Zhou, Jinpei,Zhang, Huibin
, p. 5987 - 5999 (2018/11/23)
Factor Xa (fXa) is a crucial player in various thromboembolic disorders. Inhibition of fXa can provide safe and effective antithrombotic effects. In this study, a series of anthranilamide compounds were designed by utilizing structure-based design strategies. Optimization at P1 and P4 groups led to the discovery of compound 16g: a highly potent, selective fXa inhibitor with pronounced in vitro anticoagulant activity. Moreover, 16g also displayed excellent in vivo antithrombotic activity in the rat venous thrombosis (VT) and arteriovenous shunt (AV-SHUNT) models. The bleeding risk evaluation showed that 16g had a safer profile than that of betrixaban at 1 mg/kg and 5 mg/kg dose. Additionally, 16g also exhibited satisfactory PK profiles. Eventually, 16g was selected to investigate its effect on hypoxia-reoxygenation- induced H9C2 cell viability. MTT results showed that H9C2 cell viability can be remarkably alleviated by 16g.
METHOD FOR PRODUCING INHIBITOR OF ACTIVATED BLOOD COAGULATION FACTOR X (FXA)
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Paragraph 0195; 0196, (2017/03/21)
An object of the present invention is to provide a novel method for producing a compound, a salt thereof, or a hydrate of the compound or the salt, which is an FXa inhibitor. The object can be attained by a production method in which a production method via a compound represented by formula (1-1), etc., from a compound represented by the following formula (1-x), etc., is used for a method for producing a compound represented by the following formula (X), etc. [wherein X represents a halogen atom or the like, and R1 represents an optionally substituted phenyl group].
Substituted oxazolidinone compounds and method and use thereof
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Paragraph 0286; 0293; 0294, (2017/02/02)
The invention provides a substituted oxazolidinone compound represented by a formula (I) shown in specifications, or stereoisomers, tautomers, nitrogen oxides, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof. The compound i
