365462-14-2

Upstream product

• 365462-13-1 3-hydroxy-4'-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide hydrochloride 
• 365462-73-3 3-hydroxy-4'-methoxy-2-nitrobenzanilide 
• 104-94-9 4-methoxy-aniline 
• 602-00-6 3-hydroxy-2-nitrobenzoic acid 
• 303134-03-4 4-(4-methyl-1,4-diazepan-1-yl)benzoic acid hydrochloride 
• 365462-74-4 2-amino-3-hydroxy-4'-methoxybenzanilide 
• 7285-11-2 chloroform methanol 

Downstream Products

• 365462-13-1 3-hydroxy-4'-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide hydrochloride 

Relevant academic research and scientific papers

Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system

Anticoagulant agents have emerged as a promising class of therapeutic drugs for the treatment and prevention of arterial and venous thrombosis. We investigated a series of novel orally active factor Xa inhibitors designed using our previously reported conjugation strategy to boost oral anticoagulant effect. Structural optimization of anthranilamide derivative 3 as a lead compound with installation of phenolic hydroxyl group and extensive exploration of the P1 binding element led to the identification of 5-chloro-N-(5-chloro-2-pyridyl)-3-hydroxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzamide (33, AS1468240) as a potent factor Xa inhibitor with significant oral anticoagulant activity. We also reported a newly developed Free-Wilson-like fragment recommender system based on the integration of R-group decomposition with collaborative filtering for the structural optimization process.

Diazepane derivatives or salts thereof

To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan deriva