24115-90-0Relevant academic research and scientific papers
Novel strategy to boost oral anticoagulant activity of blood coagulation enzyme inhibitors based on biotransformation into hydrophilic conjugates
Ishihara, Tsukasa,Koga, Yuji,Mori, Kenichi,Sugasawa, Keizo,Iwatsuki, Yoshiyuki,Hirayama, Fukushi
, p. 6324 - 6332 (2014)
The blood coagulation cascade represents an attractive target for antithrombotic drug development, and recent studies have attempted to identify oral anticoagulants with inhibitory activity for enzymes in this cascade, with particular attention focused on
Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system
Ishihara, Tsukasa,Koga, Yuji,Iwatsuki, Yoshiyuki,Hirayama, Fukushi
, p. 277 - 289 (2015/02/05)
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.
Heterocyclic amido derivatives of substituted benzoic acids and therapeutic compositions which contain them as active principle
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, (2008/06/13)
Heterocyclic amido derivatives of substituted benzoic acids of general formula (I): in which:, R1 is H; 3-OCH3; 3-Cl; 4-Cl; 5-Cl; 3-CH3; 5-CH3; or 3-OH; -CH2-COOH; or -CH2-CO2-C
