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Novel factor Xa inhibitors: a patent review

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Pages 1535-1580 | Published online: 10 Sep 2009

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Zhi-Hao Shi, Nian-Guang Li, Yu-Ping Tang & Jin-Ao Duan. (2014) Prolinamide derivatives as thrombin inhibitors for the treatment of thrombin-mediated diseases: a patent evaluation of US2013296245. Expert Opinion on Therapeutic Patents 24:10, pages 1139-1148.
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Donald J P Pinto, Jennifer X Qiao & Robert M Knabb. (2012) The emergence of factor Xa inhibitors for the treatment of cardiovascular diseases: a patent review. Expert Opinion on Therapeutic Patents 22:6, pages 645-661.
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Articles from other publishers (27)

Atul N. Khadse, Hardik H. Savsani, Rupesh V. Chikhale, Rahul B. Ghuge, Dixit R. Prajapati, Goshiya Kureshi, Prashant R. Murumkar, Kirti V. Patel, Sadhana J. Rajput & Mange Ram Yadav. (2022) Design, synthesis and biological evaluation of Piperazinylanthranilamides as potential factor Xa inhibitors. Journal of Molecular Structure 1270, pages 133974.
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María Isabel Fernández-Bachiller, Songhwan Hwang, María Elena Schembri, Peter Lindemann, Mónica Guberman, Svenja Herziger, Edgar Specker, Hans Matter, David W. Will, Jörg Czech, Michael Wagner, Armin Bauer, Herman Schreuder, Kurt Ritter, Matthias Urmann, Volkmar Wehner, Han Sun & Marc Nazaré. (2022) Probing Factor Xa Protein–Ligand Interactions: Accurate Free Energy Calculations and Experimental Validations of Two Series of High-Affinity Ligands. Journal of Medicinal Chemistry 65:19, pages 13013-13028.
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Rosa Purgatorio, Nicola Gambacorta, Francesco Samarelli, Gianfranco Lopopolo, Modesto de Candia, Marco Catto, Orazio Nicolotti & Cosimo D. Altomare. (2022) Assessing the Role of a Malonamide Linker in the Design of Potent Dual Inhibitors of Factor Xa and Cholinesterases. Molecules 27:13, pages 4269.
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N. S. Dubovik, D. F. Guranda, G. V. Ramenskaya, D. G. Tovbin, D. N. Tarasov, A. Yu. Savchenko & V. S. Arnautov. (2022) Development and Validation of the HPLC Method for Quantification of the Innovative Drug DD217, Factor Xa Inhibitor, in Rat Plasma for a Pharmacokinetic Study. Drug development & registration 11:2, pages 197-206.
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Nikolaos P. Tripolitsiotis, Maria Thomaidi & Constantinos G. Neochoritis. (2020) The Ugi Three‐Component Reaction; a Valuable Tool in Modern Organic Synthesis. European Journal of Organic Chemistry 2020:42, pages 6525-6554.
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Nadezhda Novichikhina, Ivan Ilin, Anna Tashchilova, Alexey Sulimov, Danil Kutov, Irina Ledenyova, Mikhail Krysin, Khidmet Shikhaliev, Anna Gantseva, Ekaterina Gantseva, Nadezhda Podoplelova & Vladimir Sulimov. (2020) Synthesis, Docking, and In Vitro Anticoagulant Activity Assay of Hybrid Derivatives of Pyrrolo[3,2,1-ij]Quinolin-2(1H)-one as New Inhibitors of Factor Xa and Factor XIa. Molecules 25:8, pages 1889.
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Nicolás E. Núñez-Navarro, Fabián M. Santana, Loreto P. Parra & Flavia C. Zacconi. (2019) Surfing the Blood Coagulation Cascade: Insight into the Vital Factor Xa. Current Medicinal Chemistry 26:17, pages 3175-3200.
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Flavia C. Zacconi. 2018. Anticoagulant Drugs. Anticoagulant Drugs.
Ruwan Gunaratne, Shekhar Kumar, James W Frederiksen, Steven Stayrook, Jens L Lohrmann, Kay Perry, Kristin M Bompiani, Charlene V Chabata, Nabil K Thalji, Michelle D Ho, Gowthami Arepally, Rodney M Camire, Sriram Krishnaswamy & Bruce A Sullenger. (2018) Combination of aptamer and drug for reversible anticoagulation in cardiopulmonary bypass. Nature Biotechnology 36:7, pages 606-613.
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Carlos Lagos, Gerardine Segovia, Nicolás Nuñez-Navarro, Mario Faúndez & Flavia Zacconi. (2017) Novel FXa Inhibitor Identification through Integration of Ligand- and Structure-Based Approaches. Molecules 22:10, pages 1588.
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Nirav R. Patel, Dushyant V. Patel, Prashant R. Murumkar & Mange Ram Yadav. (2016) Contemporary developments in the discovery of selective factor Xa inhibitors: A review. European Journal of Medicinal Chemistry 121, pages 671-698.
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Cristiana A. Zaharia, Saverio Cellamare & Cosimo D. Altomare. 2016. Bioactive Carboxylic Compound Classes: Pharmaceuticals and Agrochemicals. Bioactive Carboxylic Compound Classes: Pharmaceuticals and Agrochemicals 149 166 .
Soo Lee, Wonhwa Lee, Jong-Sup Bae & Eunsook Ma. (2016) Synthesis and in Vitro and in Vivo Anticoagulant and Antiplatelet Activities of Amidino- and Non-Amidinobenzamides. Molecules 21:5, pages 676.
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Edyta Burda & Jörg Rademann. (2014) Catalytic activation of pre-substrates via dynamic fragment assembly on protein templates. Nature Communications 5:1.
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Benny D. Belviso, Rocco Caliandro, Modesto de Candia, Giorgia Zaetta, Gianfranco Lopopolo, Francesca Incampo, Mario Colucci & Cosimo D. Altomare. (2014) How a β- d -Glucoside Side Chain Enhances Binding Affinity to Thrombin of Inhibitors Bearing 2-Chlorothiophene as P1 Moiety: Crystallography, Fragment Deconstruction Study, and Evaluation of Antithrombotic Properties . Journal of Medicinal Chemistry 57:20, pages 8563-8575.
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Jan A Hiss, Michael Reutlinger, Christian P Koch, Anna M Perna, Petra Schneider, Tiago Rodrigues, Sarah Haller, Gerd Folkers, Lutz Weber, Renato B Baleeiro, Peter Walden, Paul Wrede & Gisbert Schneider. (2014) Combinatorial chemistry by ant colony optimization. Future Medicinal Chemistry 6:3, pages 267-280.
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Meganathan Chandrasekaran, Sugunadevi Sakkiah & Keun Woo Lee. (2011) Combined chemical feature-based assessment and Bayesian model studies to identify potential inhibitors for Factor Xa. Medicinal Chemistry Research 21:12, pages 4083-4099.
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Calvin H. YehJames C. FredenburghJeffrey I. Weitz. (2012) Oral Direct Factor Xa Inhibitors. Circulation Research 111:8, pages 1069-1078.
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Anilkumar R KoreMuthian Shanmugasundaram. (2012) Novel serine protease inhibitors. Pharmaceutical Patent Analyst 1:4, pages 457-468.
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Gianfranco Lopopolo, Modesto de Candia, Luigi Panza, Maria Rosaria Romano, Marcello Diego Lograno, Francesco Campagna & Cosimo Altomare. (2012) β-D-Glucosyl Conjugates of Highly Potent Inhibitors of Blood Coagulation Factor Xa Bearing 2-Chorothiophene as a P1 Motif. ChemMedChem 7:9, pages 1669-1677.
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Yan Shi, Stephen P. O’Connor, Doree Sitkoff, Jing Zhang, Mengxiao Shi, Sharon N. Bisaha, Ying Wang, Chi Li, Zheming Ruan, R. Michael Lawrence, Herbert E. Klei, Kevin Kish, Eddie C.-K. Liu, Steve M. Seiler, Liang Schweizer, Thomas E. Steinbacher, William A. Schumacher, Jeffrey A. Robl, John E. Macor, Karnail S. Atwal & Philip D. Stein. (2011) Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors. Bioorganic & Medicinal Chemistry Letters 21:24, pages 7516-7521.
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Robert J. Young. (2011) The successful quest for oral factor Xa inhibitors; learnings for all of medicinal chemistry?. Bioorganic & Medicinal Chemistry Letters 21:21, pages 6228-6235.
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Kanti V. Mardia, Vysaul B. Nyirongo, Christopher J. Fallaize, Stuart Barber & Richard M. Jackson. (2011) Hierarchical Bayesian Modeling of Pharmacophores in Bioinformatics. Biometrics 67:2, pages 611-619.
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Kenji Yoshikawa, Toshiharu Yoshino, Yoshihiro Yokomizo, Kouichi Uoto, Hiroyuki Naito, Katsuhiro Kawakami, Akiyoshi Mochizuki, Tsutomu Nagata, Makoto Suzuki, Hideyuki Kanno, Makoto Takemura & Toshiharu Ohta. (2011) Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors. Bioorganic & Medicinal Chemistry Letters 21:7, pages 2133-2140.
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Gianfranco Lopopolo, Filomena Fiorella, Modesto de Candia, Orazio Nicolotti, Sophie Martel, Pierre-Alain Carrupt & Cosimo Altomare. (2011) Biarylmethoxy isonipecotanilides as potent and selective inhibitors of blood coagulation factor Xa. European Journal of Pharmaceutical Sciences 42:3, pages 180-191.
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Susanne Alban, Susanne Lühn & Simone Schiemann. (2010) Combination of a two-step fluorescence assay and a two-step anti-Factor Xa assay for detection of heparin falsifications and protein in heparins. Analytical and Bioanalytical Chemistry 399:2, pages 681-690.
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Lilli Anselm, David W. Banner, Jörg Benz, Katrin Groebke Zbinden, Jacques Himber, Hans Hilpert, Walter Huber, Bernd Kuhn, Jean-Luc Mary, Michael B. Otteneder, Narendra Panday, Fabienne Ricklin, Martin Stahl, Stefan Thomi & Wolfgang Haap. (2010) Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-{[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide} as a clinical candidate. Bioorganic & Medicinal Chemistry Letters 20:17, pages 5313-5319.
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