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Review

Factor Xa inhibitors

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Pages 931-953 | Published online: 25 Feb 2005

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (4)

Modesto de Candia, Gianfranco Lopopolo & Cosimo Altomare. (2009) Novel factor Xa inhibitors: a patent review. Expert Opinion on Therapeutic Patents 19:11, pages 1535-1580.
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Agustin Casimiro-Garcia, Danette A Dudley, Ronald J Heemstra, Kevin J Filipski, Christopher F Bigge & Jeremy J Edmunds. (2006) Progress in the discovery of Factor Xa inhibitors. Expert Opinion on Therapeutic Patents 16:2, pages 119-145.
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Andreas Betz. (2001) Recent advances in Factor Xa inhibitors. Expert Opinion on Therapeutic Patents 11:6, pages 1007-1017.
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. (2001) Inhibitors of Factor Xa. Expert Opinion on Therapeutic Patents 11:5, pages 891-895.
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Articles from other publishers (25)

Zhi-Li Zhang, Changming Chen, Si-Ying Qu, Qiulan Ding & Qin Xu. (2022) Unexpected Dynamic Binding May Rescue the Binding Affinity of Rivaroxaban in a Mutant of Coagulation Factor X. Frontiers in Molecular Biosciences 9.
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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.
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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Yasuhiro Imaeda, Takanobu Kuroita, Hiroki Sakamoto, Tetsuji Kawamoto, Mamoru Tobisu, Noriko Konishi, Katsuhiko Hiroe, Masaki Kawamura, Toshimasa Tanaka & Keiji Kubo. (2008) Discovery of Imidazo[1,5- c ]imidazol-3-ones: Weakly Basic, Orally Active Factor Xa Inhibitors . Journal of Medicinal Chemistry 51:12, pages 3422-3436.
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Yasuhiro Imaeda, Toshio Miyawaki, Hiroki Sakamoto, Fumio Itoh, Noriko Konishi, Katsuhiko Hiroe, Masaki Kawamura, Toshimasa Tanaka & Keiji Kubo. (2008) Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors. Bioorganic & Medicinal Chemistry 16:5, pages 2243-2260.
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Jeffrey T. Kohrt, Christopher F. Bigge, John W. Bryant, Agustin Casimiro-Garcia, Liguo Chi, Wayne L. Cody, Tawny Dahring, Danette A. Dudley, Kevin J. Filipski, Staci Haarer, Ron Heemstra, Nancy Janiczek, Lakshmi Narasimhan, Thomas McClanahan, J. Thomas Peterson, Vaisheli Sahasrabudhe, Robert Schaum, Chad A. Van Huis, Kathleen M. Welch, Erli Zhang, Robert J. Leadley & Jeremy J. Edmunds. (2007) The Discovery of (2R,4R)-N-(4-chlorophenyl)-N- (2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolidine-1,2-dicarboxamide (PD 0348292), an Orally Efficacious Factor Xa Inhibitor. Chemical Biology & Drug Design 70:2, pages 100-112.
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Jeffrey T. Kohrt, Kevin J. Filipski, Wayne L. Cody, Christopher F. Bigge, Frances La, Kathleen Welch, Tawny Dahring, John W. Bryant, Daniele Leonard, Gary Bolton, Lakshmi Narasimhan, Erli Zhang, J. Thomas Peterson, Staci Haarer, Vaishali Sahasrabudhe, Nancy Janiczek, Shrilakshmi Desiraju, Mostofa Hena, Charles Fiakpui, Neerja Saraswat, Raman Sharma, Shaoyi Sun, Samarendra N. Maiti, Robert Leadley & Jeremy J. Edmunds. (2006) The discovery of glycine and related amino acid-based factor Xa inhibitors. Bioorganic & Medicinal Chemistry 14:13, pages 4379-4392.
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Brigitte Kaiser. (2006) DX‐9065a, a Direct Inhibitor of Factor Xa. Cardiovascular Drug Reviews 21:2, pages 91-104.
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Kazuyuki Sagi, Tadakiyo Nakagawa, Masahiro Yamanashi, Shingo Makino, Mitsuo Takahashi, Masaru Takayanagi, Kaoru Takenaka, Nobuyasu Suzuki, Seiji Oono, Noriyasu Kataoka, Kohki Ishikawa, Sayaka Shima, Yumiko Fukuda, Takashi Kayahara, Shunji Takehana, Yoichiro Shima, Kazumi Tashiro, Hiroshi Yamamoto, Ryota Yoshimoto, Seinosuke Iwata, Takashi Tsuji, Kuniya Sakurai & Masataka Shoji. (2003) Rational Design, Synthesis, and Structure−Activity Relationships of Novel Factor Xa Inhibitors:  (2-Substituted-4-amidinophenyl)pyruvic and -propionic Acids. Journal of Medicinal Chemistry 46:10, pages 1845-1857.
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Jean-Yves Mérour, Yann Davion, Gérald Guillaumet, Jean-Michel Léger, Christian Jarry & Brigitte Lesur. (2003) Synthesis of 5-(4-Aryl)-2-phenyl-5,6-dihydrobenzo[b][1,5]oxazocin-4-ones. HETEROCYCLES 60:8, pages 1793.
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Cecilia Chi, Li Liang, Patty Padovani & Steve Unger. (2003) Development and validation of a liquid chromatography–mass spectrometric method for the determination of DPC 423, an antithrombotic agent, in rat and dog plasma. Journal of Chromatography B 783:1, pages 163-172.
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Gabriele Cruciani, Emanuele Carosati & Sergio Clementi. 2003. The Practice of Medicinal Chemistry. The Practice of Medicinal Chemistry 405 416 .
Mark Czekaj, Scott I Klein, Kevin R Guertin, Charles J Gardner, Allison L Zulli, Henry W Pauls, Alfred P Spada, Daniel L Cheney, Karen D Brown, Dennis J Colussi, Valeria Chu, Robert J Leadley & Christopher T Dunwiddie. (2002) Optimization of the β-Aminoester class of factor Xa inhibitors. part 1: P4 and side-Chain modifications for improved In vitro potency. Bioorganic & Medicinal Chemistry Letters 12:12, pages 1667-1670.
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John W. LiebeschuetzStuart D. JonesPhillip J. MorganChris W. MurrayAndrew D. RimmerJonathan M. E. RoscoeBohdan WaszkowyczPauline M. WelshWilliam A. WylieStephen C. YoungHarry MartinJacqui MahlerLeo BradyKay Wilkinson. (2002) PRO_SELECT:  Combining Structure-Based Drug Design and Array-Based Chemistry for Rapid Lead Discovery. 2. The Development of a Series of Highly Potent and Selective Factor Xa Inhibitors. Journal of Medicinal Chemistry 45:6, pages 1221-1232.
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Wei He, Barbara Hanney, Michael R Myers, Stephen Condon, Michael R Becker, Alfred P Spada, Christopher Burns, Karen Brown, Dennis Colussi & Valeria Chu. (2002) Benzimidazoles and isosteric compounds as potent and selective factor Xa inhibitors. Bioorganic & Medicinal Chemistry Letters 12:6, pages 919-922.
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M. M. Mueller, S. Sperl, J. Stürzebecher, W. Bode & L. Moroder. (2002) (R)-3-Amidinophenylalanine-Derived Inhibitors of Factor Xa with a Novel Active-Site Binding Mode. Biological Chemistry 383:7-8.
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Thomas B McClanahan, Gary W Hicks, Angela L Morrison, Yun-Wen Peng, Nancy Janiczek-Dolphin, Thomas E Mertz, Mark E Sullivan, John Morser, Paul L Juneau & Robert Leadley. (2001) The antithrombotic effects of CI-1031 (ZK-807834) and enoxaparin in a canine electrolytic injury model of arterial and venous thrombosis. European Journal of Pharmacology 432:2-3, pages 187-194.
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Herbert Nar, Margit Bauer, Angela Schmid, Jean-Marie Stassen, Wolfgang Wienen, Henning W.M Priepke, Iris K Kauffmann, Uwe J Ries & Norbert H Hauel. (2001) Structural Basis for Inhibition Promiscuity of Dual Specific Thrombin and Factor Xa Blood Coagulation Inhibitors. Structure 9:1, pages 29-37.
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Uwe Heinelt, Silke Herok, Hans Matter & Peter Wildgoose. (2001) Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors. Bioorganic & Medicinal Chemistry Letters 11:2, pages 227-230.
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Danette A. Dudley, Amy M. Bunker, Liguo Chi, Wayne L. Cody, Debra R. Holland, Diane P. Ignasiak, Nancy Janiczek-Dolphin, Thomas B. McClanahan, Thomas E. Mertz, Lakshmi S. Narasimhan, Stephen T. Rapundalo, Julia A. Trautschold, Chad A. Van Huis & Jeremy J. Edmunds. (2000) Rational Design, Synthesis, and Biological Activity of Benzoxazinones as Novel Factor Xa Inhibitors. Journal of Medicinal Chemistry 43:22, pages 4063-4070.
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Wei He, Barbara Hanney, Michael R Myers, Alfred P Spada, Karen Brown, Dennis Colussi & Valeria Chu. (2000) Nonbenzamidine compounds as selective factor xa inhibitors. Bioorganic & Medicinal Chemistry Letters 10:15, pages 1737-1739.
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Jeffrey T Kohrt, Kevin J Filipski, Stephen T Rapundalo, Wayne L Cody & Jeremy J Edmunds. (2000) An efficient synthesis of 2-(3-(4-amidinophenylcarbamoyl)naphthalen-2-yl)-5-((2,2-methylpropyl)carbamoyl)benzoic acid: a factor VIIa inhibitor discovered by the Ono Pharmaceutical Company. Tetrahedron Letters 41:32, pages 6041-6044.
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Yong Gong, Michael Becker, Yong Mi Choi-Sledeski, Roderick S Davis, Joseph M Salvino, Valeria Chu, Karen D Brown & Henry W Pauls. (2000) Solid-phase parallel synthesis of azarene pyrrolidinones as factor Xa inhibitors. Bioorganic & Medicinal Chemistry Letters 10:10, pages 1033-1036.
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Yong Gong, Henry W. Pauls, Alfred P. Spada, Mark Czekaj, Guyan Liang, Valeria Chu, Dennis J. Colussi, Karen D. Brown & Jingbo Gao. (2000) Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa. Bioorganic & Medicinal Chemistry Letters 10:3, pages 217-221.
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