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Review

Recent advances in Factor Xa inhibitors

Pages 1007-1017 | Published online: 25 Feb 2005

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

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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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Marc A Ilies, Claudiu T Supuran & Andrea Scozzafava. (2002) Therapeutic applications of serine protease inhibitors. Expert Opinion on Therapeutic Patents 12:8, pages 1181-1214.
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Articles from other publishers (24)

Anilkumar R KoreMuthian Shanmugasundaram. (2012) Novel serine protease inhibitors. Pharmaceutical Patent Analyst 1:4, pages 457-468.
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R. S. Bhatta, Y. S. Chhonker, D. Kumar, A. K. Saxena & G. K. Jain. (2010) Bioanalytical method development and validation for simultaneous estimation of (R)- and (S)-isomers of S002-333: a potent novel anti-thrombotic agent using LC–MS/MS. Medicinal Chemistry Research 20:9, pages 1581-1588.
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Yan Shi, Chi Li, Stephen P. O’Connor, Jing Zhang, Mengxiao Shi, Sharon N. Bisaha, Ying Wang, Doree Sitkoff, Andrew T. Pudzianowski, Christine Huang, Herbert E. Klei, Kevin Kish, Joseph YanchunasJr.Jr., Eddie C.-K. Liu, Karen S. Hartl, Steve M. Seiler, Thomas E. Steinbacher, William A. Schumacher, Karnail S. Atwal & Philip D. Stein. (2009) Aroylguanidine-based factor Xa inhibitors: The discovery of BMS-344577. Bioorganic & Medicinal Chemistry Letters 19:24, pages 6882-6889.
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Yan Shi, Jing Zhang, Mengxiao Shi, Stephen P. O’Connor, Sharon N. Bisaha, Chi Li, Doree Sitkoff, Andrew T. Pudzianowski, Saeho Chong, Herbert E. Klei, Kevin Kish, Joseph YanchunasJr.Jr., Eddie C.-K. Liu, Karen S. Hartl, Steve M. Seiler, Thomas E. Steinbacher, William A. Schumacher, Karnail S. Atwal & Philip D. Stein. (2009) Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors. Bioorganic & Medicinal Chemistry Letters 19:15, pages 4034-4041.
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Yan Shi, Doree Sitkoff, Jing Zhang, Herbert E. Klei, Kevin Kish, Eddie C.-K. Liu, Karen S. Hartl, Steve M. Seiler, Ming Chang, Christine Huang, Sonia Youssef, Thomas E. Steinbacher, William A. Schumacher, Nyeemah Grazier, Andrew Pudzianowski, Atsu Apedo, Lorell Discenza, Joseph YanchunasJr.Jr., Philip D. Stein & Karnail S. Atwal. (2008) Design, Structure−Activity Relationships, X-ray Crystal Structure, and Energetic Contributions of a Critical P1 Pharmacophore: 3-Chloroindole-7-yl-Based Factor Xa Inhibitors. Journal of Medicinal Chemistry 51:23, pages 7541-7551.
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Stephen P. O’Connor, Karnail Atwal, Chi Li, Eddie C.-K. Liu, Steven M. Seiler, Mengxiao Shi, Yan Shi, Philip D. Stein & Ying Wang. (2008) Synthesis and evaluation of acylguanidine FXa inhibitors. Bioorganic & Medicinal Chemistry Letters 18:16, pages 4696-4699.
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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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Yan Shi, Doree Sitkoff, Jing Zhang, Wei Han, Zilun Hu, Philip D. Stein, Ying Wang, Lawrence J. Kennedy, Stephen P. O’Connor, Saleem Ahmad, Eddie C.-K. Liu, Steve M. Seiler, Patrick Y.S. Lam, Jeffrey A. Robl, John E. Macor, Karnail S. Atwal & Robert Zahler. (2007) Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors. Bioorganic & Medicinal Chemistry Letters 17:21, pages 5952-5958.
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Masanori Miura, Norio Seki, Takanori Koike, Tsukasa Ishihara, Tatsuya Niimi, Fukushi Hirayama, Takeshi Shigenaga, Yumiko Sakai-Moritani, Tomihisa Kawasaki, Shuichi Sakamoto, Minoru Okada, Mitsuaki Ohta & Shin-ichi Tsukamoto. (2006) Potent and selective TF/FVIIa inhibitors containing a neutral P1 ligand. Bioorganic & Medicinal Chemistry 14:23, pages 7688-7705.
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Samuel Chackalamannil. (2006) Thrombin Receptor (Protease Activated Receptor-1) Antagonists as Potent Antithrombotic Agents with Strong Antiplatelet Effects. Journal of Medicinal Chemistry 49:18, pages 5389-5403.
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Yan Shi, Jing Zhang, Philip D. Stein, Mengxiao Shi, Stephen P. O’Connor, Sharon N. Bisaha, Chi Li, Karnail S. Atwal, Gregory S. Bisacchi, Doree Sitkoff, Andrew T. Pudzianowski, Eddie C. Liu, Karen S. Hartl, Steven M. Seiler, Sonia Youssef, Thomas E. Steinbacher, William A. Schumacher, Alan R. Rendina, Jeffrey M. Bozarth, Tara L. Peterson, Ge Zhang & Robert Zahler. (2005) Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors. Bioorganic & Medicinal Chemistry Letters 15:24, pages 5453-5458.
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Paul Edwards. (2005) Monitor – chemistry. Drug Discovery Today 10:20, pages 1403-1404.
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Hiroshi Ueno, Katsuyuki Yokota, Jun-ichi Hoshi, Katsutaka Yasue, Mikio Hayashi, Yasunori Hase, Itsuo Uchida, Kazuo Aisaka, Susumu Katoh & Hidetsura Cho. (2005) Synthesis and Structure−Activity Relationships of Novel Selective Factor Xa Inhibitors with a Tetrahydroisoquinoline Ring. Journal of Medicinal Chemistry 48:10, pages 3586-3604.
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Hiroshi Ueno, Katsuyuki Yokota, Jun-ichi Hoshi, Katsutaka Yasue, Mikio Hayashi, Itsuo Uchida, Kazuo Aisaka, Yasunori Hase, Susumu Katoh & Hidetsura Cho. (2005) Discovery of novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors. Bioorganic & Medicinal Chemistry Letters 15:1, pages 185-189.
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Shojiro Kadono, Akihisa Sakamoto, Yasufumi Kikuchi, Masayoshi Oh-eda, Naohiro Yabuta, Takaki Koga, Kunihiro Hattori, Takuya Shiraishi, Masayuki Haramura, Hirofumi Kodama, Toru Esaki, Haruhiko Sato, Yoshiaki Watanabe, Susumu Itoh, Masateru Ohta & Toshiro Kozono. (2004) Crystal structure of human factor VIIa/tissue factor in complex with peptide mimetic inhibitor. Biochemical and Biophysical Research Communications 324:4, pages 1227-1233.
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John J. Parlow, Ravi G. Kurumbail, Roderick A. Stegeman, Anna M. Stevens, William C. Stallings & Michael S. South. (2003) Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex. Bioorganic & Medicinal Chemistry Letters 13:21, pages 3721-3725.
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John J. ParlowBrenda L. CaseThomas A. DiceRicky L. FentonMichael J. HayesDarin E. JonesWilliam L. NeumannRhonda S. WoodRhonda M. LachanceThomas J. GirardNancy S. NicholsonMichael ClareRoderick A. StegemanAnna M. StevensWilliam C. StallingsRavi G. KurumbailMichael S. South. (2003) Design, Parallel Synthesis, and Crystal Structures of Pyrazinone Antithrombotics as Selective Inhibitors of the Tissue Factor VIIa Complex. Journal of Medicinal Chemistry 46:19, pages 4050-4062.
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John J Parlow & Michael S South. (2003) Synthesis of 2-pyridones as tissue factor VIIa inhibitors. Tetrahedron 59:39, pages 7695-7701.
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Mimi L. Quan, Christopher D. Ellis, Ming Y. He, Ann Y. Liauw, Patrick Y.S. Lam, Karen A. Rossi, Robert M. Knabb, Joseph M. Luettgen, Matthew R. Wright, Pancras C. Wong & Ruth R. Wexler. (2003) Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors. Bioorganic & Medicinal Chemistry Letters 13:6, pages 1023-1028.
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Donald J. AbrahamGregory S. Bisacchi. 2003. Burger's Medicinal Chemistry and Drug Discovery. Burger's Medicinal Chemistry and Drug Discovery 283 338 .
Mimi L Quan, Christopher D Ellis, Ming Y He, Ann Y Liauw, Francis J Woerner, Richard S Alexander, Robert M Knabb, Patrick Y.S Lam, Joseph M Luettgen, Pancras C Wong, Matthew R Wright & Ruth R Wexler. (2003) Nonbenzamidine tetrazole derivatives as factor Xa inhibitors. Bioorganic & Medicinal Chemistry Letters 13:3, pages 369-373.
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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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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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