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Factor XIa inhibitors: A review of the patent literature

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Pages 323-345 | Received 25 Nov 2015, Accepted 10 Feb 2016, Published online: 25 Feb 2016

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Giovanni Santostasi, Gentian Denas & Vittorio Pengo. (2023) New pharmacotherapeutic options for oral anticoagulant treatment in atrial fibrillation patients aged 65 and older: factor XIa inhibitors and beyond. Expert Opinion on Pharmacotherapy 24:12, pages 1335-1347.
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Rami A. Al-Horani. (2020) Factor XI(a) inhibitors for thrombosis: an updated patent review (2016-present). Expert Opinion on Therapeutic Patents 30:1, pages 39-55.
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Antonio Gómez-Outes, Minerva García-Fuentes & Mª Luisa Suárez-Gea. (2017) Discovery methods of coagulation-inhibiting drugs. Expert Opinion on Drug Discovery 12:12, pages 1195-1205.
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Yunqing Xia, Yu Hu & Liang Tang. (2023) Factor XIa Inhibitors as a Novel Anticoagulation Target: Recent Clinical Research Advances. Pharmaceuticals 16:6, pages 866.
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Zhouling Xie, Zhiwei Meng, Xiaoxiao Yang, Yajun Duan, Qin Wang & Chenzhong Liao. (2023) Factor XIa Inhibitors in Anticoagulation Therapy: Recent Advances and Perspectives. Journal of Medicinal Chemistry 66:8, pages 5332-5363.
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Xinkang Wang, Qiu Li, Fuyong Du, Neetu Shukla, Andrea R. Nawrocki & Madhu Chintala. (2023) Antithrombotic Effects of the Novel Small-Molecule Factor XIa Inhibitor Milvexian in a Rabbit Arteriovenous Shunt Model of Venous Thrombosis. TH Open 07:02, pages e97-e104.
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Wu YangJames R. CorteJoseph M. Luettgen. 2022. 2022 Medicinal Chemistry Reviews. 2022 Medicinal Chemistry Reviews 117 141 .
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Lisha Lin, Longyan Zhao, Na Gao, Ronghua Yin, Sujuan Li, Huifang Sun, Lutan Zhou, Guiling Zhao, Steven W. Purcell & Jinhua Zhao. (2020) From multi-target anticoagulants to DOACs, and intrinsic coagulation factor inhibitors. Blood Reviews 39, pages 100615.
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A. S. Kabankin, E. I. Sinauridze, E. N. Lipets & F. I. Ataullakhanov. (2019) Computer Design of Low-Molecular-Weight Inhibitors of Coagulation Factors. Biochemistry (Moscow) 84:2, pages 119-136.
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Mimi L. Quan, Donald J. P. Pinto, Joanne M. Smallheer, William R. Ewing, Karen A. Rossi, Joseph M. Luettgen, Dietmar A. Seiffert & Ruth R. Wexler. (2018) Factor XIa Inhibitors as New Anticoagulants. Journal of Medicinal Chemistry 61:17, pages 7425-7447.
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Rami A. Al-Horani & Daniel K. Afosah. (2018) Recent advances in the discovery and development of factor XI/XIa inhibitors. Medicinal Research Reviews 38:6, pages 1974-2023.
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Crossref
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Azeemullah A. Syed & Alka Mehta. (2018) Target Specific Anticoagulant Peptides: A Review. International Journal of Peptide Research and Therapeutics 24:1, pages 1-12.
Crossref
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