Milvexian, an orally bioavailable, small‐molecule, reversible, direct inhibitor of factor XIa: In vitro studies and in vivo evaluation in experimental thrombosis in rabbits
Wong, Pancras C., Crain, Earl J., Bozarth, Jeffrey M., Wu, Yiming, Dilger, Andrew K., Wexler, Ruth R., Ewing, William R., Gordon, David, Luettgen, Joseph M.
Published in Journal of thrombosis and haemostasis (01.02.2022)
Published in Journal of thrombosis and haemostasis (01.02.2022)
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Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa
Pinto, Donald J. P, Orwat, Michael J, Koch, Stephanie, Rossi, Karen A, Alexander, Richard S, Smallwood, Angela, Wong, Pancras C, Rendina, Alan R, Luettgen, Joseph M, Knabb, Robert M, He, Kan, Xin, Baomin, Wexler, Ruth R, Lam, Patrick Y. S
Published in Journal of medicinal chemistry (01.11.2007)
Published in Journal of medicinal chemistry (01.11.2007)
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Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212)
Pinto, Donald J. P., Orwat, Michael J., Smith, Leon M., Quan, Mimi L., Lam, Patrick Y. S., Rossi, Karen A., Apedo, Atsu, Bozarth, Jeffrey M., Wu, Yiming, Zheng, Joanna J., Xin, Baomin, Toussaint, Nathalie, Stetsko, Paul, Gudmundsson, Olafur, Maxwell, Brad, Crain, Earl J., Wong, Pancras C., Lou, Zhen, Harper, Timothy W., Chacko, Silvi A., Myers, Joseph E., Sheriff, Steven, Zhang, Huiping, Hou, Xiaoping, Mathur, Arvind, Seiffert, Dietmar A., Wexler, Ruth R., Luettgen, Joseph M., Ewing, William R.
Published in Journal of medicinal chemistry (14.12.2017)
Published in Journal of medicinal chemistry (14.12.2017)
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Inhibition of Factor XIa as a New Approach to Anticoagulation
Schumacher, William A, Luettgen, Joseph M, Quan, Mimi L, Seiffert, Dietmar A
Published in Arteriosclerosis, thrombosis, and vascular biology (01.03.2010)
Published in Arteriosclerosis, thrombosis, and vascular biology (01.03.2010)
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In vitro, antithrombotic and bleeding time studies of BMS-654457, a small-molecule, reversible and direct inhibitor of factor XIa
Wong, Pancras C., Quan, Mimi L., Watson, Carol A., Crain, Earl J., Harpel, Mark R., Rendina, Alan R., Luettgen, Joseph M., Wexler, Ruth R., Schumacher, William A., Seiffert, Dietmar A.
Published in Journal of thrombosis and thrombolysis (01.11.2015)
Published in Journal of thrombosis and thrombolysis (01.11.2015)
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Discovery of 1-(3‘-Aminobenzisoxazol-5‘-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2‘-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide Hydrochloride (Razaxaban), a Highly Potent, Selective, and Orally Bioavailable Factor Xa Inhibitor
Quan, Mimi L, Lam, Patrick Y. S, Han, Qi, Pinto, Donald J. P, He, Ming Y, Li, Renhua, Ellis, Christopher D, Clark, Charles G, Teleha, Christopher A, Sun, Jung-Hui, Alexander, Richard S, Bai, Steve, Luettgen, Joseph M, Knabb, Robert M, Wong, Pancras C, Wexler, Ruth R
Published in Journal of medicinal chemistry (24.03.2005)
Published in Journal of medicinal chemistry (24.03.2005)
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Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor
Priestley, E. Scott, De Lucca, Indawati, Zhou, Jinglan, Zhou, Jiacheng, Saiah, Eddine, Stanton, Robert, Robinson, Leslie, Luettgen, Joseph M., Wei, Anzhi, Wen, Xiao, Knabb, Robert M., Wong, Pancras C., Wexler, Ruth R.
Published in Bioorganic & medicinal chemistry letters (15.04.2013)
Published in Bioorganic & medicinal chemistry letters (15.04.2013)
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Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor
He, Kan, Luettgen, Joseph M., Zhang, Donglu, He, Bing, Grace, James E., Xin, Baomin, Pinto, Donald J. P., Wong, Pancras C., Knabb, Robert M., Lam, Patrick Y. S., Wexler, Ruth R., Grossman, Scott J.
Published in European journal of drug metabolism and pharmacokinetics (01.09.2011)
Published in European journal of drug metabolism and pharmacokinetics (01.09.2011)
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Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: Discovery of novel, highly potent inhibitors of Factor Xa
Qiao, Jennifer X., Cheney, Daniel L., Alexander, Richard S., Smallwood, Angela M., King, Sarah R., He, Kan, Rendina, Alan R., Luettgen, Joseph M., Knabb, Robert M., Wexler, Ruth R., Lam, Patrick Y.S.
Published in Bioorganic & medicinal chemistry letters (15.07.2008)
Published in Bioorganic & medicinal chemistry letters (15.07.2008)
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Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy
Dilger, Andrew K, Pabbisetty, Kumar B, Corte, James R, De Lucca, Indawati, Fang, Tianan, Yang, Wu, Pinto, Donald J. P, Wang, Yufeng, Zhu, Yeheng, Mathur, Arvind, Li, Jianqing, Hou, Xiaoping, Smith, Daniel, Sun, Dawn, Zhang, Huiping, Krishnananthan, Subramaniam, Wu, Dauh-Rurng, Myers, Joseph E, Sheriff, Steven, Rossi, Karen A, Chacko, Silvi, Zheng, Joanna J, Galella, Michael A, Ziemba, Theresa, Dierks, Elizabeth A, Bozarth, Jeffrey M, Wu, Yiming, Crain, Earl, Wong, Pancras C, Luettgen, Joseph M, Wexler, Ruth R, Ewing, William R
Published in Journal of medicinal chemistry (10.02.2022)
Published in Journal of medicinal chemistry (10.02.2022)
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Factor XIa Inhibitors as New Anticoagulants
Quan, Mimi L, Pinto, Donald J. P, Smallheer, Joanne M, Ewing, William R, Rossi, Karen A, Luettgen, Joseph M, Seiffert, Dietmar A, Wexler, Ruth R
Published in Journal of medicinal chemistry (13.09.2018)
Published in Journal of medicinal chemistry (13.09.2018)
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N-in-1 Dosing Pharmacokinetics in Drug Discovery: Experience, Theoretical and Practical Considerations
He, Kan, Qian, Mingxin, Wong, Harvey, Bai, Stephen A., He, Bing, Brogdon, Bernice, Grace, James E., Xin, Baomin, Wu, Jingtao, Ren, Shelly X., Zeng, Hang, Deng, Yuzhong, Graden, Danielle M., Olah, Timothy V., Unger, Steve E., Luettgen, Joseph M., Knabb, Robert M., Pinto, Donald J., Lam, Patrick Y.S., Duan, James, Wexler, Ruth R., Decicco, Carl P., Christ, David D., Grossman, Scott J.
Published in Journal of pharmaceutical sciences (01.07.2008)
Published in Journal of pharmaceutical sciences (01.07.2008)
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First‐in‐human study to assess the safety, pharmacokinetics and pharmacodynamics of BMS‐962212, a direct, reversible, small molecule factor XIa inhibitor in non‐Japanese and Japanese healthy subjects
Perera, Vidya, Luettgen, Joseph M., Wang, Zhaoqing, Frost, Charles E., Yones, Cynthia, Russo, Cesare, Lee, John, Zhao, Yue, LaCreta, Frank P., Ma, Xuewen, Knabb, Robert M., Seiffert, Dietmar, DeSouza, Mary, Mugnier, Pierre, Cirincione, Brenda, Ueno, Takayo, Frost, Robert J. A.
Published in British journal of clinical pharmacology (01.05.2018)
Published in British journal of clinical pharmacology (01.05.2018)
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Design, structure–activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors
Varnes, Jeffrey G., Wacker, Dean A., Jacobson, Irina C., Quan, Mimi L., Ellis, Christopher D., Rossi, Karen A., He, Ming Y., Luettgen, Joseph M., Knabb, Robert M., Bai, Steven, He, Kan, Lam, Patrick Y.S., Wexler, Ruth R.
Published in Bioorganic & medicinal chemistry (01.12.2007)
Published in Bioorganic & medicinal chemistry (01.12.2007)
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Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker
Corte, James R, Fang, Tianan, Osuna, Honey, Pinto, Donald J. P, Rossi, Karen A, Myers, Joseph E, Sheriff, Steven, Lou, Zhen, Zheng, Joanna J, Harper, Timothy W, Bozarth, Jeffrey M, Wu, Yiming, Luettgen, Joseph M, Seiffert, Dietmar A, Decicco, Carl P, Wexler, Ruth R, Quan, Mimi L
Published in Journal of medicinal chemistry (09.02.2017)
Published in Journal of medicinal chemistry (09.02.2017)
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Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species
Yang, Wu, Wang, Yufeng, Lai, Amy, Clark, Charles G, Corte, James R, Fang, Tianan, Gilligan, Paul J, Jeon, Yoon, Pabbisetty, Kumar B, Rampulla, Richard A, Mathur, Arvind, Kaspady, Mahammed, Neithnadka, Premsai Rai, Arumugam, Arunachalam, Raju, Sivashankaran, Rossi, Karen A, Myers, Joseph E, Sheriff, Steven, Lou, Zhen, Zheng, Joanna J, Chacko, Silvi A, Bozarth, Jeffrey M, Wu, Yiming, Crain, Earl J, Wong, Pancras C, Seiffert, Dietmar A, Luettgen, Joseph M, Lam, Patrick Y. S, Wexler, Ruth R, Ewing, William R
Published in Journal of medicinal chemistry (09.07.2020)
Published in Journal of medicinal chemistry (09.07.2020)
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Journal Article
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups
Corte, James R, Pinto, Donald J. P, Fang, Tianan, Osuna, Honey, Yang, Wu, Wang, Yufeng, Lai, Amy, Clark, Charles G, Sun, Jung-Hui, Rampulla, Richard, Mathur, Arvind, Kaspady, Mahammed, Neithnadka, Premsai Rai, Li, Yi-Xin Cindy, Rossi, Karen A, Myers, Joseph E, Sheriff, Steven, Lou, Zhen, Harper, Timothy W, Huang, Christine, Zheng, Joanna J, Bozarth, Jeffrey M, Wu, Yiming, Wong, Pancras C, Crain, Earl J, Seiffert, Dietmar A, Luettgen, Joseph M, Lam, Patrick Y. S, Wexler, Ruth R, Ewing, William R
Published in Journal of medicinal chemistry (23.01.2020)
Published in Journal of medicinal chemistry (23.01.2020)
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Journal Article
Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors
Hu, Zilun, Wang, Cailan, Han, Wei, Rossi, Karen A., Bozarth, Jeffrey M., Wu, Yiming, Sheriff, Steven, Myers, Joseph E., Luettgen, Joseph M., Seiffert, Dietmar A., Wexler, Ruth R., Quan, Mimi L.
Published in Bioorganic & medicinal chemistry letters (01.04.2018)
Published in Bioorganic & medicinal chemistry letters (01.04.2018)
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