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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Journal Article
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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Preclinical discovery of apixaban, a direct and orally bioavailable factor Xa inhibitor
Wong, Pancras C., Pinto, Donald J. P., Zhang, Donglu
Published in Journal of thrombosis and thrombolysis (01.05.2011)
Published in Journal of thrombosis and thrombolysis (01.05.2011)
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Journal Article
Factor Xa Inhibitors: Next-Generation Antithrombotic Agents
Pinto, Donald J. P, Smallheer, Joanne M, Cheney, Daniel L, Knabb, Robert M, Wexler, Ruth R
Published in Journal of medicinal chemistry (09.09.2010)
Published in Journal of medicinal chemistry (09.09.2010)
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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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Journal Article
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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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
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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Journal Article
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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Journal Article
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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Journal Article
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group
Corte, James R., Fang, Tianan, Pinto, Donald J.P., Orwat, Michael J., Rendina, Alan R., Luettgen, Joseph M., Rossi, Karen A., Wei, Anzhi, Ramamurthy, Vidhyashankar, Myers, Joseph E., Sheriff, Steven, Narayanan, Rangaraj, Harper, Timothy W., Zheng, Joanna J., Li, Yi-Xin, Seiffert, Dietmar A., Wexler, Ruth R., Quan, Mimi L.
Published in Bioorganic & medicinal chemistry (15.05.2016)
Published in Bioorganic & medicinal chemistry (15.05.2016)
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Journal Article
Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties
Orwat, Michael J., Qiao, Jennifer X., He, Kan, Rendina, Alan R., Luettgen, Joseph M., Rossi, Karen A., Xin, Baomin, Knabb, Robert M., Wexler, Ruth R., Lam, Patrick Y. S., Pinto, Donald J. P.
Published in Bioorganic & medicinal chemistry letters (01.08.2014)
Published in Bioorganic & medicinal chemistry letters (01.08.2014)
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Journal Article
Structure–activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors
Varnes, Jeffrey G., Wacker, Dean A., Pinto, Donald J.P., Orwat, Michael J., Theroff, Jay P., Wells, Brian, Galemo, Robert A., Luettgen, Joseph M., Knabb, Robert M., Bai, Steven, He, Kan, Lam, Patrick Y.S., Wexler, Ruth R.
Published in Bioorganic & medicinal chemistry (15.01.2008)
Published in Bioorganic & medicinal chemistry (15.01.2008)
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Journal Article
Structure-Based Design of Novel Guanidine/Benzamidine Mimics: Potent and Orally Bioavailable Factor Xa Inhibitors as Novel Anticoagulants
Lam, Patrick Y. S, Clark, Charles G, Li, Renhua, Pinto, Donald J. P, Orwat, Michael J, Galemmo, Robert A, Fevig, John M, Teleha, Christopher A, Alexander, Richard S, Smallwood, Angela M, Rossi, Karen A, Wright, Matthew R, Bai, Stephen A, He, Kan, Luettgen, Joseph M, Wong, Pancras C, Knabb, Robert M, Wexler, Ruth R
Published in Journal of medicinal chemistry (09.10.2003)
Published in Journal of medicinal chemistry (09.10.2003)
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Journal Article
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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Journal Article
Structure–activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties
Corte, James R., Fang, Tianan, Pinto, Donald J.P., Han, Wei, Hu, Zilun, Jiang, Xiang-Jun, Li, Yun-Long, Gauuan, Jolicia F., Hadden, Mark, Orton, Darren, Rendina, Alan R., Luettgen, Joseph M., Wong, Pancras C., He, Kan, Morin, Paul E., Chang, Chong-Hwan, Cheney, Daniel L., Knabb, Robert M., Wexler, Ruth R., Lam, Patrick Y.S.
Published in Bioorganic & medicinal chemistry letters (01.05.2008)
Published in Bioorganic & medicinal chemistry letters (01.05.2008)
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Journal Article
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties
Pinto, Donald J.P., Galemmo, Robert A., Quan, Mimi L., Orwat, Michael J., Clark, Charles, Li, Renhua, Wells, Brian, Woerner, Francis, Alexander, Richard S., Rossi, Karen A., Smallwood, Angela, Wong, Pancras C., Luettgen, Joseph M., Rendina, Alan R., Knabb, Robert M., He, Kan, Wexler, Ruth R., Lam, Patrick Y.S.
Published in Bioorganic & medicinal chemistry letters (01.11.2006)
Published in Bioorganic & medicinal chemistry letters (01.11.2006)
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Journal Article
Phenyltriazolinones as potent factor Xa inhibitors
Quan, Mimi L., Pinto, Donald J.P., Rossi, Karen A., Sheriff, Steven, Alexander, Richard S., Amparo, Eugene, Kish, Kevin, Knabb, Robert M., Luettgen, Joseph M., Morin, Paul, Smallwood, Angela, Woerner, Francis J., Wexler, Ruth R.
Published in Bioorganic & medicinal chemistry letters (15.02.2010)
Published in Bioorganic & medicinal chemistry letters (15.02.2010)
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Journal Article
Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues
Qiao, Jennifer X., Cheng, Xuhong, Smallheer, Joanne M., Galemmo, Robert A., Drummond, Spencer, Pinto, Donald J.P., Cheney, Daniel L., He, Kan, Wong, Pancras C., Luettgen, Joseph M., Knabb, Robert M., Wexler, Ruth R., Lam, Patrick Y.S.
Published in Bioorganic & medicinal chemistry letters (01.03.2007)
Published in Bioorganic & medicinal chemistry letters (01.03.2007)
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