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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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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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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Conformationally Constrained ortho-Anilino Diaryl Ureas: Discovery of 1‑(2-(1′-Neopentylspiro[indoline-3,4′-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a Potent, Selective, and Bioavailable P2Y1 Antagonist
Qiao, Jennifer X, Wang, Tammy C, Ruel, Réjean, Thibeault, Carl, L’Heureux, Alexandre, Schumacher, William A, Spronk, Steven A, Hiebert, Sheldon, Bouthillier, Gilles, Lloyd, John, Pi, Zulan, Schnur, Dora M, Abell, Lynn M, Hua, Ji, Price, Laura A, Liu, Eddie, Wu, Qimin, Steinbacher, Thomas E, Bostwick, Jeffrey S, Chang, Ming, Zheng, Joanna, Gao, Qi, Ma, Baoqing, McDonnell, Patricia A, Huang, Christine S, Rehfuss, Robert, Wexler, Ruth R, Lam, Patrick Y. S
Published in Journal of medicinal chemistry (27.11.2013)
Published in Journal of medicinal chemistry (27.11.2013)
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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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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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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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Triphenylethanamine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors: Discovery of N‑[(1R)‑1-(3-Cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide (BMS-795311)
Qiao, Jennifer X, Wang, Tammy C, Adam, Leonard P, Chen, Alice Ye A, Taylor, David S, Yang, Richard Z, Zhuang, Shaobin, Sleph, Paul G, Li, Julia P, Li, Danshi, Yin, Xiaohong, Chang, Ming, Chen, Xue-Qing, Shen, Hong, Li, Jianqing, Smith, Daniel, Wu, Dauh-Rurng, Leith, Leslie, Harikrishnan, Lalgudi S, Kamau, Muthoni G, Miller, Michael M, Bilder, Donna, Rampulla, Richard, Li, Yi-Xin, Xu, Carrie, Lawrence, R. Michael, Poss, Michael A, Levesque, Paul, Gordon, David A, Huang, Christine S, Finlay, Heather J, Wexler, Ruth R, Salvati, Mark E
Published in Journal of medicinal chemistry (25.11.2015)
Published in Journal of medicinal chemistry (25.11.2015)
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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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Journal Article
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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Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding
Wong, Pancras C, Seiffert, Dietmar, Bird, J Eileen, Watson, Carol A, Bostwick, Jeffrey S, Giancarli, Mary, Allegretto, Nick, Hua, Ji, Harden, David, Guay, Jocelyne, Callejo, Mario, Miller, Michael M, Lawrence, R Michael, Banville, Jacques, Guy, Julia, Maxwell, Brad D, Priestley, E Scott, Marinier, Anne, Wexler, Ruth R, Bouvier, Michel, Gordon, David A, Schumacher, William A, Yang, Jing
Published in Science translational medicine (04.01.2017)
Published in Science translational medicine (04.01.2017)
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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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Phthalazinone-based lactams and cyclic ureas as ROCK2 selective inhibitors
Hu, Zilun, Sitkoff, Doree, Glunz, Peter W., Zou, Yan, Wang, Cailan, Muckelbauer, Jodi K., Adam, Leonard P., Wexler, Ruth R., Quan, Mimi L.
Published in Bioorganic & medicinal chemistry letters (15.05.2023)
Published in Bioorganic & medicinal chemistry letters (15.05.2023)
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Identification of a Hydroxypyrimidinone Compound (21) as a Potent APJ Receptor Agonist for the Potential Treatment of Heart Failure
Meng, Wei, Pi, Zulan, Brigance, Robert, Rossi, Karen A, Schumacher, William A, Bostwick, Jeffrey S, Gargalovic, Peter S, Onorato, Joelle M, Luk, Chiuwa E, Generaux, Claudia N, Wang, Tao, Wexler, Ruth R, Finlay, Heather J
Published in Journal of medicinal chemistry (23.12.2021)
Published in Journal of medicinal chemistry (23.12.2021)
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Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4
Priestley, E. Scott, Banville, Jacques, Deon, Daniel, Dubé, Laurence, Gagnon, Marc, Guy, Julia, Lapointe, Philippe, Lavallée, Jean-François, Martel, Alain, Plamondon, Serge, Rémillard, Roger, Ruediger, Edward, Tremblay, François, Posy, Shana L., Guarino, Victor R., Richter, Jeremy M., Li, Jianqing, Gupta, Anuradha, Vetrichelvan, Muthalagu, Balapragalathan, T. J., Mathur, Arvind, Hua, Ji, Callejo, Mario, Guay, Jocelyne, Sum, Chi Shing, Cvijic, Mary Ellen, Watson, Carol, Wong, Pancras, Yang, Jing, Bouvier, Michel, Gordon, David A., Wexler, Ruth R., Marinier, Anne
Published in Journal of medicinal chemistry (14.07.2022)
Published in Journal of medicinal chemistry (14.07.2022)
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