Tissue factor–fVIIa inhibition: update on an unfinished quest for a novel oral antithrombotic von Priestley, E. Scott

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Discovery of Potent, Highly Selective, and Efficacious SMARCA2 Degraders von Li, Zhenwu, Harikrishnan, Lalgudi S, Xu, Guozhang, Samanta, Debangshu, Clemente, Jose C, Leng, Lingying, Tu, Wenbin, Yang, Lin, Huang, Liyue, Wang, Mi, Wang, Shaomeng, Deng, Qiaolin, Behshad, Elham, Nagilla, Rakesh, Orth, Peter, Rice, Cory, Strickland, Corey, Mohammad, Helai P, Priestley, E Scott, Sui, Zhihua

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Discovery of ERD-1233 as a Potent and Orally Efficacious Estrogen Receptor PROTAC Degrader for the Treatment of ER+ Human Breast Cancer von Acharyya, Ranjan Kumar, Rej, Rohan Kalyan, Hu, Biao, Chen, Zhixiang, Wu, Dimin, Lu, Jianfeng, Metwally, Hoda, McEachern, Donna, Wang, Yu, Jiang, Wei, Bai, Longchuan, Tošović, Jelena, Gersch, Christina L., Xu, Guozhang, Zhang, Weihong, Wu, WenXue, Priestley, E. Scott, Sui, Zhihua, Sarkari, Farzad, Wen, Bo, Sun, Duxin, Rae, James M., Wang, Shaomeng

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Discovery of Potent and Selective Quinoxaline-Based Protease-Activated Receptor 4 (PAR4) Antagonists for the Prevention of Arterial Thrombosis von Zhang, Xiaojun, Jiang, Wen, Richter, Jeremy M., Bates, J. Alex, Reznik, Samuel K., Stachura, Sylwia, Rampulla, Richard, Doddalingappa, Dyamanna, Ulaganathan, Sankar, Hua, Ji, Bostwick, Jeffrey S., Sum, Chi, Posy, Shana, Malmstrom, Sarah, Dickey, Joyce, Harden, David, Lawrence, R. Michael, Guarino, Victor R., Schumacher, William A., Wong, Pancras, Yang, Jing, Gordon, David A., Wexler, Ruth R., Priestley, E. Scott

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Discovery of ERD-12310A as an Exceptionally Potent and Orally Efficacious PROTAC Degrader of Estrogen Receptor α (ERα) von Rej, Rohan Kalyan, Hu, Biao, Chen, Zhixiang, Acharyya, Ranjan Kumar, Wu, Dimin, Metwally, Hoda, McEachern, Donna, Wang, Yu, Jiang, Wei, Bai, Longchuan, Nishimura, Leticia S, Gersch, Christina L., Wang, Meilin, Wen, Bo, Sun, Duxin, Carlson, Kathryn, Katzenellenbogen, John A., Xu, Guozhang, Zhang, Weihong, Wu, Wenxue, Priestley, E. Scott, Sui, Zhihua, Rae, James M., Wang, Shaomeng

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Microscale purification in support of high-throughput medicinal chemistry von Barhate, Chandan L, Donnell, Andrew F, Davies, Merrill, Li, Ling, Zhang, Yong, Yang, Fukang, Black, Regina, Zipp, Greg, Zhang, Yingru, Cavallaro, Cullen L, Priestley, E. Scott, Weller, Harold N

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Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4 von 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

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Discovery of BMS-986308: A Renal Outer Medullary Potassium Channel Inhibitor for the Treatment of Heart Failure von Richter, Jeremy M., Gunaga, Prashantha, Yadav, Navnath, Bora, Rajesh Onkardas, Bhide, Rajeev, Rajugowda, Nagendra, Govindrajulu, Kavitha, Godesi, Sreenivasulu, Akuthota, Nagarjuna, Rao, Prasanna, Sivaraman, Aneesh, Panda, Manoranjan, Kaspady, Mahammed, Gupta, Anuradha, Mathur, Arvind, Levesque, Paul C., Gulia, Jyoti, Dokania, Manoj, Ramarao, Manjunath, Kole, Prashant, Chacko, Silvi, Lentz, Kimberley A., Sivaprasad LVJ, Sankara, Thatipamula, Rajendra Prasad, Sridhar, Srikanth, Kamble, Shyam, Govindrajan, Arun, Soleman, Sharif I., Gordon, David A., Wexler, Ruth R., Priestley, E. Scott

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Atropisomer Control in Macrocyclic Factor VIIa Inhibitors von Glunz, Peter W, Mueller, Luciano, Cheney, Daniel L, Ladziata, Vladimir, Zou, Yan, Wurtz, Nicholas R, Wei, Anzhi, Wong, Pancras C, Wexler, Ruth R, Priestley, E. Scott

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Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors von Priestley, E. Scott, Cheney, Daniel L, DeLucca, Indawati, Wei, Anzhi, Luettgen, Joseph M, Rendina, Alan R, Wong, Pancras C, Wexler, Ruth R

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Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor von 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.

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Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy von Miller, Michael M, Banville, Jacques, Friends, Todd J, Gagnon, Mark, Hangeland, Jon J, Lavallée, Jean-François, Martel, Alain, O’Grady, Harold, Rémillard, Roger, Ruediger, Edward, Tremblay, François, Posy, Shana L, Allegretto, Nick J, Guarino, Victor R, Harden, David G, Harper, Timothy W, Hartl, Karen, Josephs, Jonathan, Malmstrom, Sarah, Watson, Carol, Yang, Yanou, Zhang, Ge, Wong, Pancras, Yang, Jing, Bouvier, Michel, Seiffert, Dietmar A, Wexler, Ruth R, Lawrence, R. Michael, Priestley, E. Scott, Marinier, Anne

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The Synthesis and evaluation of a novel class of ( E)-3-(1-cyclohexyl-1 H-pyrazol-3-yl)-2-methylacrylic acid Hepatitis C virus polymerase NS5B inhibitors von Martin, Scott W., Glunz, Peter, Beno, Brett R., Bergstrom, Carl, Romine, Jeffrey L., Scott Priestley, E., Newman, Makenzie, Gao, Min, Roberts, Susan, Rigat, Karen, Fridell, Robert, Qiu, Dike, Knobloh, Galina, Wang, Ying-Kai

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Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa–Tissue Factor Complex von Zhang, Xiaojun, Glunz, Peter W, Johnson, James A, Jiang, Wen, Jacutin-Porte, Swanee, Ladziata, Vladimir, Zou, Yan, Phillips, Monique S, Wurtz, Nicholas R, Parkhurst, Brandon, Rendina, Alan R, Harper, Timothy M, Cheney, Daniel L, Luettgen, Joseph M, Wong, Pancras C, Seiffert, Dietmar, Wexler, Ruth R, Priestley, E. Scott

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Correction to “Atropisomer Control in Macrocyclic Factor VIIa Inhibitors” von Glunz, Peter W, Mueller, Luciano, Cheney, Daniel L, Ladziata, Vladimir, Zou, Yan, Wurtz, Nicholas R, Wei, Anzhi, Wong, Pancras C, Wexler, Ruth R, Priestley, E. Scott

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Discovery of Novel P1 Groups for Coagulation Factor VIIa Inhibition Using Fragment-Based Screening von Cheney, Daniel L, Bozarth, Jeffrey M, Metzler, William J, Morin, Paul E, Mueller, Luciano, Newitt, John A, Nirschl, Alexandra H, Rendina, Alan R, Tamura, James K, Wei, Anzhi, Wen, Xiao, Wurtz, Nicholas R, Seiffert, Dietmar A, Wexler, Ruth R, Priestley, E. Scott

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Neutral macrocyclic factor VIIa inhibitors von Wurtz, Nicholas R., Parkhurst, Brandon L., DeLucca, Indawati, Glunz, Peter W., Jiang, Wen, Zhang, Xiaojun, Cheney, Daniel L., Bozarth, Jeffrey M., Rendina, Alan R., Wei, Anzhi, Harper, Tim, Luettgen, Joseph M., Wu, Yiming, Wong, Pancras C., Seiffert, Dietmar A., Wexler, Ruth R., Priestley, E. Scott

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Synthesis and P1′ SAR exploration of potent macrocyclic tissue factor-factor VIIa inhibitors von Ladziata, Vladimir (Uladzimir), Glunz, Peter W., Zou, Yan, Zhang, Xiaojun, Jiang, Wen, Jacutin-Porte, Swanee, Cheney, Daniel L., Wei, Anzhi, Luettgen, Joseph M., Harper, Timothy M., Wong, Pancras C., Seiffert, Dietmar, Wexler, Ruth R., Priestley, E. Scott

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BMS-593214, an active site-directed factor VIIa inhibitor: Enzyme kinetics, antithrombotic and antihaemostatic studies von Wong, Pancras C., Luettgen, Joseph M., Rendina, Alan R., Kettner, Charles A., Xin, Baomin, Knabb, Robert M., Wexler, Ruth R., Priestley, E. Scott

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Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF–FVIIa inhibitors von Zhang, Xiaojun, Glunz, Peter W., Jiang, Wen, Schmitt, Aaron, Newman, Makenzie, Barbera, Frank A., Bozarth, Jeffery M., Rendina, Alan R., Wei, Anzhi, Wen, Xiao, Rossi, Karen A., Luettgen, Joseph M., Wong, Pancras C., Knabb, Robert M., Wexler, Ruth R., Scott Priestley, E.

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