未登录 XPO1-Targeting Selective Inhibitors of Transcriptional Activation Suppress Graft-versus-Host Disease XPO1靶向选择性转录激活抑制剂可抑制移植物抗宿主病 Shen, Yanqiu; Chen, Yi Fan; Yan, David F.; Contreras, Lyannah A.; Petroze, Frederick N.; Srinivasan, Ramya; Farrar, Amanda N.; Trainor, George L.; Desai, Amar B.; Adams, Drew J. 分享 收藏
Discovery and Optimization of Novel Pyrazolopyrimidines as Potent and Orally Bioavailable Allosteric HIV-1 Integrase Inhibitors Li, Guo; Meanwell, Nicholas A.; Krystal, Mark R.; Langley, David R.; Naidu, B. Narasimhulu; Sivaprakasam, Prasanna; Lewis, Hal; Kish, Kevin; Khan, Javed A.; Ng, Alicia; Trainor, George L.; Cianci, Christopher; Dicker, Ira B.; Walker, Michael A.; Lin, Zeyu; Protack, Tricia; Discotto, Linda; Jenkins, Susan; Gerritz, Samuel W.; Pendri, Annapurna 分享 收藏
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Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer 用于治疗前列腺癌的选择性CYP17A1裂解酶抑制剂BMS-351的发现 Huang, Audris; Jayaraman, Lata; Fura, Aberra; Vite, Gregory D.; Trainor, George L.; Gottardis, Marco M.; Spires, Thomas E.; Spires, Vanessa M.; Rizzo, Cheryl A.; Obermeier, Mary T.; Elzinga, Paul A.; Todderud, Gordon; Fan, Yi; Newitt, John A.; Beyer, Sophie M.; Zhu, Yongxin; Warrack, Bethanne M.; Goodenough, Angela K.; Tebben, Andrew J.; Doweyko, Arthur M.; Gold, David L.; Balog, Aaron 分享 收藏
Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors Hart, Amy C.; Schroeder, Gretchen M.; Wan, Honghe; Grebinski, James; Inghrim, Jennifer; Kempson, James; Guo, Junqing; Pitts, William J.; Tokarski, John S.; Sack, John S.; Khan, Javed A.; Lippy, Jonathan; Lorenz, Matthew V.; You, Dan; McDevitt, Theresa; Vuppugalla, Ragini; Zhang, Yueping; Lombardo, Louis J.; Trainor, George L.; Purandare, Ashok V. 分享 收藏
Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms Wan, Honghe; Schroeder, Gretchen M.; Hart, Amy C.; Inghrim, Jennifer; Grebinski, James; Tokarski, John S.; Lorenz, Matthew V.; You, Dan; Mcdevie, Theresa; Penhallow, Becky; Vuppugalla, Ragini; Zhang, Yueping; Gu, Xiaomei; Iyer, Ramaswamy; Lombardo, Louis J.; Trainor, George L.; Ruepp, Stefan; Lippy, Jonathan; Blat, Yuval; Sack, John S.; Khan, Javed A.; Stefanski, Kevin; Sleczka, Bogdan; Mathur, Arvind; Sun, Jung-Hui; Wong, Michael K.; Wu, Dauh-Rurng; Li, Peng; Gupta, Anuradha; Arunachalam, P. N.; Pragalathan, Bala; Narayanan, Sankara; Nanjundaswamy, K. C.; Kuppusamy, Prakasam; Purandare, Ashok V. 分享 收藏
Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer Balog, Aaron; Rampulla, Richard; Martin, Gregory S.; Krystek, Stanley R.; Attar, Ricardo; Dell-John, Janet; DiMarco, John D.; Fairfax, David; Gougoutas, Jack; Hoist, Christian L.; Nation, Andrew; Rizzo, Cheryl; Rossiter, Lana M.; Schweizer, Liang; Shan, Weifang; Spergel, Steven; Spires, Thomas; Cornelius, Georgia; Gottardis, Marco; Trainor, George; Vite, Gregory D.; Salvatit, Mark E. 分享 收藏
Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors Gavai, Ashvinikumar V.; Quesnelle, Claude; Norris, Derek; Han, Wen-Ching; Gill, Patrice; Shan, Weifang; Balog, Aaron; Chen, Ke; Tebben, Andrew; Rampulla, Richard; Wu, Dauh-Rurng; Zhang, Yingru; Mathur, Arvind; White, Ronald; Rose, Anne; Wang, Haiqing; Yang, Zheng; Ranasinghe, Asoka; D'Arienzo, Celia; Guarino, Victor; Xiao, Lan; Su, Ching; Everlof, Gerry; Arora, Vinod; Shen, Ding Ren; Cvijic, Mary Ellen; Menard, Krista; Wen, Mei-Li; Meredith, Jere; Trainor, George; Lombardo, Louis J.; Olson, Richard; Baran, Phil S.; Hunt, John T.; Vite, Gregory D.; Fischer, Bruce S.; Westhouse, Richard A.; Lee, Francis Y. 分享 收藏
BMS-983970, an oral pan-Notch inhibitor for the treatment of cancer Gavai, Ashvinikumar V.; Zhao, Yufen; O'Malley, Daniel; Fink, Brian; Quesnelle, Claude; Norris, Derek; Chen, Libing; Kim, Soong-Hoon; Han, Wen-Ching; Gill, Patrice; Shan, Weifang; Balog, Aaron; Tebben, Andrew; Rampulla, Richard; Wu, Dauh-Rurng; Zhang, Yingru; Mathur, Arvind; Wang, Haiqing; Yang, Zheng; Ruan, Qian; Moore, Robin; Rodrigues, David; Ranasinghe, Asoka; D'Arienzo, Celia; Tye, Ching Kim; Su, Ching; Everlof, Gerry; Yarde, Melissa; Cvijic, Mary Ellen; Menard, Krista; Wen, Mei-Li; Trainor, George; Fischer, Bruce; Hunt, John; Vite, Gregory; Westhouse, Richard; Lee, Francis 分享 收藏
Biochemical and transcriptional profiling to triage additional activities in a series of IGF-1R/IR inhibitors Ross-Macdonald, Petra; de Silva, Heshani; Patel, Vishal; Amy Truong; He, Aiqing; Neuhaus, Isaac; Tilford, Charles; Ji, RuiRu; Siemers, Nathan; Greer, Ann; Carboni, Joan; Gottardis, Marco; Menard, Krista; Lee, Frank; Dodier, Marco; Frennesson, David; Sampognaro, Anthony; Saulnier, Mark; Trainor, George; Vyas, Dolatrai; Zimmermann, Kurt; Wittman, Mark 分享 收藏
Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2 Purandare, A. V.; McDevitt, T. M.; Wan, H.; You, D.; Penhallow, B.; Han, X.; Vuppugalla, R.; Zhang, Y.; Ruepp, S. U.; Trainor, G. L.; Lombardo, L.; Pedicord, D.; Gottardis, M. M.; Ross-Macdonald, P.; de Silva, H.; Hosbach, J.; Emanuel, S. L.; Blat, Y.; Fitzpatrick, E.; Taylor, T. L.; McIntyre, K. W.; Michaud, E.; Mulligan, C.; Lee, F. Y.; Woolfson, A.; Lasho, T. L.; Pardanani, A.; Tefferi, A.; Lorenzi, M. V. 分享 收藏
Discovery of BMS-911543, a highly selective JAK2 inhibitor, as a clinical candidate for the treatment of myeloproliferative disease and other malignancies Purandare, Ashok V.; Wan, Honghe; Schroeder, Gretchen; Hart, Amy; Grebinski, James; Inghrim, Jennifer; Tokarski, John; You, Dan; Penhallow, Becky; McDevitt, Theresa; Vuppugalla, Ragini; Zhang, Yueping; Ruepp, Stefan; Trainor, George; Han, Xia; Lombardo, Louis; Lee, Francis Y.; Gottardis, Marco; Hosbach, Jennifer; Fitzpatrick, Elizabeth; Emanuel, Stuart; Pardanani, Animesh; Lasho, Terra L.; Tefferi, Ayalew; Lorenzi, Matthew V. 分享 收藏
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BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR Carboni, Joan M.; Wittman, Mark; Yang, Zheng; Lee, Francis; Greer, Ann; Hurlburt, Warren; Hillerman, Stephen; Cao, Carolyn; Cantor, Glenn H.; Dell-John, Janet; Chen, Cliff; Discenza, Lorell; Menard, Krista; Li, Aixin; Trainor, George; Vyas, Dolatrai; Kramer, Robert; Attar, Ricardo M.; Gottardis, Marco M. 分享 收藏
Discovery of a 2,4-Disubstituted Pyrrolo[1,2-f][1,2,4]triazine Inhibitor (BMS-754807) of Insulin-like Growth Factor Receptor (IGF-1R) Kinase in Clinical Development Wittman, Mark D.; Carboni, Joan M.; Yang, Zheng; Lee, Francis Y.; Antman, Melissa; Attar, Ricardo; Balimane, Praveen; Chang, Chiehying; Chen, Cliff; Discenza, Lorell; Frennesson, David; Gottardis, Marco M.; Greer, Ann; Hurlburt, Warren; Johnson, Walter; Langley, David R.; Li, Aixin; Li, Jianqing; Liu, Peiying; Mastalerz, Harold; Mathur, Arvind; Menard, Krista; Patel, Karishma; Sack, John; Sang, Xiaopeng; Saulnier, Mark; Smith, Daniel; Stefanski, Kevin; Trainor, George; Velaparthi, Upender; Zhang, Guifen; Zimmermann, Kurt; Vyas, Dolatrai M. 分享 收藏
Synthesis and Structure-Activity Relationships of 8-(Pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: Potent, Orally Bioavailable Corticotropin Releasing Factor Receptor-1 (CRF1) Antagonists Gilligan, Paul J.; Clarke, Todd; He, Liqi; Lelas, Snjezana; Li, Yu-Wen; Heman, Karen; Fitzgerald, Lawrence; Miller, Keith; Zhang, Ge; Marshall, Anne; Krause, Carol; McElroy, John F.; Ward, Kathyrn; Zeller, Kim; Wong, Harvey; Bai, Steven; Saye, Joanne; Grossman, Scott; Zaczek, Robert; Arneric, Stephen P.; Hartig, Paul; Robertson, David; Trainor, George 分享 收藏
8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines: Selective and Centrally Active Corticotropin-Releasing Factor Receptor-1 (CRF1) Antagonists Gilligan, Paul J.; He, Liqi; Clarke, Todd; Tivitmahaisoon, Parcharee; Lelas, Snjezana; Li, Yu-Wen; Heman, Karen; Fitzgerald, Lawrence; Miller, Keith; Zhang, Ge; Marshall, Anne; Krause, Carol; McElroy, John; Ward, Kathyrn; Shen, Helen; Wong, Harvey; Grossman, Scott; Nemeth, Gregory; Zaczek, Robert; Arneric, Stephen P.; Hartig, Paul; Robertson, David W.; Trainor, George 分享 收藏
Discovery of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily Schroeder, Gretchen M.; An, Yongmi; Cai, Zhen-Wei; Chen, Xiao-Tao; Clark, Cheryl; Cornelius, Lyndon A. M.; Dai, Jun; Gullo-Brown, Johnni; Gupta, Ashok; Henley, Benjamin; Hunt, John T.; Jeyaseelan, Robert; Kamath, Amrita; Kim, Kyoung; Lippy, Jonathan; Lombardo, Louis J.; Manne, Veeraswamy; Oppenheimer, Simone; Sack, John S.; Schmidt, Robert J.; Shen, Guoxiang; Stefanski, Kevin; Tokarski, John S.; Trainor, George L.; Wautlet, Barri S.; Wei, Donna; Williams, David K.; Zhang, Yingru; Zhang, Yueping; Fargnoli, Joseph; Borzilleri, Robert M. 分享 收藏
Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoro-propyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity Velaparthi, Upender; Wittman, Mark; Liu, Peiying; Carboni, Joan M.; Lee, Francis Y.; Attar, Ricardo; Balimane, Praveen; Clarke, Wendy; Sinz, Michael W.; Hurlburt, Warren; Patel, Karishma; Discenza, Lorell; Kim, Sean; Gottardis, Marco; Greer, Ann; Li, Aixin; Saulnier, Mark; Yang, Zheng; Zimmermann, Kurt; Trainor, George; Vyas, Dolatrai 分享 收藏
Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: Synthesis, X-ray crystallographic analysis, and biological activities Kim, Kyoung Soon; Zhang, Liping; Schmidt, Robert; Cai, Zhen-Wei; Wei, Donna; Williams, David K.; Lombardo, Louis J.; Trainor, George L.; Xie, Dianlin; Zhang, Yaquan; An, Yongmi; Sack, John S.; Tokarski, John S.; Darienzo, Celia; Kamath, Amrita; Marathe, Punit; Zhang, Yueping; Lippy, Jonathan; Jeyaseelan, Robert, Sr.; Wautlet, Barri; Henley, Benjamin; Gullo-Brown, Johnni; Manne, Veeraswamy; Hunt, John T.; Fargnoli, Joseph; Borzilleri, Robert M. 分享 收藏
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