Discovery of Brivanib Alaninate ((S)-((R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), A Novel Prodrug of... von Cai, Zhen-wei, Zhang, Yongzheng, Borzilleri, Robert M, Qian, Ligang, Barbosa, Stephanie, Wei, Donna, Zheng, Xiaoping, Wu, Lawrence, Fan, Junying, Shi, Zhongping, Wautlet, Barri S, Mortillo, Steve, Jeyaseelan, Robert, Kukral, Daniel W, Kamath, Amrita, Marathe, Punit, D’Arienzo, Celia, Derbin, George, Barrish, Joel C, Robl, Jeffrey A, Hunt, John T, Lombardo, Louis J, Fargnoli, Joseph, Bhide, Rajeev S

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The antiangiogenic activity in xenograft models of brivanib, a dual inhibitor of vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinases von Bhide, Rajeev S, Lombardo, Louis J, Hunt, John T, Cai, Zhen-Wei, Barrish, Joel C, Galbraith, Susan, Jeyaseelan, Sr, Robert, Mortillo, Steven, Wautlet, Barri S, Krishnan, Bala, Kukral, Daniel, Malone, Harold, Lewin, Anne C, Henley, Benjamin J, Fargnoli, Joseph

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Concise and Efficient Synthesis of 4-Fluoro-1H-pyrrolo[2,3-b]pyridine von Thibault, Carl, L'Heureux, Alexandre, Bhide, Rajeev S, Ruel, Réjean

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Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors von Bhide, Rajeev S., Keon, Alec, Weigelt, Carolyn, Sack, John S., Schmidt, Robert J., Lin, Shuqun, Xiao, Hai-Yun, Spergel, Steven H., Kempson, James, Pitts, William J., Carman, Julie, Poss, Michael A.

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Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors von Qin, Lan-Ying, Ruan, Zheming, Cherney, Robert J., Dhar, T.G. Murali, Neels, James, Weigelt, Carolyn A., Sack, John S., Srivastava, Anurag S., Cornelius, Lyndon A.M., Tino, Joseph A., Stefanski, Kevin, Gu, Xiaomei, Xie, Jenny, Susulic, Vojkan, Yang, Xiaoxia, Yarde-Chinn, Melissa, Skala, Stacey, Bosnius, Ruth, Goldstein, Christine, Davies, Paul, Ruepp, Stefan, Salter-Cid, Luisa, Bhide, Rajeev S., Poss, Michael A.

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Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3‑Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders von Liu, Qingjie, Shi, Qing, Marcoux, David, Batt, Douglas G, Cornelius, Lyndon, Qin, Lan-Ying, Ruan, Zheming, Neels, James, Beaudoin-Bertrand, Myra, Srivastava, Anurag S, Li, Ling, Cherney, Robert J, Gong, Hua, Watterson, Scott H, Weigelt, Carolyn, Gillooly, Kathleen M, McIntyre, Kim W, Xie, Jenny H, Obermeier, Mary T, Fura, Aberra, Sleczka, Bogdan, Stefanski, Kevin, Fancher, R. M, Padmanabhan, Shweta, RP, Thatipamula, Kundu, Ipsit, Rajareddy, Kallem, Smith, Rodney, Hennan, James K, Xing, Dezhi, Fan, Jingsong, Levesque, Paul C, Ruan, Qian, Pitt, Sidney, Zhang, Rosemary, Pedicord, Donna, Pan, Jie, Yarde, Melissa, Lu, Hao, Lippy, Jonathan, Goldstine, Christine, Skala, Stacey, Rampulla, Richard A, Mathur, Arvind, Gupta, Anuradha, Arunachalam, Pirama Nayagam, Sack, John S, Muckelbauer, Jodi K, Cvijic, Mary Ellen, Salter-Cid, Luisa M, Bhide, Rajeev S, Poss, Michael A, Hynes, John, Carter, Percy H, Macor, John E, Ruepp, Stefan, Schieven, Gary L, Tino, Joseph A

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Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis von Nair, Satheesh, Kumar, Sreekantha Ratna, Paidi, Venkatram Reddy, Sistla, Ramesh, Kantheti, Durgarao, Polimera, Subba Rao, Thangavel, Soodamani, Mukherjee, Amrita Jha, Das, Mitalee, Bhide, Rajeev S, Pitts, William J, Murugesan, Natesan, Dudhgoankar, Shailesh, Nagar, Jignesh, Subramani, Siva, Mazumder, Debarati, Carman, Julie A, Holloway, Deborah A, Li, Xin, Fereshteh, Mark P, Ruepp, Stefan, Palanisamy, Kamalavenkatesh, Mariappan, T. Thanga, Maddi, Srinivas, Saxena, Ajay, Elzinga, Paul, Chimalakonda, Anjaneya, Ruan, Qian, Ghosh, Kaushik, Bose, Sucharita, Sack, John, Yan, Chunhong, Kiefer, Susan E, Xie, Dianlin, Newitt, John A, Saravanakumar, S. Pon, Rampulla, Richard A, Barrish, Joel C, Carter, Percy H, Hynes, John

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Discovery and SAR of pyrrolo[2,1-f][1,2,4]triazin-4-amines as potent and selective PI3Kδ inhibitors von Bhide, Rajeev S., Neels, James, Qin, Lan-Ying, Ruan, Zheming, Stachura, Sylwia, Weigelt, Carolyn, Sack, John S., Stefanski, Kevin, Gu, Xiaomei, Xie, Jenny H., Goldstine, Christine B., Skala, Stacey, Pedicord, Donna L., Ruepp, Stefan, Dhar, T.G. Murali, Carter, Percy H., Salter-Cid, Luisa M., Poss, Michael A., Davies, Paul

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Design, synthesis, functional and structural characterization of an inhibitor of N-acetylneuraminate-9-phosphate phosphatase: Observation of extensive dynamics in an enzyme/inhibit... von Kim, Soong-Hoon, Constantine, Keith L., Duke, Gerald J., Goldfarb, Valentina, Hunt, John T., Johnson, Stephen, Kish, Kevin, Klei, Herbert E., McDonnell, Patricia A., Metzler, William J., Mueller, Luciano, Poss, Michael A., Fairchild, Craig R., Bhide, Rajeev S.

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Discovery and Evaluation of N-Cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a Selective and Orally Efficacious Inhibitor of V... von Borzilleri, Robert M, Bhide, Rajeev S, Barrish, Joel C, D'Arienzo, Celia J, Derbin, George M, Fargnoli, Joseph, Hunt, John T, Jeyaseelan, Robert, Kamath, Amrita, Kukral, Daniel W, Marathe, Punit, Mortillo, Steve, Qian, Ligang, Tokarski, John S, Wautlet, Barri S, Zheng, Xiaoping, Lombardo, Louis J

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Design, Synthesis, and Evaluation of Orally Active 4-(2,4-Difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as Dual Vascular Endothelial Growth Factor Recepto... von Borzilleri, Robert M, Zheng, Xiaoping, Qian, Ligang, Ellis, Christopher, Cai, Zhen-wei, Wautlet, Barri S, Mortillo, Steve, Jeyaseelan, Robert, Kukral, Daniel W, Fura, Aberra, Kamath, Amrita, Vyas, Viral, Tokarski, John S, Barrish, Joel C, Hunt, John T, Lombardo, Louis J, Fargnoli, Joseph, Bhide, Rajeev S

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Synthesis, SAR, and Evaluation of 4-[2,4-Difluoro-5-(cyclopropylcarbamoyl)phenylamino]pyrrolo[2,1- f][1,2,4]triazine-based VEGFR-2 kinase inhibitors von Cai, Zhen-wei, Wei, Donna, Borzilleri, Robert M., Qian, Ligang, Kamath, Amrita, Mortillo, Steven, Wautlet, Barri, Henley, Benjamin J., Jeyaseelan, Robert, Tokarski, John, Hunt, John T., Bhide, Rajeev S., Fargnoli, Joseph, Lombardo, Louis J.

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Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors von Kim, Kyoung Soon, Lu, Songfeng, Cornelius, Lyndon A., Lombardo, Louis J., Borzilleri, Robert M., Schroeder, Gretchen M., Sheng, Christopher, Rovnyak, George, Crews, Donald, Schmidt, Robert J., Williams, David K., Bhide, Rajeev S., Traeger, Sarah C., McDonnell, Patricia A., Mueller, Luciano, Sheriff, Steven, Newitt, John A., Pudzianowski, Andrew T., Yang, Zheng, Wild, Robert, Lee, Frances Y., Batorsky, Roberta, Ryder, James S., Ortega-Nanos, Marie, Shen, Henry, Gottardis, Marco, Roussell, Deborah L.

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Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1- f][1,2,4]triazine based VEGFR-2 kinase inhibitors von Borzilleri, Robert M., Cai, Zhen-wei, Ellis, Christopher, Fargnoli, Joseph, Fura, Aberra, Gerhardt, Tracy, Goyal, Bindu, Hunt, John T., Mortillo, Steven, Qian, Ligang, Tokarski, John, Vyas, Viral, Wautlet, Barri, Zheng, Xioping, Bhide, Rajeev S.

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Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)- N-(2-methyl-1 H-pyrrolo[2,3- b]pyridin-5-yl)pyrrolo[2,1- f][1,2,4]triazin-4-amine (BMS-645737),... von Ruel, Réjean, Thibeault, Carl, L’Heureux, Alexandre, Martel, Alain, Cai, Zhen-Wei, Wei, Donna, Qian, Ligang, Barrish, Joel C., Mathur, Arvind, D’Arienzo, Celia, Hunt, John T., Kamath, Amrita, Marathe, Punit, Zhang, Yueping, Derbin, George, Wautlet, Barri, Mortillo, Steven, Jeyaseelan, Robert, Henley, Benjamin, Tejwani, Ravindra, Bhide, Rajeev S., Trainor, George L., Fargnoli, Joseph, Lombardo, Louis J.

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Design, synthesis, and structure–activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors von Lombardo, Louis J., Camuso, Amy, Clark, John, Fager, Krista, Gullo-Brown, Johnni, Hunt, John T., Inigo, Ivan, Kan, David, Koplowitz, Barry, Lee, Francis, McGlinchey, Kelly, Qian, Ligang, Ricca, Carolyn, Rovnyak, George, Traeger, Sarah, Tokarski, John, Williams, David K., Wu, Laurence I., Zhao, Yufen, Manne, Veeraswamy, Bhide, Rajeev S.

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Development of Highly Potent Inhibitors of Ras Farnesyltransferase Possessing Cellular and in Vivo Activity von Leftheris, Katerina, Kline, Toni, Vite, Gregory D, Cho, Young H, Bhide, Rajeev S, Patel, Dinesh V, Patel, Manorama M, Schmidt, Robert J, Weller, Harold N, Andahazy, Mary L, Carboni, Joan M, Gullo-Brown, Johnni L, Lee, Francis Y. F, Ricca, Carol, Rose, William C, Yan, Ning, Barbacid, Mariano, Hunt, John T, Meyers, Chester A, Seizinger, Bernd R, Zahler, Robert, Manne, Veeraswamy

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Discovery and Preclinical Studies of (R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an In Vivo Active Potent... von Bhide, Rajeev S, Cai, Zhen-Wei, Zhang, Yong-Zheng, Qian, Ligang, Wei, Donna, Barbosa, Stephanie, Lombardo, Louis J, Borzilleri, Robert M, Zheng, Xiaoping, Wu, Laurence I, Barrish, Joel C, Kim, Soong-Hoon, Leavitt, Kenneth, Mathur, Arvind, Leith, Leslie, Chao, Sam, Wautlet, Barri, Mortillo, Steven, Jeyaseelan, Robert, Kukral, Daniel, Hunt, John T, Kamath, Amrita, Fura, Aberra, Vyas, Viral, Marathe, Punit, D'Arienzo, Celia, Derbin, George, Fargnoli, Joseph

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Discovery of Brivanib Alaninate: A Dual Vascular Endothelial Growth Factor and Fibroblast Growth Factor Receptor Inhibitor von Bhide, Rajeev S, Fargnoli, Joseph

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Concise and Efficient Synthesis of 4-Fluoro-1 H -pyrrolo[2,3- b ]pyridine von Thibault, Carl, L'Heureux, Alexandre, Bhide, Rajeev S., Ruel, Réjean

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