Preclinical Characteristics of the Hepatitis C Virus NS3/4A Protease Inhibitor ITMN-191 (R7227) von Seiwert, Scott D, Andrews, Steven W, Jiang, Yutong, Serebryany, Vladimir, Tan, Hua, Kossen, Karl, Rajagopalan, P T Ravi, Misialek, Shawn, Stevens, Sarah K, Stoycheva, Antitsa, Hong, Jin, Lim, Sharlene R, Qin, Xiaoli, Rieger, Robert, Condroski, Kevin R, Zhang, Hailong, Do, Mary Geck, Lemieux, Christine, Hingorani, Gary P, Hartley, Dylan P, Josey, John A, Pan, Lin, Beigelman, Leonid, Blatt, Lawrence M

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Phase I Dose-Escalation Trial of PT2385, a First-in-Class Hypoxia-Inducible Factor-2α Antagonist in Patients With Previously Treated Advanced Clear Cell Renal Cell Carcinoma von Courtney, Kevin D, Infante, Jeffrey R, Lam, Elaine T, Figlin, Robert A, Rini, Brian I, Brugarolas, James, Zojwalla, Naseem J, Lowe, Ann M, Wang, Keshi, Wallace, Eli M, Josey, John A, Choueiri, Toni K

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On-target efficacy of a HIF-2α antagonist in preclinical kidney cancer models von Cho, Hyejin, Du, Xinlin, Rizzi, James P., Liberzon, Ella, Chakraborty, Abhishek A., Gao, Wenhua, Carvo, Ingrid, Signoretti, Sabina, Bruick, Richard K., Josey, John A., Wallace, Eli M., Kaelin, William G.

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Targeting renal cell carcinoma with a HIF-2 antagonist von Chen, Wenfang, Hill, Haley, Christie, Alana, Kim, Min Soo, Holloman, Eboni, Pavia-Jimenez, Andrea, Homayoun, Farrah, Ma, Yuanqing, Patel, Nirav, Yell, Paul, Hao, Guiyang, Yousuf, Qurratulain, Joyce, Allison, Pedrosa, Ivan, Geiger, Heather, Zhang, He, Chang, Jenny, Gardner, Kevin H., Bruick, Richard K., Reeves, Catherine, Hwang, Tae Hyun, Courtney, Kevin, Frenkel, Eugene, Sun, Xiankai, Zojwalla, Naseem, Wong, Tai, Rizzi, James P., Wallace, Eli M., Josey, John A., Xie, Yang, Xie, Xian-Jin, Kapur, Payal, McKay, Renée M., Brugarolas, James

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3‑[(1S,2S,3R)‑2,3-Difluoro-1-hydroxy-7-methylsulfonyl­indan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell... von Xu, Rui, Wang, Keshi, Rizzi, James P, Huang, Heli, Grina, Jonas A, Schlachter, Stephen T, Wang, Bin, Wehn, Paul M, Yang, Hanbiao, Dixon, Darryl D, Czerwinski, Robert M, Du, Xinlin, Ged, Emily L, Han, Guangzhou, Tan, Huiling, Wong, Tai, Xie, Shanhai, Josey, John A, Wallace, Eli M

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A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma von Wallace, Eli M, Rizzi, James P, Han, Guangzhou, Wehn, Paul M, Cao, Zhaodan, Du, Xinlin, Cheng, Tzuling, Czerwinski, Robert M, Dixon, Darryl D, Goggin, Barry S, Grina, Jonas A, Halfmann, Megan M, Maddie, Melissa A, Olive, Sarah R, Schlachter, Stephen T, Tan, Huiling, Wang, Bin, Wang, Keshi, Xie, Shanhai, Xu, Rui, Yang, Hanbiao, Josey, John A

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Discovery of (1S,2R,3R)-2,3-Dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: Novel and Highly Selective Aggrecanase Inhibitors von Shiozaki, Makoto, Maeda, Katsuya, Miura, Tomoya, Kotoku, Masayuki, Yamasaki, Takayuki, Matsuda, Isamu, Aoki, Kenta, Yasue, Katsutaka, Imai, Hiroto, Ubukata, Minoru, Suma, Akira, Yokota, Masahiro, Hotta, Takahiro, Tanaka, Masahiro, Hase, Yasunori, Haas, Julia, Fryer, Andrew M, Laird, Ellen R, Littmann, Nicole M, Andrews, Steven W, Josey, John A, Mimura, Takayuki, Shinozaki, Yuichi, Yoshiuchi, Hiromi, Inaba, Takashi

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Identification of 4-Aminopyrazolylpyrimidines as Potent Inhibitors of Trk Kinases von Wang, Tao, Lamb, Michelle L, Scott, David A, Wang, Haixia, Block, Michael H, Lyne, Paul D, Lee, John W, Davies, Audrey M, Zhang, Hai-Jun, Zhu, Yanyi, Gu, Fei, Han, Yongxin, Wang, Bin, Mohr, Peter J, Kaus, Robert J, Josey, John A, Hoffmann, Ethan, Thress, Ken, MacIntyre, Terry, Wang, Haiyun, Omer, Charles A, Yu, Dingwei

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Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S)‑3-((2,2-Di... von Wehn, Paul M, Rizzi, James P, Dixon, Darryl D, Grina, Jonas A, Schlachter, Stephen T, Wang, Bin, Xu, Rui, Yang, Hanbiao, Du, Xinlin, Han, Guangzhou, Wang, Keshi, Cao, Zhaodan, Cheng, Tzuling, Czerwinski, Robert M, Goggin, Barry S, Huang, Heli, Halfmann, Megan M, Maddie, Melissa A, Morton, Emily L, Olive, Sarah R, Tan, Huiling, Xie, Shanhai, Wong, Tai, Josey, John A, Wallace, Eli M

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Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-D... von Wehn, Paul M, Rizzi, James P, Dixon, Darryl D, Grina, Jonas A, Schlachter, Stephen T, Wang, Bin, Xu, Rui, Yang, Hanbiao, Du, Xinlin, Han, Guangzhou, Wang, Keshi, Cao, Zhaodan, Cheng, Tzuling, Czerwinski, Robert M, Goggin, Barry S, Huang, Heli, Halfmann, Megan M, Maddie, Melissa A, Morton, Emily L, Olive, Sarah R, Tan, Huiling, Xie, Shanhai, Wong, Tai, Josey, John A, Wallace, Eli M

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A New Resin-Bound Universal Isonitrile for the Ugi 4CC Reaction:  Preparation and Applications to the Synthesis of 2,5-Diketopiperazines and 1,4-Benzodiazepine-2,5-diones von Kennedy, April L, Fryer, Andrew M, Josey, John A

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A Nucleic Acid Triple Helix Formed by a Peptide Nucleic Acid-DNA Complex von Betts, Laurie, Josey, John A., Veal, James M., Jordan, Steven R.

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Discovery of Danoprevir (ITMN-191/R7227), a Highly Selective and Potent Inhibitor of Hepatitis C Virus (HCV) NS3/4A Protease von Jiang, Yutong, Andrews, Steven W., Condroski, Kevin R., Buckman, Brad, Serebryany, Vlad, Wenglowsky, Steve, Kennedy, April L., Madduru, Machender R., Wang, Bin, Lyon, Michael, Doherty, George A., Woodard, Benjamin T., Lemieux, Christine, Do, Mary Geck, Zhang, Hailong, Ballard, Joshua, Vigers, Guy, Brandhuber, Barbra J., Stengel, Peter, Josey, John A., Beigelman, Leonid, Blatt, Lawrence, Seiwert, Scott D.

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Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors von SHIOZAKI, Makoto, MAEDA, Katsuya, MIMURA, Takayuki, SHINOZAKI, Yuichi, YOSHIUCHI, Hiromi, INABA, Takashi, MIURA, Tomoya, OGOSHI, Yosuke, HAAS, Julia, FRYER, Andrew M, LAIRD, Ellen R, LITTMANN, Nicole M, ANDREWS, Steven W, JOSEY, John A

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Lead change of a HIF-2α antagonist guided by multiparameter optimization and utilization of an Olp→πAr interaction von Wehn, Paul M., Yang, Song, Grina, Jonas A., Rizzi, James P., Schlachter, Stephen T., Wang, Bin, Xu, Rui, Yang, Hanbiao, Du, Xinlin, Han, Guangzhou, Wang, Keshi, Czerwinski, Robert M., Ged, Emily L., Huang, Heli, Halfmann, Megan M., Maddie, Melissa A., Morton, Emily R., Olive, Sarah R., Tan, Huiling, Xie, Shanhai, Josey, John A., Wallace, Eli M.

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3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymerase von Hendricks, Robert T., Spencer, Stacey R., Blake, James F., Fell, Jay B., Fischer, John P., Stengel, Peter J., Leveque, Vincent J.P., LePogam, Sophie, Rajyaguru, Sonal, Najera, Isabel, Josey, John A., Swallow, Steven

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General Method for the Synthesis of Phospholipid Derivatives of 1,2-O-Diacyl-sn-Glycerols von Martin, Stephen F, Josey, John A, Wong, Yue-Ling, Dean, Daniel W

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Discovery of Disubstituted Imidazo[4,5‑b]pyridines and Purines as Potent TrkA Inhibitors von Wang, Tao, Lamb, Michelle L, Block, Michael H, Davies, Audrey Molina, Han, Yongxin, Hoffmann, Ethan, Ioannidis, Stephanos, Josey, John A, Liu, Zhong-Ying, Lyne, Paul D, MacIntyre, Terry, Mohr, Peter J, Omer, Charles A, Sjögren, Tove, Thress, Kenneth, Wang, Bin, Wang, Haiyun, Yu, Dingwei, Zhang, Hai-Jun

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Non-nucleoside inhibitors of HCV NS5B polymerase. Part 1: Synthetic and computational exploration of the binding modes of benzothiadiazine and 1,4-benzothiazine HCV NS5b polymerase... von Hendricks, Robert T., Fell, Jay B., Blake, James F., Fischer, John P., Robinson, John E., Spencer, Stacey R., Stengel, Peter J., Bernacki, April L., Leveque, Vincent J.P., Pogam, Sophie Le, Rajyaguru, Sonal, Najera, Isabel, Josey, John A., Harris, Jason R., Swallow, Steven

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Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors von Shiozaki, Makoto, Imai, Hiroto, Maeda, Katsuya, Miura, Tomoya, Yasue, Katsutaka, Suma, Akira, Yokota, Masahiro, Ogoshi, Yosuke, Haas, Julia, Fryer, Andrew M., Laird, Ellen R., Littmann, Nicole M., Andrews, Steven W., Josey, John A., Mimura, Takayuki, Shinozaki, Yuichi, Yoshiuchi, Hiromi, Inaba, Takashi

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