Preclinical Characteristics of the Hepatitis C Virus NS3/4A Protease Inhibitor ITMN-191 (R7227)
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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Published in Antimicrobial Agents and Chemotherapy (01.12.2008)
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Published in Journal of medicinal chemistry (28.04.2011)
Published in Journal of medicinal chemistry (28.04.2011)
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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
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Published in Journal of clinical oncology (20.03.2018)
Published in Journal of clinical oncology (20.03.2018)
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Published in Nature (London) (03.11.2016)
Published in Nature (London) (03.11.2016)
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Identification of 4-Aminopyrazolylpyrimidines as Potent Inhibitors of Trk Kinases
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
Published in Journal of medicinal chemistry (14.08.2008)
Published in Journal of medicinal chemistry (14.08.2008)
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Targeting renal cell carcinoma with a HIF-2 antagonist
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
Published in Nature (London) (03.11.2016)
Published in Nature (London) (03.11.2016)
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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 Renal Cell Carcinoma
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
Published in Journal of medicinal chemistry (08.08.2019)
Published in Journal of medicinal chemistry (08.08.2019)
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A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma
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
Published in Cancer research (Chicago, Ill.) (15.09.2016)
Published in Cancer research (Chicago, Ill.) (15.09.2016)
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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-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)
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
Published in Journal of medicinal chemistry (08.11.2018)
Published in Journal of medicinal chemistry (08.11.2018)
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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-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro‑1H‑inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)
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
Published in Journal of medicinal chemistry (08.11.2018)
Published in Journal of medicinal chemistry (08.11.2018)
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Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors
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
Published in Bioorganic & medicinal chemistry letters (15.03.2009)
Published in Bioorganic & medicinal chemistry letters (15.03.2009)
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Discovery of Danoprevir (ITMN-191/R7227), a Highly Selective and Potent Inhibitor of Hepatitis C Virus (HCV) NS3/4A Protease
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.
Published in Journal of medicinal chemistry (13.03.2014)
Published in Journal of medicinal chemistry (13.03.2014)
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Lead change of a HIF-2α antagonist guided by multiparameter optimization and utilization of an Olp→πAr interaction
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.
Published in Medicinal chemistry research (01.07.2023)
Published in Medicinal chemistry research (01.07.2023)
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General Method for the Synthesis of Phospholipid Derivatives of 1,2-O-Diacyl-sn-Glycerols
Martin, Stephen F, Josey, John A, Wong, Yue-Ling, Dean, Daniel W
Published in Journal of organic chemistry (01.08.1994)
Published in Journal of organic chemistry (01.08.1994)
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3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymerase
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
Published in Bioorganic & medicinal chemistry letters (15.01.2009)
Published in Bioorganic & medicinal chemistry letters (15.01.2009)
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Discovery of Disubstituted Imidazo[4,5‑b]pyridines and Purines as Potent TrkA Inhibitors
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
Published in ACS medicinal chemistry letters (13.09.2012)
Published in ACS medicinal chemistry letters (13.09.2012)
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Journal Article
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 inhibitors
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
Published in Bioorganic & medicinal chemistry letters (01.07.2009)
Published in Bioorganic & medicinal chemistry letters (01.07.2009)
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Journal Article
Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors
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
Published in Bioorganic & medicinal chemistry letters (01.11.2009)
Published in Bioorganic & medicinal chemistry letters (01.11.2009)
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