Discovery of N‑Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo‑1H‑pyrrolo[2,3‑c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain
Sheppard, George S, Wang, Le, Fidanze, Steven D, Hasvold, Lisa A, Liu, Dachun, Pratt, John K, Park, Chang H, Longenecker, Kenton, Qiu, Wei, Torrent, Maricel, Kovar, Peter J, Bui, Mai, Faivre, Emily, Huang, Xiaoli, Lin, Xiaoyu, Wilcox, Denise, Zhang, Lu, Shen, Yu, Albert, Daniel H, Magoc, Terrance J, Rajaraman, Ganesh, Kati, Warren M, McDaniel, Keith F
Published in Journal of medicinal chemistry (28.05.2020)
Published in Journal of medicinal chemistry (28.05.2020)
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Journal Article
Discovery of N -Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1 H -pyrrolo[2,3- c ]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain
Sheppard, George S, Wang, Le, Fidanze, Steven D, Hasvold, Lisa A, Liu, Dachun, Pratt, John K, Park, Chang H, Longenecker, Kenton, Qiu, Wei, Torrent, Maricel, Kovar, Peter J, Bui, Mai, Faivre, Emily, Huang, Xiaoli, Lin, Xiaoyu, Wilcox, Denise, Zhang, Lu, Shen, Yu, Albert, Daniel H, Magoc, Terrance J, Rajaraman, Ganesh, Kati, Warren M, McDaniel, Keith F
Published in Journal of medicinal chemistry (28.05.2020)
Published in Journal of medicinal chemistry (28.05.2020)
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Journal Article
Discovery of N‑(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro‑1H‑pyrrolo[2,3‑c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor
McDaniel, Keith F, Wang, Le, Soltwedel, Todd, Fidanze, Steven D, Hasvold, Lisa A, Liu, Dachun, Mantei, Robert A, Pratt, John K, Sheppard, George S, Bui, Mai H, Faivre, Emily J, Huang, Xiaoli, Li, Leiming, Lin, Xiaoyu, Wang, Rongqi, Warder, Scott E, Wilcox, Denise, Albert, Daniel H, Magoc, Terrance J, Rajaraman, Ganesh, Park, Chang H, Hutchins, Charles W, Shen, Jianwei J, Edalji, Rohinton P, Sun, Chaohong C, Martin, Ruth, Gao, Wenqing, Wong, Shekman, Fang, Guowei, Elmore, Steven W, Shen, Yu, Kati, Warren M
Published in Journal of medicinal chemistry (26.10.2017)
Published in Journal of medicinal chemistry (26.10.2017)
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Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors
Wang, Le, Pratt, John K, Soltwedel, Todd, Sheppard, George S, Fidanze, Steven D, Liu, Dachun, Hasvold, Lisa A, Mantei, Robert A, Holms, James H, McClellan, William J, Wendt, Michael D, Wada, Carol, Frey, Robin, Hansen, T. Matthew, Hubbard, Robert, Park, Chang H, Li, Leiming, Magoc, Terrance J, Albert, Daniel H, Lin, Xiaoyu, Warder, Scott E, Kovar, Peter, Huang, Xiaoli, Wilcox, Denise, Wang, Rongqi, Rajaraman, Ganesh, Petros, Andrew M, Hutchins, Charles W, Panchal, Sanjay C, Sun, Chaohong, Elmore, Steven W, Shen, Yu, Kati, Warren M, McDaniel, Keith F
Published in Journal of medicinal chemistry (11.05.2017)
Published in Journal of medicinal chemistry (11.05.2017)
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Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors
Fidanze, Steven D., Liu, Dachun, Mantei, Robert A., Hasvold, Lisa A., Pratt, John K., Sheppard, George S., Wang, Le, Holms, James H., Dai, Yujia, Aguirre, Ana, Bogdan, Andrew, Dietrich, Justin D., Marjanovic, Jasmina, Park, Chang H., Hutchins, Charles W., Lin, Xiaoyu, Bui, Mai H., Huang, Xiaoli, Wilcox, Denise, Li, Leiming, Wang, Rongqi, Kovar, Peter, Magoc, Terrance J., Rajaraman, Ganesh, Albert, Daniel H., Shen, Yu, Kati, Warren M., McDaniel, Keith F.
Published in Bioorganic & medicinal chemistry letters (01.06.2018)
Published in Bioorganic & medicinal chemistry letters (01.06.2018)
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Methylpyrrole inhibitors of BET bromodomains
Hasvold, Lisa A., Sheppard, George S., Wang, Le, Fidanze, Steven D., Liu, Dachun, Pratt, John K., Mantei, Robert A., Wada, Carol K., Hubbard, Robbert, Shen, Yu, Lin, Xiaoyu, Huang, Xiaoli, Warder, Scott E., Wilcox, Denise, Li, Leiming, Buchanan, F. Greg, Smithee, Lauren, Albert, Daniel H., Magoc, Terrance J., Park, Chang H., Petros, Andrew M., Panchal, Sanjay C., Sun, Chaohong, Kovar, Peter, Soni, Nirupama B., Elmore, Steven W., Kati, Warren M., McDaniel, Keith F.
Published in Bioorganic & medicinal chemistry letters (15.05.2017)
Published in Bioorganic & medicinal chemistry letters (15.05.2017)
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TETRACYCLIC BROMODOMAIN INHIBITORS
JOHN PRATT, ROBERT A MANTEI, HASVOLD LISA A, GEORGE S SHEPPARD, JOHN H HOLMS, DAI YUJIA, JASMINA MARJANOVIC, LE WANG, LIU DACHUN, JUSTIN D DIETRICH, STEVEN D FIDANZE, MCDANIEL KEITH F, ANDREW BOGDAN
Year of Publication 31.01.2019
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Year of Publication 31.01.2019
Patent
BROMODOMAIN INHIBITORS
WILLIAM J MCCLELLAN, ROBERT A MANTEI, JOHN H HOLMS, GEORGE S SHEPPARD, DAI YUJIA, CAROL K WADA, WARREN M KATI, LE WANG, LISA HASVOLD, LIU DACHUN, STEVEN D FIDANZE, MCDANIEL KEITH F, JOHN K PRATT
Year of Publication 08.11.2018
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Year of Publication 08.11.2018
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BROMODOMAIN INHIBITORS
WILLIAM J MCCLELLAN, ROBERT A MANTEI, JOHN H HOLMS, GEORGE S SHEPPARD, DAI YUJIA, CAROL K WADA, WARREN M KATI, LE WANG, LISA HASVOLD, LIU DACHUN, STEVEN D FIDANZE, MCDANIEL KEITH F, JOHN K PRATT
Year of Publication 27.07.2017
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Year of Publication 27.07.2017
Patent
Abstract 931: Discovery of ABBV-744, a first-in-class highly BDII-selective BET bromodomain inhibitor
Sheppard, George S., Wang, Le, Fidanze, Steven D., Hasvold, Lisa A., Liu, Dachun, Pratt, John K., Park, Chang H., Bui, Mai-Ha, Faivre, Emily J., Huang, Xiaoli, Lin, Xiaoyu, Wilcox, Denise M., Shen, Yu, Albert, Daniel H., Magoc, Terrance J., Rajaraman, Ganesh, Kati, Warren M., McDaniel, Keith F.
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Methylpyrrole inhibitors of BET bromodomains
Hasvold, Lisa A., Sheppard, George S., Wang, Le, Fidanze, Steven D., Liu, Dachun, Pratt, John K., Mantei, Robert A., Wada, Carol K., Hubbard, Robbert, Shen, Yu, Lin, Xiaoyu, Huang, Xiaoli, Warder, Scott E., Wilcox, Denise, Li, Leiming, Buchanan, F. Greg, Smithee, Lauren, Albert, Daniel H., Magoc, Terrance J., Park, Chang H., Petros, Andrew M., Panchal, Sanjay C., Sun, Chaohong, Kovar, Peter, Soni, Nirupama B., Elmore, Steven W., Kati, Warren M., McDaniel, Keith F.
Published in Bioorganic & medicinal chemistry letters (01.05.2017)
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Published in Bioorganic & medicinal chemistry letters (01.05.2017)
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TRIAZADIBENZO[CD,F]AZULENE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF USEFUL AS BROMODOMAIN INHIBITORS
MCDANIEL, KEITH F, MARJANOVIC, JASMINA, HASVOLD, LISA A, LIU, DACHUN, MANTEI, ROBERT A, DIETRICH, JUSTIN D, SHEPPARD, GEORGE S, HOLMS, JAMES H, WANG, LE, FIDANZE, STEVEN D, PRATT, JOHN, DAI, YUJIA, BOGDAN, ANDREW
Year of Publication 15.08.2023
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Year of Publication 15.08.2023
Patent
BROMODOMAIN INHIBITORS
Fidanze, Steven D, Kati, Warren M, Sheppard, George S, Wada, Carol K, Wang, Le, McDaniel, Keith F, Holms, James H, Mantei, Robert A, Pratt, John K, McClellan, William J, Liu, Dachun, Dai, Yujia, Hasvold, Lisa
Year of Publication 25.05.2023
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Year of Publication 25.05.2023
Patent
BROMODOMAIN INHIBITORS
Michael SCHRIMPF, George S. SHEPPARD, Steven D. FIDANZE, Le WANG, Keith F. MCDANIEL, John PRATT, Dachun LIU, Bing LI, Lisa A. HASVOLD
Year of Publication 12.05.2022
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Year of Publication 12.05.2022
Patent
INHIBITEURS DE BROMODOMAINE
LI, Bing, LIU, Dachun, HASVOLD, Lisa A, WANG, Le, SCHRIMPF, Michael, SHEPPARD, George S, PRATT, John, FIDANZE, Steven D, MCDANIEL, Keith F
Year of Publication 27.04.2022
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Year of Publication 27.04.2022
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Bromodomain Inhibitors
Fidanze, Steven D, Wang, Le, Pratt, John, Sheppard, George, McDaniel, Keith F, Liu, Dachun, Schrimpf, Michael, Hasvold, Lisa A, Li, Bing
Year of Publication 20.01.2022
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Year of Publication 20.01.2022
Patent
Bdii-selective bromodomain inhibitor
PRATT John, SCHRIMPF Michael, LI Bing, MCDANIEL Keith F, WANG Le, FIDANZE Steven D, LIU Dachun, HASVOLD Lisa A, SHEPPARD George S
Year of Publication 31.05.2021
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Year of Publication 31.05.2021
Patent
BROMODOMAIN INHIBITORS
JOHN PRATT, LE WANG, LISA A HASVOLD, STEVEN D FIDANZE, BING LI, DACHUN LIU, GEORGE S SHEPPARD, KEITH F MCDANIEL, MICHAEL SCHRIMPF
Year of Publication 28.04.2021
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Year of Publication 28.04.2021
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BROMODOMAIN INHIBITORS
LIU, Dachun, LI, Bing, HASVOLD, Lisa A, WANG, Le, SCHRIMPF, Michael, SHEPPARD, George S, PRATT, John, FIDANZE, Steven D, MCDANIEL, Keith F
Year of Publication 20.04.2021
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Year of Publication 20.04.2021
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Bromodomain inhibitors
LIU, Dachun, LI, Bing, HASVOLD, Lisa A, WANG, Le, SCHRIMPF, Michael, SHEPPARD, George S, PRATT, John, FIDANZE, Steven D, MCDANIEL, Keith F
Year of Publication 18.03.2021
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Year of Publication 18.03.2021
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