Search Results - "Loe, Brad"

Discovery of 6-(2,4-Difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8 H -pyrido[2,3- d ]pyrimidin-7-one (Pamapimod) and 6-(2,4-Difluorophenoxy)-8-methyl-2-(tetrahydro-2 H -pyran-4-ylamino)pyrido[2,3- d ]pyrimidin-7(8 H )-one (R1487) as Orally Bioavailable and Highly Selective Inhibitors of p38α Mitogen-Activated Protein Kinase by Goldstein, David M., Soth, Michael, Gabriel, Tobias, Dewdney, Nolan, Kuglstatter, Andreas, Arzeno, Humberto, Chen, Jeffrey, Bingenheimer, William, Dalrymple, Stacie A., Dunn, James, Farrell, Robert, Frauchiger, Sandra, La Fargue, JoAnn, Ghate, Manjiri, Graves, Bradford, Hill, Ronald J., Li, Fujun, Litman, Renee, Loe, Brad, McIntosh, Joel, McWeeney, Daniel, Papp, Eva, Park, Jaehyeon, Reese, Harlan F., Roberts, Richard T., Rotstein, David, San Pablo, Bong, Sarma, Keshab, Stahl, Martin, Sung, Man-Ling, Suttman, Rebecca T., Sjogren, Eric B., Tan, Yunchou, Trejo, Alejandra, Welch, Mary, Weller, Paul, Wong, Brian R., Zecic, Hasim

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Discovery of 6-(2,4-Difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (Pamapimod) and 6-(2,4-Difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as Orally Bioavailable and Highly Selective Inhibitors of p38α Mitogen-Activated Protein Kinase by Goldstein, David M, Soth, Michael, Gabriel, Tobias, Dewdney, Nolan, Kuglstatter, Andreas, Arzeno, Humberto, Chen, Jeffrey, Bingenheimer, William, Dalrymple, Stacie A, Dunn, James, Farrell, Robert, Frauchiger, Sandra, La Fargue, JoAnn, Ghate, Manjiri, Graves, Bradford, Hill, Ronald J, Li, Fujun, Litman, Renee, Loe, Brad, McIntosh, Joel, McWeeney, Daniel, Papp, Eva, Park, Jaehyeon, Reese, Harlan F, Roberts, Richard T, Rotstein, David, San Pablo, Bong, Sarma, Keshab, Stahl, Martin, Sung, Man-Ling, Suttman, Rebecca T, Sjogren, Eric B, Tan, Yunchou, Trejo, Alejandra, Welch, Mary, Weller, Paul, Wong, Brian R, Zecic, Hasim

“…The development of a new series of p38α inhibitors resulted in the identification of two clinical candidates, one of which was advanced into a phase 2 clinical…”
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Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): Optimization for JNK potency and physicochemical properties by Gong, Leyi, Han, Xiaochun, Silva, Tania, Tan, Yun-Chou, Goyal, Bindu, Tivitmahaisoon, Parch, Trejo, Alejandra, Palmer, Wylie, Hogg, Heather, Jahagir, Alam, Alam, Muzaffar, Wagner, Paul, Stein, Karin, Filonova, Lubov, Loe, Brad, Makra, Ferenc, Rotstein, David, Rapatova, Lubica, Dunn, James, Zuo, Fengrong, Porto, Joseph Dal, Wong, Brian, Jin, Sue, Chang, Alice, Tran, Patricia, Hsieh, Gary, Niu, Linghao, Shao, Ada, Reuter, Deborah, Hermann, Johaness, Kuglstatter, Andreas, Goldstein, David

“…Structure guided optimization led to a potent series of JNK inhibitors with good physicochemical properties and desirable kinase selectivity as exemplified by…”
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3-Amino-pyrazolo[3,4-d]pyrimidines as p38α kinase inhibitors: Design and development to a highly selective lead by Soth, Michael, Abbot, Sarah, Abubakari, Allassan, Arora, Nidhi, Arzeno, Humberto, Billedeau, Roland, Dewdney, Nolan, Durkin, Kieran, Frauchiger, Sandra, Ghate, Manjiri, Goldstein, David M., Hill, Ronald J., Kuglstatter, Andreas, Li, Fujun, Loe, Brad, McCaleb, Kristen, McIntosh, Joel, Papp, Eva, Park, Jaehyeon, Stahl, Martin, Sung, Man-Ling, Suttman, Rebecca, Swinney, David C., Weller, Paul, Wong, Brian, Zecic, Hasim, Gabriel, Tobias

“…Learnings from previous Roche p38-selective inhibitors were applied to a new fragment hit, which was optimized to a potent, exquisitely selective preclinical…”
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Topical nonsteroidal antipsoriatic agents. 2. 2,3-(Alkylidenedioxy)naphthalene analogs of lonapalene by Venuti, Michael C, Loe, Brad E, Jones, Gordon H, Young, John M

“…A series of 2,3-(alkylidenedioxy)naphthalene (5a-p) analogues of lonapalene (RS-43179, 1), a 5-lipoxygenase inhibitor currently under clinical investigation…”
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Novel Series of Dihydropyridinone P2X7 Receptor Antagonists by Lopez-Tapia, Francisco, Walker, Keith A. M, Brotherton-Pleiss, Christine, Caroon, Joanie, Nitzan, Dov, Lowrie, Lee, Gleason, Shelley, Zhao, Shu-Hai, Berger, Jacob, Cockayne, Debra, Phippard, Deborah, Suttmann, Rebecca, Fitch, William L, Bourdet, David, Rege, Pankaj, Huang, Xiaojun, Broadbent, Scott, Dvorak, Charles, Zhu, Jiang, Wagner, Paul, Padilla, Fernando, Loe, Brad, Jahangir, Alam, Alker, André

“…Identification of singleton P2X7 inhibitor 1 from HTS gave a pharmacophore that eventually turned into potential clinical candidates 17 and 19. During…”
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Topical nonsteroidal antipsoriatic agents. 1. 1,2,3,4-Tetraoxygenated naphthalene derivatives by Jones, Gordon H, Venuti, Michael C, Young, John M, Murthy, D. V. Krishna, Loe, Brad E, Simpson, Richard A, Berks, Andrew H, Spires, Doreen A, Maloney, Patrick J

“…On the basis of previous observations that both 2,3-dihydro-2,2,3,3-tetrahydroxy-1,4-naphthoquinone (oxoline, 1) and 6-chloroisonaphthazarin (2) had…”
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Additions and Corrections - Topical Nonsteroidal Antipsoriatic Agents. 1. 1,2,3,4-Tetraoxygenated Naphthalene Derivatives by Jones, Gordon, Venuti, Michael, Young, John, Krishna Murthy, D, Loe, Brad, Simpson, Richard, Berks, Andrew, Spires, Doreen, Maloney, Patrick, Kruseman, Myriam, Rouhafza, Sussan, Kappas, Karen, Beard, Colin, Unger, Stefan, Cheung, Paul

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