Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Brad Loe"'
Autor:
Mcintosh Joel, Andreas Kuglstatter, Paul Weller, Sarah C. Abbot, David C. Swinney, Brad Loe, Tobias Gabriel, Roland J. Billedeau, Martin Stahl, Hasim Zecic, Nidhi Arora, Eva Papp, Humberto Bartolome Arzeno, Brian Wong, Allassan Abubakari, Nolan James Dewdney, David Michael Goldstein, Man-Ling Sung, Rebecca T Suttman, Michael Soth, Jaehyeon Park, Kieran Durkin, Fujun Li, Manjiri Ghate, Kristen Lynn Mccaleb, Sandra Frauchiger, Ronald J. Hill
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3452-3456
Learnings from previous Roche p38-selective inhibitors were applied to a new fragment hit, which was optimized to a potent, exquisitely selective preclinical lead with a good pharmacokinetic profile.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa8eb5a3a44a865221a520c55232f9f7
https://doi.org/10.1016/j.bmcl.2011.03.098
https://doi.org/10.1016/j.bmcl.2011.03.098
Autor:
Jaehyeon Park, Harlan F Reese, Yun-Chou Tan, Hasim Zecic, Martin Stahl, Keshab Sarma, Renee Litman, Alejandra Trejo, William Bingenheimer, Michael Soth, David Michael Goldstein, Mary Welch, Eric Brian Sjogren, Man-Ling Sung, Sandra Frauchiger, Nolan James Dewdney, Bong San Pablo, Eva Papp, Daniel McWeeney, Ronald J. Hill, Paul Weller, Manjiri Ghate, JoAnn La Fargue, Brian Wong, Stacie A. Dalrymple, James Patrick Dunn, David Mark Rotstein, Richard T. Roberts, Bradford Graves, Rebecca T Suttman, Mcintosh Joel, Farrell Robert P, Andreas Kuglstatter, Chen Jian Jeffrey, Fujun Li, Humberto Bartolome Arzeno, Brad Loe, Tobias Gabriel
Publikováno v:
Journal of Medicinal Chemistry. 54:2255-2265
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 study for rheumatoid arthritis. The original lead, an lck inhibitor that also potently in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5bdfa3e0a0a96eaca0eea2feab67e249
https://doi.org/10.1021/jm101423y
https://doi.org/10.1021/jm101423y
Autor:
Charles Alois Dvorak, Francisco Javier Lopez-Tapia, Xiaojun Huang, Brad Loe, Debra A. Cockayne, William L. Fitch, Scott Broadbent, Berger Jacob, Christine E. Brotherton-Pleiss, Keith A. M. Walker, Rebecca Suttmann, David L. Bourdet, Lee Edwin Lowrie, Shelley K. Gleason, Dov Nitzan, Paul J. Wagner, Jiang Zhu, Zhao Shu-Hai, Fernando Padilla, André Alker, Joanie Caroon, Deborah Phippard, Alam Jahangir, Pankaj D. Rege
Publikováno v:
Journal of medicinal chemistry. 58(21)
Identification of singleton P2X7 inhibitor 1 from HTS gave a pharmacophore that eventually turned into potential clinical candidates 17 and 19. During development, a number of issues were successfully addressed, such as metabolic stability, plasma st
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e880f027ef8eadeaef6f8cc77b4f99c
https://pubmed.ncbi.nlm.nih.gov/26460788
https://pubmed.ncbi.nlm.nih.gov/26460788
Autor:
Xiaochun Han, Yun-Chou Tan, Sue Jin, Paul J. Wagner, Alejandra Trejo, Parch Tivitmahaisoon, David Mark Rotstein, Bindu Goyal, Andreas Kuglstatter, Wylie Solang Palmer, Leyi Gong, Brian Wong, Patricia Tran, Alam Jahagir, Alice Chang, Joseph Dal Porto, Linghao Niu, Johaness Hermann, Fengrong Zuo, James Patrick Dunn, Karin Ann Stein, Heather Hogg, Muzaffar Alam, Ada Shao, David Michael Goldstein, Deborah Carol Reuter, Ferenc Makra, Gary Hsieh, Brad Loe, Lubov Filonova, Lubica Rapatova, Tania Silva
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(12)
A novel series of indole/indazole-aminopyrimidines was designed and synthesized with an aim to achieve optimal potency and selectivity for the c-Jun kinase family or JNKs. Structure guided design was used to optimize the series resulting in a signifi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e1d571f35d6a4f78286cd06b8fa7d5d
https://pubmed.ncbi.nlm.nih.gov/23664880
https://pubmed.ncbi.nlm.nih.gov/23664880
Autor:
David M, Goldstein, Michael, Soth, Tobias, Gabriel, Nolan, Dewdney, Andreas, Kuglstatter, Humberto, Arzeno, Jeffrey, Chen, William, Bingenheimer, Stacie A, Dalrymple, James, Dunn, Robert, Farrell, Sandra, Frauchiger, JoAnn, La Fargue, Manjiri, Ghate, Bradford, Graves, Ronald J, Hill, Fujun, Li, Renee, Litman, Brad, Loe, Joel, McIntosh, Daniel, McWeeney, Eva, Papp, Jaehyeon, Park, Harlan F, Reese, Richard T, Roberts, David, Rotstein, Bong, San Pablo, Keshab, Sarma, Martin, Stahl, Man-Ling, Sung, Rebecca T, Suttman, Eric B, Sjogren, Yunchou, Tan, Alejandra, Trejo, Mary, Welch, Paul, Weller, Brian R, Wong, Hasim, Zecic
Publikováno v:
Journal of medicinal chemistry. 54(7)
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 study for rheumatoid arthritis. The original lead, an lck inhibitor that also potently in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::cda31600d6054cc75ed83ea768d5f392
https://pubmed.ncbi.nlm.nih.gov/21375264
https://pubmed.ncbi.nlm.nih.gov/21375264
Autor:
Brad Loe, S. H. Unger, P. Cheung, S. Rouhafza, J. M. Young, K. C. Kappas, P. J. Maloney, M. C. Venuti, Doreen A. Spires, D. V. K. Murthy, Colin C. Beard, R. A. Simpson, M. Kruseman, G. H. Jones, A. H. Berks
Publikováno v:
ChemInform. 18
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::578e20670d16f2aef65d0d1d5cae7377
https://doi.org/10.1002/chin.198703158
https://doi.org/10.1002/chin.198703158
Publikováno v:
ChemInform. 20
Diels-Alder reaction of chloroprene (I) with the benzoquinones (II) gives the adducts (III) which are oxidized to yield the naphthoquinones (IV).
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e630324552bdcf11245bf2766e523cb1
https://doi.org/10.1002/chin.198920197
https://doi.org/10.1002/chin.198920197
Publikováno v:
Journal of medicinal chemistry. 31(11)
A series of 2,3-(alkylidenedioxy)naphthalene (5a-p) analogues of lonapalene (RS-43179, 1), a 5-lipoxygenase inhibitor currently under clinical investigation for the treatment of psoriasis, has been prepared and evaluated for topical inhibitory activi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e4c762337279a4f51ad10f7edf117107
https://pubmed.ncbi.nlm.nih.gov/3141623
https://pubmed.ncbi.nlm.nih.gov/3141623
Autor:
M. Kruseman, Brad Loe, G. H. Jones, Doreen A. Spires, P. J. Maloney, A. H. Berks, D. V. K. Murthy, R. A. Simpson, M. C. Venuti, John M. Young
Publikováno v:
Journal of medicinal chemistry. 29(8)
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 demonstrated antipsoriatic activity in vivo, a series of structural derivatives of 2 were prepared an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3fce34e11bad9a6327bdcf21368b52b
https://pubmed.ncbi.nlm.nih.gov/3016268
https://pubmed.ncbi.nlm.nih.gov/3016268
Autor:
Richard J. Simpson, Doreen A. Spires, Murthy D V Krishna, Patrick R. Maloney, John K. Young, Paul S. Cheung, Karen Kappas, S. H. Unger, A. H. Berks, Sussan Rouhafza, Brad Loe, Michael C. Venuti, Colin C. Beard, Myriam Kruseman, Jones Gordon H
Publikováno v:
Journal of Medicinal Chemistry. 29:2534-2534
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::91dc7b27944392b8de27892a955b2826
https://doi.org/10.1021/jm00162a604
https://doi.org/10.1021/jm00162a604