Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Richard James Bull"'
Autor:
Ken Grime, Keith Bowers, Escott Katherine Jane, Antonio Mete, Vince Russell, Andrew Mather, David Donald, Richard James Bull, Rhonan Ford, Helen Coope, Nicholas C. Ray
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6248-6253
A novel series of muscarinic receptor antagonists was developed, with the aim of identifying a compound with high M3 receptor potency and a reduced risk of dose-limiting side effects with potential for the treatment of COPD. Initial compound modifica
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::83d4a9990cb12edeaca3dd9007ee173d
https://doi.org/10.1016/j.bmcl.2013.09.092
https://doi.org/10.1016/j.bmcl.2013.09.092
Autor:
Richard A. Goldsmith, Cristina Lewis, Binqing Wei, Jeffery J. Wallin, Erin K. Bradley, Nicole Blaquiere, Leslie Lee, Steven T. Staben, Jim Nonomiya, Steven Do, Deepak Sampath, Laurent Salphati, Timothy P. Heffron, Jodie Pang, Chudi Ndubaku, Kyle A. Edgar, Danette Dudley, Robert Heald, Richard James Bull, Matthew Baumgardner, Steve Price, Wei Wei Prior, Steve Sideris, Jennafer Dotson, Lan Wang, Michelle Nannini, Aleksandr Kolesnikov, Lori Friedman, Olivero Alan G
Publikováno v:
Journal of Medicinal Chemistry. 56:4597-4610
Dysfunctional signaling through the phosphoinositide 3-kinase (PI3K)/AKT/mTOR pathway leads to uncontrolled tumor proliferation. In the course of the discovery of novel benzoxepin PI3K inhibitors, we observed a strong dependency of in vivo antitumor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b01e2e5b34b3b320b0e198385feb2c87
https://doi.org/10.1021/jm4003632
https://doi.org/10.1021/jm4003632
Autor:
Kathy Barrett, Paul Gibbons, Steven Shia, Jane R. Kenny, Mark Zak, Charles Ellwood, Sharada Labadie, Richard James Bull, Chris Hamman, Peter H. Crackett, Peter Gribling, Peter S. Dragovich, Scott Savage, Jiangpeng Liao, Jason DeVoss, Christine Chang, Paroma Chakravarty, Mercedesz Balazs, Wyne P. Lee, Tony Johnson, Rebecca Pulk, Michael F. T. Koehler, Gauri Deshmukh, Marya Liimatta, Janusz J. Kulagowski, Pawan Bir Kohli, Anne van Abbema, Austin John Reeve, Rohan Mendonca, Adam R. Johnson, Ignacio Aliagas, Simon Gaines, Charles Eigenbrot, Yisong Xiao, Nico Ghilardi, Jing Yang, Christopher A. Hurley, Philippe Bergeron, Wade S. Blair, Peter Hewitt, Stuart Ward, Eric Harstad, Micah Steffek, Barbara Avitabile-Woo, Stefan Gradl, Raman Narukulla, Savita Ubhayakar
Publikováno v:
Journal of medicinal chemistry. 56(11)
Herein we report on the structure-based discovery of a C-2 hydroxyethyl moiety which provided consistently high levels of selectivity for JAK1 over JAK2 to the imidazopyrrolopyridine series of JAK1 inhibitors. X-ray structures of a C-2 hydroxyethyl a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::53d0d607376d7e1e01099fe1e9376df8
https://pubmed.ncbi.nlm.nih.gov/23659214
https://pubmed.ncbi.nlm.nih.gov/23659214
Autor:
Adam R. Johnson, Raman Narukulla, Janusz J. Kulagowski, Robert James Maxey, Rina Fong, Stuart Ward, Wade S. Blair, Hazel Joan Dyke, Jane R. Kenny, Marya Liimatta, Nico Ghilardi, Mark Zak, Patrick J. Lupardus, Christopher A. Hurley, Paul Gibbons, Rebecca Pulk, Richard James Bull, Pawan Bir Kohli, Peter H. Crackett, Christine Chang, Savita Ubhayakar, Anne van Abbema, Peter Hewitt, Bohdan Waszkowycz, Gauri Deshmukh, Tony Johnson, Rohan Mendonca
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(12)
The identification of a novel fused triazolo-pyrrolopyridine scaffold, optimized derivatives of which display nanomolar inhibition of Janus kinase 1, is described. Prototypical example 3 demonstrated lower cell potency shift, better permeability in c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e5dd453bc11f612af005089b1b8eb7f
https://pubmed.ncbi.nlm.nih.gov/23642482
https://pubmed.ncbi.nlm.nih.gov/23642482
Autor:
Nicole Blaquiere, Cristina Lewis, Ping Wu, Steven T. Staben, Jeremy Murray, Aleks Kolesnikov, Robert Heald, Richard James Bull, Leslie Lee, Jones Mark, Lan Wang, Timothy P. Heffron, Jeff Wallin, Christian Weismann, Jodie Pang, Binqing Wei, Graham Elgin Jones, Wei Wei Prior, Alan G. Olivero, Daniel C. Gray, Rachel Ord, Kyle A. Edgar, Jim Nonomiya, Danette Dudley, Deepak Sampath, Neville James Mclean, Marcia Belvin, Laurent Salphati, Chudi Ndubaku, Stephen Price, Lionel Rouge, John Lesnick
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(9)
A series of suitable five-membered heterocyclic alternatives to thiophenes within a thienobenzoxepin class of PI3-kinase (PI3K) inhibitors was discovered. Specific thiazolobenzoxepin 8-substitution was identified that increased selectivity over PI3K
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5724e89337ad63dc70f387ab6026b1e7
https://pubmed.ncbi.nlm.nih.gov/23540645
https://pubmed.ncbi.nlm.nih.gov/23540645