Zobrazeno 1 - 10
of 78
pro vyhledávání: '"Jeremy J Edmunds"'
Autor:
Dawn M George, Raymond J Huntley, Kevin Cusack, David B Duignan, Michael Hoemann, Jacqueline Loud, Regina Mario, Terry Melim, Kelly Mullen, Gagandeep Somal, Lu Wang, Jeremy J Edmunds
Publikováno v:
PLoS ONE, Vol 13, Iss 9, p e0203567 (2018)
The ability to restrict low molecular weight compounds to the gastrointestinal (GI) tract may enable an enhanced therapeutic index for molecular targets known to be associated with systemic toxicity. Using a triazolopyrazine CSF1R inhibitor scaffold,
Externí odkaz:
https://doaj.org/article/f9e4d7a1ef864cb18c1b355c36fdb091
Autor:
Jeremy J. Edmunds
Publikováno v:
Medicinal Chemistry Reviews ISBN: 9780996293280
Medicinal Chemistry Reviews
Medicinal Chemistry Reviews
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c46d11bb1a66a84f817e704f33a639fd
https://doi.org/10.29200/acsmedchemrev-v54.ch6
https://doi.org/10.29200/acsmedchemrev-v54.ch6
Autor:
Kevin P. Cusack, David B. Duignan, Jacqueline Loud, Michael Z. Hoemann, Lu Wang, Kelly D. Mullen, Regina Mario, Jeremy J. Edmunds, Dawn M. George, Gagandeep Somal, Raymond Huntley, Terry Melim
Publikováno v:
PLoS ONE, Vol 13, Iss 9, p e0203567 (2018)
PLoS ONE
PLoS ONE
The ability to restrict low molecular weight compounds to the gastrointestinal (GI) tract may enable an enhanced therapeutic index for molecular targets known to be associated with systemic toxicity. Using a triazolopyrazine CSF1R inhibitor scaffold,
Autor:
Anwar Murtaza, Edit Tarcsa, Ana L. Aguirre, Neil Wishart, Gagandeep Somal, Lu Wang, Kent D. Stewart, Stacy Van Epps, Kristine E. Frank, Heather Davis, Michael Friedman, Bin Li, Jeffrey W. Voss, Maria A. Argiriadi, Jonathan George, Morytko Michael J, Jeremy J. Edmunds, Dawn M. George, Deborah Hyland, Kevin R. Woller, Eric R. Goedken, Bryan A. Fiamengo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:4399-4404
Previous work investigating tricyclic pyrrolopyrazines as kinase cores led to the discovery that 1-cyclohexyl-6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazine (12) had Jak inhibitory activity. Herein we describe our initial efforts to develop orally b
Autor:
Cornel Catana, Lisa A. Perrin, Jeff Ohren, Jeremy J. Edmunds, John Quin, Derek James Sheehan, Sangita M. Baxi, Jennifer K. Hoffman, Jeffrey T. Kohrt, Amy M. Delaney, Fred L. Ciske, Michael Kaufman, Noel A. Powell, Patrick I. McConnell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1046-1050
We report the SAR around a series of 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. 2-Aminophenethyl analogs demonstrate excellent potency but moderate kinase selectivity, while 2-aminobenzyl analogs that fill the Ala571 subpocket exhi
Autor:
Chad L. Stoner, Teresa Ellis, Robert Ostroski, Ronald J. Heemstra, Jeffrey F. Ohren, Nadia Esmaeil, Christopher F. Bigge, Geyer Andrew George, Jo Ann Davis, Mehran Jalaie, Declan Flynn, Filzen Gary Frederick, Agustin Casimiro-Garcia, Danette Dudley, Jeremy J. Edmunds, Robert P. Schaum, Jing Chen
Publikováno v:
Journal of Medicinal Chemistry. 54:4219-4233
Mining of an in-house collection of angiotensin II type 1 receptor antagonists to identify compounds with activity at the peroxisome proliferator-activated receptor-γ (PPARγ) revealed a new series of imidazo[4,5-b]pyridines 2 possessing activity at
Autor:
Noel A. Powell, Joseph E. Duran, Timothy J. Hagen, Robert M. Kennedy, Fred L. Ciske, Daniel D. Holsworth, Cuiman Cai, Jeremy J. Edmunds, Daniele M. Leonard
Publikováno v:
Tetrahedron Letters. 51:4441-4444
We have optimized the Pd-catalyzed intramolecular α-arylation of 2-(2-halo-benzyl)-cyclohexanones and found that the use of 2-(dicyclohexylphosphino)-2′,4′,6′-tri-i-propyl-1,1′-biphenyl (X-Phos) as an added ligand led to a reproducible, effi
Publikováno v:
Journal of Medicinal Chemistry. 53:4830-4841
IntroductionCheminformatics can be broadly described as any attempttousechemicalinformationtoinfertherelationshipsbetweenor attributes of chemical structures. From a drug discoveryperspective, cheminformatic principles can be applied fromthe earliest
Autor:
Robert P. Schaum, Lakshmi Narasimhan, Agustin Casimiro-Garcia, Chad A. Van Huis, Danette Dudley, Kevin J. Filipski, Wayne L. Cody, Christopher F. Bigge, Michael Pamment, Jeremy J. Edmunds, Thomas B. McClanahan, Ronald J. Heemstra, Vaishali Sahasrabudhe, Robert J. Leadley, Igor Mochalkin, J. Thomas Peterson, Jeffrey T. Kohrt
Publikováno v:
Bioorganic & Medicinal Chemistry. 17:2501-2511
Aiming to improve upon previously disclosed Factor Xa inhibitors, a series of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides were explored with the intent of increasing the projected human half-life versus 5 (projected human t1/2 = 6 h). A stereosp
Publikováno v:
Chemical Research in Toxicology. 21:1095-1106
Compound I (4,5-dihydropyrazole-1,5-dicarboxylic acid-1-[(4-chlorophenyl)-amide] 5-[(2-oxo-2 H-[1,3']bipyridinyl-6'-yl)-amide] was found to undergo metabolic activation in rat liver microsomes in the presence of NADPH. A reactive intermediate, postul