Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Emma J. Carlson"'
Autor:
Wai-Si Eng, Xinchun Tong, Richard Tschirret-Guth, Song Zheng, Gary G. Chicchi, Geoge A. Doss, Koppara Samuel, Richard Hargreaves, Terence G. Hamill, Marc M. Kurtz, Robert J. DeVita, Sanjeev Kumar, Alan Wheeldon, Emma J. Carlson, Alana Upthagrove, Jaime Lynn Bunda, Stephen Krause, Jinlong Jiang, Christine Ryan, Sander G. Mills, Donald Burns, Kwei-Lan C. Tsao
Publikováno v:
Journal of Medicinal Chemistry. 52:3039-3046
3-[(3aR,4R,5S,7aS)-5-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}-4-(4-fluorophenyl)octahydro-2H-isoindol-2-yl]cyclopent-2-en-1-one (17) is a high affinity, brain-penetrant, hydroisoindoline-based neurokinin-1 (NK(1)) receptor antagonist with a lo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d21762545018b32ec2dc16a2b6444d66
https://doi.org/10.1021/jm8016514
https://doi.org/10.1021/jm8016514
Autor:
Janusz Jozef Kulagowski, Gary G. Chicchi, Clare London, Alan Wheeldon, Ian Thomas Huscroft, Emma J. Carlson, Marc M. Kurtz, Piotr Raubo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:2008-2012
1-Phenyl-8-azabicyclo[3.2.1]octane ethers are NK1 receptor antagonists. Substitution at the 6-exo-position led to high affinity NK1 antagonists with a prolonged duration of action in vivo. Incorporation of an α-methyl substituent in the pendent benz
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e93157e3f9b3b77746bfe5a3bca6ab93
https://doi.org/10.1016/j.bmcl.2005.12.069
https://doi.org/10.1016/j.bmcl.2005.12.069
Autor:
Angela Williams, Raymond G. Hill, Guanghan Liu, Margaret A. Cascieri, John J. Sramek, John P. Feighner, Gary G. Chicchi, Ram K. Shrivastava, Malcolm MacCoss, Edward M. Scolnick, Duane B. Snavely, Emma J. Carlson, Louise Hewson, Christopher John Swain, Jeffrey J. Hale, Sharon Sadowski, N.R. Cutler, David D. Smith, Nadia M.J. Rupniak, Franz Hefti, Timothy Harrison, Edwina Wyatt-Knowles, Sander G. Mills, Scott A. Reines, Richard Hargreaves, John Carman, Mark S. Kramer
Publikováno v:
Science. 281:1640-1645
The localization of substance P in brain regions that coordinate stress responses and receive convergent monoaminergic innervation suggested that substance P antagonists might have psychotherapeutic properties. Like clinically used antidepressant and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::888508e4bee9b37a82f2f5da6928e9e3
https://doi.org/10.1126/science.281.5383.1640
https://doi.org/10.1126/science.281.5383.1640
Autor:
Susan Boyce, Kwei-Lan Tsao, Gary G. Chicchi, Karen Townson, Sander G. Mills, Julie A. DeMartino, Neil Collinson, Marc M. Kurtz, Gregori J. Morriello, Robert J. DeVita, Alan Wheeldon, Nadia M.J. Rupniak, Emma J. Carlson, Tricia Johnson, Xinchun Tong, Song Zheng
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(19)
Previously, we had disclosed a novel class of hNK(1) antagonists based on the 5,5-fused pyrrolidine core. These compounds displayed subnanomolar hNK(1) affinity along with good efficacy in a gerbil foot-tapping (GFT) model, but unfortunately they had
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a8e996df1a1b78f6c5cafc9b1d3ed98
https://pubmed.ncbi.nlm.nih.gov/20729082
https://pubmed.ncbi.nlm.nih.gov/20729082
Autor:
Gary G. Chicchi, Kwei-Lan C. Tsao, Huagang Lu, Xinchun Tong, Gregori J. Morriello, Robert J. DeVita, Alan Wheeldon, Emma J. Carlson, Sander G. Mills, Song Zheng, Jianming Bao, Marc M. Kurtz
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(7)
A new class of potent NK1 receptor antagonists with a tetrahydroindolizinone core has been identified. This series of compounds demonstrated improved functional activities as compared to previously identified 5,5-fused pyrrolidine lead structures. SA
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f528cd8177c783967c22911a6cf6d1ce
https://pubmed.ncbi.nlm.nih.gov/20188553
https://pubmed.ncbi.nlm.nih.gov/20188553
Autor:
Karen Townson, Gregori J. Morriello, Kwei-Lan Tsao, Gary G. Chicchi, Nadia M.J. Rupniak, Sander G. Mills, Mikhail Reibarkh, Philip Davies, Julie A. DeMartino, Neil Collinson, Alan Wheeldon, Marc M. Kurtz, Stephen Moore, Tricia Johnson, F.D. Tattersall, Susan Boyce, Robert J. DeVita, Emma J. Carlson, Song Zheng, Xinchun Tong
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(6)
Previous work on human NK(1) (hNK(1)) antagonists in which the core of the structure is a 5,5-fused pyrrolizinone has been disclosed. The structural-activity-relationship studies on simple alpha- and beta-substituted compounds of this series provided
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c5f1466795a40ae5e39fb30c2992976
https://pubmed.ncbi.nlm.nih.gov/20153964
https://pubmed.ncbi.nlm.nih.gov/20153964
Autor:
Cherilyn Turner, Alan Wheeldon, Sander G. Mills, Gary G. Chicchi, Robert J. DeVita, Jonathan R. Young, Kwei-Lan C. Tsao, Emma J. Carlson, Marc M. Kurtz, Ronsar Eid
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(19)
The preparation and structure-activity-relationships of novel pyrrolidine-carboxamides and oxadiazoles are described. Compounds in this series were found to be potent hNK(1) antagonists in vitro and efficacious in vivo with minimal interactions with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff751abca0250c4b312599844e5efbe8
https://pubmed.ncbi.nlm.nih.gov/17723300
https://pubmed.ncbi.nlm.nih.gov/17723300
Autor:
Robert J. DeVita, Kwei-Lan C. Tsao, Gary G. Chicchi, Jonathan R. Young, Emma J. Carlson, Sander G. Mills, Lehua Chang, Song Zheng, Ronsar Eid, Marc M. Kurtz, H. Donald Burns, Alan Wheeldon, Xinchun Tong, Nancy N. Tsou, Richard Hargreaves, Richard G. Ball, Peter Lin, Wai-Si Eng
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(18)
SAR studies on amides, ureas, and vinylogous amides derived from pyrrolidine led to the discovery of several potent hNK(1) antagonists. One particular vinylogous amide (45b) had excellent potency, selectivity, pharmacokinetic profile, and functional
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d9e4f91caeb41ac6da432e0550d31e62
https://pubmed.ncbi.nlm.nih.gov/17637506
https://pubmed.ncbi.nlm.nih.gov/17637506
Autor:
Gary G. Chicchi, Marc M. Kurtz, Emma J. Carlson, Alan Wheeldon, Kwei-Lan C. Tsao, Christopher Thomson, Janusz Jozef Kulagowski, Christopher John Swain
Publikováno v:
ChemInform. 37
A series of 8-azabicyclo[3.2.1]octane amine hNK1 antagonists has been investigated and structure–activity relationships of the benzylamine and 6-exo substituents described. Acidic substituents at C6 give a series of high affinity compounds for hNK1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::716dcaa8d8ec5578f58e5c5ca792c086
https://doi.org/10.1002/chin.200617156
https://doi.org/10.1002/chin.200617156
Autor:
Jason Matthew Elliott, Gary G. Chicchi, Ute Gerhard, María Domínguez, Richard Alexander Jelley, Marc M. Kurtz, Alan Wheeldon, Emma J. Carlson, Kwei lan Tsao, Olivier Dirat, A. Brian Jones
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(11)
A new class of high affinity hNK 1 R antagonists based on seven-membered ring cores has been identified. This series, with relatively simple, compact structures, includes compounds with high affinity, good selectivity, and promising in vivo propertie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a6b72efa2a07077ff37a7612e21d1c3a
https://pubmed.ncbi.nlm.nih.gov/16574413
https://pubmed.ncbi.nlm.nih.gov/16574413