Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Kwei-Lan C. Tsao"'
Autor:
David Wilson, Bindhu V. Karanam, Mona Purcell, Maria Madeira, Gary G. Chicchi, Jianming Bao, Liza Gantert, Robert J. DeVita, Huagang Lu, Wai-Si Eng, Sander G. Mills, Richard G. Ball, Andrew J. Kassick, Peter Lin, Sanjeev Kumar, Jaime Lynn Bunda, George A. Doss, Kwei-Lan C. Tsao, Jacquelyn J. Cook, Xinchun Tong, Richard Tschirret-Guth, Jinlong Jiang, Koppara Samuel, Richard Hargreaves, Hong Wang, Donald F. Hora
Publikováno v:
Journal of Medicinal Chemistry. 56:5940-5948
Hydroisoindoline 2 has been previously identified as a potent, brain-penetrant NK1 receptor antagonist with a long duration of action and improved profile of CYP3A4 inhibition and induction compared to aprepitant. However, compound 2 is predicted, ba
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::94febe29ddadade1fbafbe0e7e0c71d3
https://doi.org/10.1021/jm400751p
https://doi.org/10.1021/jm400751p
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:
Peter Lin, Gary G. Chicchi, Julie A. DeMartino, Neil Collinson, Marc M. Kurtz, Susan Boyce, Robert J. DeVita, Alan Wheeldon, Jonathan R. Young, Stephen Moore, Emma J. Carlson, Kwei-Lan C. Tsao, Sander G. Mills, Karen Townson, George A. Doss, Gregori J. Morriello, Nadia M.J. Rupniak
Publikováno v:
Bioorganic & Medicinal Chemistry. 16:2156-2170
Previous work on human NK(1) antagonists in which the core of the structure is a substituted pyrrolidine has been disclosed. These compounds showed good binding affinity and functional IP activity, however, many did not exhibit the necessary brain pe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a07bdec5af551942f4ff8d7149d7c129
https://doi.org/10.1016/j.bmc.2007.11.081
https://doi.org/10.1016/j.bmc.2007.11.081
Autor:
Andrew J, Kassick, Jinlong, Jiang, Jaime, Bunda, David, Wilson, Jianming, Bao, Huagang, Lu, Peter, Lin, Richard G, Ball, George A, Doss, Xinchun, Tong, Kwei-Lan C, Tsao, Hong, Wang, Gary, Chicchi, Bindhu, Karanam, Richard, Tschirret-Guth, Koppara, Samuel, Donald F, Hora, Sanjeev, Kumar, Maria, Madeira, Waisi, Eng, Richard, Hargreaves, Mona, Purcell, Liza, Gantert, Jacquelyn, Cook, Robert J, DeVita, Sander G, Mills
Publikováno v:
Journal of medicinal chemistry. 56(14)
Hydroisoindoline 2 has been previously identified as a potent, brain-penetrant NK1 receptor antagonist with a long duration of action and improved profile of CYP3A4 inhibition and induction compared to aprepitant. However, compound 2 is predicted, ba
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::b81957365353e94734b4df68ad567f3d
https://pubmed.ncbi.nlm.nih.gov/23808489
https://pubmed.ncbi.nlm.nih.gov/23808489
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:
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