Zobrazeno 1 - 10
of 78
pro vyhledávání: '"Nancy N, Tsou"'
Autor:
Richard G. Ball, Narayan Variankaval, Robert A. Reamer, Jaume Balsells, Gregory York, Teresa Andreani, Varsolona Richard J, Jing Li, Andrew Brunskill, Nancy N. Tsou, Jimmy O. DaSilva, Manuel de Lera Ruiz, Nobuyoshi Yasuda, Ryan D. Cohen, C. Scott Shultz
Publikováno v:
Organic Process Research & Development. 19:1882-1890
MK-8970 is an acetal carbonate prodrug of raltegravir (Isentress). This work presents the Merck team’s investigations into the polymorphism of MK-8970, the thermodynamic relationship between the discovered crystalline forms, and implementation of t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a920d1d1119205fc3919acebe28359f8
https://doi.org/10.1021/acs.oprd.5b00129
https://doi.org/10.1021/acs.oprd.5b00129
Autor:
Richard G. Ball, Sheila M. Galloway, Katherine K. McGettigan, Harvey R. Wendt, Gregori J. Morriello, Jerry Di Salvo, Marat Vijay Reddy, Black Regina M, Amanda L. Hurley, Judy Morris, Scott D. Feighner, Eric Streckfuss, George A. Doss, Alka Bansal, Anthony Sanfiz, Scott D. Edmondson, Mary Struthers, Nancy N. Tsou, Jiafang He, Crystal McKnight, George M. Laws, Donna L. Hreniuk, Gino Salituro
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1865-1870
A novel class of human β(3)-adrenergic receptor agonists was designed in effort to improve selectivity and metabolic stability versus previous disclosed β(3)-AR agonists. As observed, many of the β(3)-AR agonists seem to need the acyclic ethanolam
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9f6c8507b7efbb2f70d1c735a63653c9
https://doi.org/10.1016/j.bmcl.2010.12.087
https://doi.org/10.1016/j.bmcl.2010.12.087
Autor:
Junying Wang, Richard G. Ball, Chun-Pyn Shen, Richard Z. Chen, Julie Lao, Vijay Bhasker G. Reddy, Xinchun Tong, Jeffrey J. Hale, Alison M. Strack, Jing Chen Xiao, Lauren P. Shearman, John S. Debenham, Tung M. Fong, D. Sloan Stribling, Christina B. Madsen-Duggan, Pei Huo, Lin Yan, Nancy N. Tsou, Thomas Bateman
Publikováno v:
Journal of Medicinal Chemistry. 53:4028-4037
This paper describes the discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596, 12c) as a novel cannabinoid-1 receptor (CB1R) inverse agonist
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8b223fd3b459aa0c611a30e5f8e83030
https://doi.org/10.1021/jm100023j
https://doi.org/10.1021/jm100023j
Autor:
Howard Y. Chen, William J. Martin, D. Euan MacIntyre, Zhixiong Ye, Raman K. Bakshi, Alison M. Strack, Doreen E. Cashen, Jian Liu, Yingjie Lai, Tianying Jian, Constantin Tamvakopoulos, Nancy N. Tsou, Shuwen He, James Dellureficio, Tung M. Fong, Peter H. Dobbelaar, David H. Weinberg, Airu S. Chen, Qingmei Hong, Iyassu K. Sebhat, Tanya MacNeil, Christopher L. Franklin, Ravi P. Nargund, Ralph A. Stearns, Rui Tang, Richard G. Ball, Matthew J. Wyvratt, Randy R. Miller, Liangqin Guo, Qianping Peng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2106-2110
We report the design, synthesis and properties of spiroindane based compound 1, a potent, selective, orally bioavailable, non-peptide melanocortin subtype-4 receptor agonist. Compound 1 shows excellent erectogenic activity in the rodent models.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ecb491322cadefd63c62faedffb60b8
https://doi.org/10.1016/j.bmcl.2010.02.058
https://doi.org/10.1016/j.bmcl.2010.02.058
Autor:
Sloan Stribling, Donald F. Thompson, Junying Wang, Xinchun Tong, Lauren P. Shearman, Cathy C. R.-R. Huang, Joana Achanfuo-Yeboah, Susan Nicolich, Andrea Frassetto, Tung M. Fong, Donald F. Hora, Chun-Pyn Shen, Nancy N. Tsou, Alison M. Strack, Richard G. Ball, Julie Lao, Gerard J. Hickey, Terry D. Faidley, Jeffrey J. Hale, Joan M. Fletcher, William K. Hagmann, Petr Vachal, Richard Z. Chen, Jing Chen Xiao
Publikováno v:
Journal of Medicinal Chemistry. 52:2550-2558
A novel series of 1-sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists was discovered through high throughput screening (HTS) and medicinal chemistry lead optimization. Potency and in vivo properties were systemati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ac1ab0a834361355e6b35a585e3c5f9d
https://doi.org/10.1021/jm900063x
https://doi.org/10.1021/jm900063x
Autor:
Ralph T. Mosley, Jason E. Imbriglio, Steven L. Colletti, Nancy N. Tsou, Subharekha Raghavan, Daniel A. DiRocco, James R. Tata, Richard G. Ball
Publikováno v:
Tetrahedron Letters. 49:4897-4900
The optimization of a palladium-catalyzed amidation reaction providing a new class of amino acid–tetrahydroanthranilic acid derivatives has been achieved. The scope of the reaction and preliminary conformational analysis of the resulting series of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e166b0124d75f4d93a0a614d3d6b3955
https://doi.org/10.1016/j.tetlet.2008.05.148
https://doi.org/10.1016/j.tetlet.2008.05.148
Publikováno v:
Tetrahedron Letters. 48:5429-5433
Platensimycin is a novel natural product antibiotic that inhibits bacterial growth by inhibiting fatty acid synthesis specifically inhibiting the elongation condensing enzyme FabF. Reaction with diazomethane at controlled temperatures led to selectiv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d74d02717fe958d1872a11b6e5905d56
https://doi.org/10.1016/j.tetlet.2007.06.009
https://doi.org/10.1016/j.tetlet.2007.06.009
Publikováno v:
Organic Process Research & Development. 11:229-236
A systematic investigation of the polymorph−hydrate system for Compound I was carried out with the objective of understanding the phase relationships between the different forms as it relates to crystallization conditions. The ternary phase diagram
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4956625cc31012a739efc90c683227f8
https://doi.org/10.1021/op600277t
https://doi.org/10.1021/op600277t
Autor:
Bruno Roy, Claudio Sturino, Nicolas Lachance, Robert Zamboni, Kathleen M. Metters, Christine Brideau, Lianhai Li, John Scheigetz, Danielle Denis, Deborah Slipetz, Marie-Claude Carrière, Elizabeth Cauchon, Gillian Greig, Gary P. O'Neill, Carl Berthelette, Michael J. Boyd, Marie-Claude Mathieu, Sonia Lamontagne, Nicole Sawyer, Robert N. Young, Nancy N. Tsou, Zhaoyin Wang, Stacia Kargman, Marc Labelle
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:3043-3048
A novel indole series of PGD2 receptor (DP receptor) antagonists is presented. Optimization of this series led to the identification of potent and selective DP receptor antagonists. In particular, antagonists 35 and 36 were identified with Ki values
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::569d39021562795735b87f35c9aa72c4
https://doi.org/10.1016/j.bmcl.2006.02.062
https://doi.org/10.1016/j.bmcl.2006.02.062
Publikováno v:
Tetrahedron Letters. 46:8909-8912
An asymmetric route to dihydroquinazolinones via the addition of ortho metalated substrates to tert-butanesulfinyl imines is reported. The scope of the nucleophile and electrophile components and the absolute stereochemical outcome are presented.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::575589955fee0fa420cd92398aa24b2f
https://doi.org/10.1016/j.tetlet.2005.10.067
https://doi.org/10.1016/j.tetlet.2005.10.067