Zobrazeno 1 - 10
of 87
pro vyhledávání: '"Ronald K. Russell"'
Autor:
Yongzheng Zhang, Stephen M. Manzo, Derek A. Beauchamp, Sergio Cesco-Cancia, Xun Li, Ahmed F. Abdel-Magid, Fuh-Rong Tsay, Scott A. Ballentine, Caterina Ferraro, Kenneth M. Wells, Christopher A. Teleha, Hua Marlon Zhong, Scott Youells, Steven J. Mehrman, Ronald K. Russell, Lorraine Scott, Jan M. Spink, Craig Diamond
Publikováno v:
Organic Process Research & Development. 19:1774-1783
The process development of Mavatrep (1), a potent transient receptor potential vanilloid-1 (TRPV1) antagonist, is described. The two key synthetic transformations are the synthesis of (E)-6-bromo-2-(4-(trifluoromethyl)styryl)1H-benzo[d]imidazole (4)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8d85dfd2095f7bcb55164604dce960af
https://doi.org/10.1021/acs.oprd.5b00271
https://doi.org/10.1021/acs.oprd.5b00271
Autor:
Ronald K. Russell, Yongzheng Zhang, Marc Verbeek, Michael Reuman, Zhihua Sui, Hilde Vanbaelen, Christopher A. Teleha, Shawn Branum, James C. Lanter, Fawzy Nagy E, Fu-An Kang, Luc Van Der Steen, Michael Kolpak, Michael P. Winters, Derek A. Beauchamp, Gregory C. Leo
Publikováno v:
Organic Process Research & Development. 18:1630-1640
The preparation of a chemokine receptor type 2 (CCR-2) antagonist bearing a cyclopenta[b]furan core is described on a 600 g scale. Compared to our previously reported synthesis of the all-carbon core CCR-2 antagonist with a similar peripheral 3-metho
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e6e2ea61a6b3e2fe6f4999868e3c1c57
https://doi.org/10.1021/op500266w
https://doi.org/10.1021/op500266w
Autor:
Shawn Branum, Fawzy Nagy E, Christopher A. Teleha, Luc Van Der Steen, Mark J. Wall, Derek A. Beauchamp, Michael Reuman, Marc Verbeek, Michael Kolpak, Zhihua Sui, Chaozhong Cai, Gregory C. Leo, Ronald K. Russell, Yongzheng Zhang, Fu-An Kang, Hilde Vanbaelen
Publikováno v:
Organic Process Research & Development. 18:1622-1629
The preparation of a novel chemokine receptor type 2 (CCR-2) antagonist is described on a 135 g scale. The synthesis of an all-carbon bicyclic core was accomplished using a radical cyclization strategy using chiral precursors, wherein elaboration led
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::30ed40727f516d73f0e1e4e53e8301d9
https://doi.org/10.1021/op500265z
https://doi.org/10.1021/op500265z
Autor:
Derek A. Beauchamp, Jan M. Spink, Scott A. Ballentine, Christopher A. Teleha, Ronald K. Russell, Kenneth M. Wells, Shawn Branum, Mark R. Player, Xun Li, William V. Murray, Raymond J. Patch, Hui Huang
Publikováno v:
Organic Process Research & Development. 18:321-330
The development of a reproducible process for multihundred gram production of (Z)-5-((1-(4-chloro-2-(trifluoromethyl)benzyl)-1H-indazol-5-yl)methylene)-3-((3R,4R)-3-fluoro-1-methylpiperidin-4-yl)thiazolidine-2,4-dione (26), a potent and selective inh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::88828a3d66c963401b5e0df09d341aef
https://doi.org/10.1021/op400325r
https://doi.org/10.1021/op400325r
Crystallization of a Cephalosporin and an ERR-1: Assembly of an Inexpensive Crystallization Platform
Autor:
Kenneth M. Wells, Lian Huang, Bao-Ping Zhao, Ronald K. Russell, Scott Youells, Derek A. Beauchamp, Zhiyong Hu, Steven J. Mehrman, Adam Fermier, Gilles Bignan, Xun Li, Micheal Gaul, James V. Weber, Mark J. Macielag, Guozhang Xu, Wenju Wu
Publikováno v:
Crystal Growth & Design. 13:4635-4641
Finding a stable crystalline form of a small molecule API can be a daunting task given short timelines and the importance of having a crystal form in the development of the molecule. Crystalline forms of small molecules are sought for various reasons
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::74fbfe37cd234cba19d9e5b76e78e481
https://doi.org/10.1021/cg401147b
https://doi.org/10.1021/cg401147b
Autor:
Zhihua Sui, Derek A. Beauchamp, Christopher A. Teleha, Ronald K. Russell, Chaozhong Cai, Fu-An Kang
Publikováno v:
Tetrahedron: Asymmetry. 24:651-656
Two cycloaddition methods were applied to chiral protected aminocyclopentenes 2 and 9 and provided novel bicyclic products 3 and 4 in good yields. The explanation for the observed stereochemistry was based on the sterically encumbered β-face forcing
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a63aa46f9ea716d2c141f8aca41fa9c1
https://doi.org/10.1016/j.tetasy.2013.04.014
https://doi.org/10.1016/j.tetasy.2013.04.014
Autor:
Kenneth M. Wells, Xun Li, Sandra Damon, Shawn Branum, William V. Murray, David Palmer, Ronald K. Russell, Scott Youells, Derek A. Beauchamp, Stephen M. Stefanick
Publikováno v:
Organic Process Research & Development. 16:1727-1732
A practical synthesis of two N-glycoside indoles 1 and 2, identified as highly potent sodium-dependent glucose transporter (SGLT) inhibitors is described. Highlights of the synthetic process include a selective and quantitative Vilsmeier acylation an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::540ba2843e6df08b5ab82fc05020c3ea
https://doi.org/10.1021/op3001355
https://doi.org/10.1021/op3001355
Autor:
Devraj Chakravarty, Sandra Damon, Kenneth J. Rhodes, Mark Ault, Robert H. Scannevin, Lori Westover, Xun Li, Vernon C. Alford, Aihua Wang, Heng-Keang Lim, Lisa Lampron, Jeffrey Crooke, Scott Youells, Paul F. Jackson, Ronald K. Russell, J. Kent Barbay, Mark T. Powell, Stefanie Rassnick, Derek A. Beauchamp, Shawn Branum, Kenneth M. Wells, Kristi A. Leonard, Nathaniel H. Wallace, Karen Carroll, Brian C. Shook
Publikováno v:
Journal of Medicinal Chemistry. 55:1402-1417
The design and characterization of two, dual adenosine A2A/A1 receptor antagonists in several animal models of Parkinson's disease is described. Compound 1 was previously reported as a potential treatment for Parkinson's disease. Further characteriza
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ee5bfe2808914e06827f196af1afcb35
https://doi.org/10.1021/jm201640m
https://doi.org/10.1021/jm201640m
Autor:
Brian C. Shook, Kenneth C. Rupert, Stefanie Rassnick, Hall Daniel A, Scott Davis, Sandra Damon, Reyes Mayra B, Lori Westover, Melville C. Osborne, Scott Youells, Yuting Tang, Ronald K. Russell, Keith T. Demarest, Xun Li, Paul F. Jackson, Shawn Branum, Devraj Chakravarty, Derek A. Beauchamp, Kristin Hansen, Kenneth J. Rhodes, David C. Palmer, James L. Bullington, Geoffrey R. Heintzelman, Kenneth M. Wells, Jamie Boulet
Publikováno v:
Journal of Medicinal Chemistry. 53:8104-8115
The in vivo characterization of a dual adenosine A(2A)/A(1) receptor antagonist in several animal models of Parkinson's disease is described. Discovery and scale-up syntheses of compound 1 are described in detail, highlighting optimization steps that
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4a3abc6b1bb2388ce859a84328d2aeb
https://doi.org/10.1021/jm100971t
https://doi.org/10.1021/jm100971t
Autor:
Sandra Damon, Lori Westover, Kenneth C. Rupert, Ronald K. Russell, Xun Li, Devraj Chakravarty, Paul F. Jackson, Brian Magliaro, Yuting Tang, Geoffrey R. Heintzelman, Kenneth M. Wells, Stefanie Rassnick, Shawn Branum, Mel Osbourne, Karen Carroll, Kenneth J. Rhodes, James L. Bullington, Robert H. Scannevin, Keith T. Demarest, Lisa Lampron, Brian C. Shook, Scott Youells, Kristen Hansen, Hall Daniel A
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2864-2867
A novel series of arylindenopyrimidines were identified as A(2A) and A(1) receptor antagonists. The series was optimized for in vitro activity by substituting the 8- and 9-positions with methylene amine substituents. The compounds show excellent acti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f81d5b2a5b35b6c6aec43edf95869ec0
https://doi.org/10.1016/j.bmcl.2010.03.042
https://doi.org/10.1016/j.bmcl.2010.03.042