Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Scott Youells"'
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
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:
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
Autor:
Scott Youells, Robert H. Scannevin, Mark T. Powell, Sandra Damon, Ronald K. Russell, Paul F. Jackson, Lori Westover, Lisa Lampron, Jeffrey Crooke, Karen Carroll, Kristen Hansen, Geoffrey R. Heintzelman, Kenneth M. Wells, Kenneth J. Rhodes, J. Kent Barbay, N. H. Wallace, Devraj Chakravarty, Stefanie Rassnick, Brian C. Shook, Aihua Wang, Hall Daniel A, Kenneth C. Rupert, Xun Li, Vernon C. Alford, Derek A. Beauchamp, Shawn Branum, Kristi A. Leonard, Mark Ault, James L. Bullington
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2868-2871
Two reactive metabolites were identified in vivo for the dual A2A/A1 receptor antagonist 1. Two strategies were implemented to successfully mitigate the metabolic liabilities associated with 1. Optimization of the arylindenopyrimidines led to a numbe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::353b6f972a700b3aa70793fd134b85a1
https://doi.org/10.1016/j.bmcl.2010.03.024
https://doi.org/10.1016/j.bmcl.2010.03.024
Autor:
Tobias Schmid, Mark J. Macielag, Armin Roessler, Xun Li, Roger Faessler, Michele A. Weidner-Wells, Ronald K. Russell, Scott Youells, Eugene B. Grant
Publikováno v:
Organic Preparations and Procedures International. 42:151-160
7-[4-(2-Amino-1-chloroethylidene)piperidin-1-yl]-1-cyclopropyl-6-fluoro-8-methoxy-4- oxo-1,4-dihydroquinoline-3-carboxylic acid (10) is a potent bacterial topoisomerase inhibitor. In vitro, compoun...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f47a2aca4cbe5e1f2bfe78c34778e6f2
https://doi.org/10.1080/00304941003680731
https://doi.org/10.1080/00304941003680731
Autor:
Ronald K. Russell, Yongzheng Zhang, Scott Youells, Xun Li, Gee-Hong Kuo, Lan Shen, Zhiyong Hu, Michael Reuman
Publikováno v:
Organic Process Research & Development. 11:1010-1014
The preparation of the PPARα,δ agonist 2-methyl-2-(2-methyl-4-(3-(4-(trifluoromethyl)phenyl)[1,2,4]thiadiazol-5-ylmethoxy)phenoxy)propionic acid sodium salt (17) is described and compared with earlier in-house preparations of this important target
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4337863a86c5a176075e322578c3cff0
https://doi.org/10.1021/op700141u
https://doi.org/10.1021/op700141u
Autor:
Shawn Branum, Ramesh M. Kanojia, Xun Li, Robert Ma, Ronald K. Russell, Nareshkumar F. Jain, Scott Youells, Sandra Beish, Richard E. Adams, Michael Reuman, Zhihua Sui, Jerry R. Roberts
Publikováno v:
Organic Process Research & Development. 11:414-421
Unsymmetrical benzopyranobenzopyran compounds are novel selective estrogen receptor modulators (SERMs). A reproducible and nonchromatographic process was developed to prepare multihundred gram quan...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3f4cb618e3ea2c58fe9d5bdadb95eb45
https://doi.org/10.1021/op700020f
https://doi.org/10.1021/op700020f