Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Eric R. Ashley"'
Autor:
Juana Du, Eric R. Ashley, Cedric L. Hugelshofer, Tao Ji, Wensheng Yu, Yeon-Hee Lim, Bin Hu, Srinivas Karampuri, Jianming Bao, Krishna Ethiraj, Dejun Liu, Ramu Rondla, Vishal Sharma
Publikováno v:
Organic Letters. 23:943-947
We provide an account of synthetic strategies aimed at the efficient preparation of 4-amino-4-methyltetrahydro-2H-thiopyran 1,1-dioxide (3), an important cyclic sulfone building block for medicinal chemistry. A practical and scalable protocol has bee
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9687944c0f52f3de335596c24d09aac6
https://doi.org/10.1021/acs.orglett.0c04141
https://doi.org/10.1021/acs.orglett.0c04141
Autor:
Barbara Pio, Ravi P. Nargund, Yan Guo, Daniel Kosinski, Josien Hubert B, Michael Wright, Michele Pachanski, Harry R. Chobanian, Xiaoping Zhang, Richard Tschirret-Guth, Melissa Kirkland, Andrew D. Howard, Sarah Souza, Eric R. Ashley, Robert K. Orr, Steven L. Colletti, Joel Mane, Jerry Di Salvo, Michael W. Miller, Boonlert Cheewatrakoolpong, Koppara Samuel, William K. Hagmann, James Lamca, Juliann Ehrhart, Maria E. Trujillo, Jackie Shang, Qing Chen, Adam B. Weinglass, Randal M. Bugianesi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:1842-1848
GPR40 (FFAR1 or FFA1) is a G protein-coupled receptor, primarily expressed in pancreatic islet β-cells and intestinal enteroendocrine cells. When activated by fatty acids, GPR40 elicits increased insulin secretion from islet β-cells only in the pre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::67130fd906c302e54806df711af08d1b
https://doi.org/10.1016/j.bmcl.2019.04.050
https://doi.org/10.1016/j.bmcl.2019.04.050
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:938-944
The evolution of a scalable process for the preparation of methylcyclobutanol-pyridyl ether 1 is described. Key aspects of this development including careful control of the stereochemistry, elimination of chromatography, and application to kilogram-s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5c7274b0cedc16be5f8927aaf280144b
https://doi.org/10.1016/j.bmc.2017.07.018
https://doi.org/10.1016/j.bmc.2017.07.018
Autor:
Steven F. Oliver, Eric R. Ashley, Christopher Wise, Robert K. Orr, Eric B. Sirota, Rebecca T. Ruck, Joseph F. Leone, Jamie M. McCabe Dunn, Andrew Nolting, Andrew W. Gibson, Alan M. Hyde, Jon A. Jurica
Publikováno v:
Green Chemistry. 20:2519-2525
Herein we describe the route scouting and process development efforts toward a green and sustainable synthesis of the HCV NS5b cyclic prodrug nucleoside (CPN) 1. Through the discovery and development of a crystallization-induced dynamic resolution an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::cf888bc06ced66f7bc5ece659cc456ba
https://doi.org/10.1039/c8gc00102b
https://doi.org/10.1039/c8gc00102b
Autor:
Melissa Kirkland, M A Powles, Francisco Velazquez, Eric R. Ashley, Nengxue Wang, Shah Unmesh G, Feroze Ujjainwalla, Taro E. Akiyama, Eric J. Gilbert, Charles Lee Jayne, Michele Pachanski, Dan Zhou, Scott D. Edmondson, Jerry Di Salvo, Andreas Verras, Maria Madeira, Takao Suzuki, Srikanth Venkatraman, Quang Truong, Wu Yin, Gregory L. Adams, Shouwu Miao
Publikováno v:
ACS Medicinal Chemistry Letters. 8:96-101
GPR120 (FFAR4) is a fatty acid sensing G protein coupled receptor (GPCR) that has been identified as a target for possible treatment of type 2 diabetes. A selective activator of GPR120 containing a chromane scaffold has been designed, synthesized, an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f5c4bd187bc901f79299111d7c132c57
https://doi.org/10.1021/acsmedchemlett.6b00394
https://doi.org/10.1021/acsmedchemlett.6b00394
Autor:
Eric R. Ashley, Alan M. Hyde
Publikováno v:
Organometallics in Process Chemistry ISBN: 9783030279608
Within the field of process chemistry, all available methods of synthesis are typically considered for the preparation of complex targets. Early in development, speed and flexibility are paramount, but as larger quantities of clinical candidates are
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1723fa32891442285320ab23a1e1772b
https://doi.org/10.1007/3418_2019_30
https://doi.org/10.1007/3418_2019_30
Autor:
Birgit Kosjek, Oscar Alvizo, Nobuyoshi Yasuda, Mark A. Huffman, John Limanto, Eric R. Ashley, Zhijian Liu, Artis Klapars, Alan M. Hyde, Xiuyan Gu, Guiquan Liu, Yong-Li Zhong, Nicholas J. Agard, Lushi Tan, David M. Tschaen
Publikováno v:
Organic Letters. 18:5888-5891
A scalable and efficient synthesis of the GPR40 agonist MK-8666 was developed from a simple pyridine building block. The key step to set the stereochemistry at two centers relied on an enzymatic dynamic kinetic reduction of an unactivated ketone. Dir
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d1a98b5df619fcaaff680f336038241
https://doi.org/10.1021/acs.orglett.6b02910
https://doi.org/10.1021/acs.orglett.6b02910
Autor:
Eric R. Ashley, Gregory L. Beutner, Brendan Grau, Amude M. Kassim, Matthew D. Truppo, Jingjun Yin, John Limanto, Hallena R. Strotman, Zhijian Liu, Mary M. Kim, Artis Klapars
Publikováno v:
Organic Letters. 16:2716-2719
A novel synthesis of vernakalant is described. Using inexpensive and readily available reagents, the key transformations involve (1) an efficient zinc-amine-promoted etherification, (2) a highly stereoselective enzyme-catalyzed dynamic asymmetric tra
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::37cfe972d367530c2775b8385cb90fd9
https://doi.org/10.1021/ol501002a
https://doi.org/10.1021/ol501002a
Autor:
Gregory L, Adams, Francisco, Velazquez, Charles, Jayne, Unmesh, Shah, Shouwu, Miao, Eric R, Ashley, Maria, Madeira, Taro E, Akiyama, Jerry, Di Salvo, Takao, Suzuki, Nengxue, Wang, Quang, Truong, Eric, Gilbert, Dan, Zhou, Andreas, Verras, Melissa, Kirkland, Michele, Pachanski, Maryann, Powles, Wu, Yin, Feroze, Ujjainwalla, Srikanth, Venkatraman, Scott D, Edmondson
Publikováno v:
ACS medicinal chemistry letters. 8(1)
GPR120 (FFAR4) is a fatty acid sensing G protein coupled receptor (GPCR) that has been identified as a target for possible treatment of type 2 diabetes. A selective activator of GPR120 containing a chromane scaffold has been designed, synthesized, an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::b516664a4a45395b9f909635d7176636
https://pubmed.ncbi.nlm.nih.gov/28105282
https://pubmed.ncbi.nlm.nih.gov/28105282
Autor:
Christopher Joseph Sinz, Sarah Souza, Aimie M. Ogawa, Dennis Leung, Eric R. Ashley, Brande Thomas-Fowlkes, Maria Madeira, Mary Ann Powles, Effie Tozzo, Hong D. Chu, Feroze Ujjainwalla, Melissa Kirkland, Matthew Lombardo, Clare London, Jerry Di Salvo, Keith Eagen, John S. Debenham, Jason M. Cox, Ping Lan, Alejandro Crespo, Adam B. Weinglass, Taro E. Akiyama, Nengxue Wang, Henry M. Vaccaro, Michele Pachanski, Shah Unmesh G, Zhongxiang Sun, Mariappan V. Chelliah, James R. Tata, Michael A. Plotkin, Candice Alleyne, Takao Suzuki, Srikanth Venkatraman
Publikováno v:
ACS medicinal chemistry letters. 8(1)
Type 2 diabetes mellitus (T2DM) is an ever increasing worldwide epidemic, and the identification of safe and effective insulin sensitizers, absent of weight gain, has been a long-standing goal of diabetes research. G-protein coupled receptor 120 (GPR
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::28a251742e59339ae232f1fad2130722
https://pubmed.ncbi.nlm.nih.gov/28105274
https://pubmed.ncbi.nlm.nih.gov/28105274