Zobrazeno 1 - 10
of 39
pro vyhledávání: '"Leonard L, Winneroski"'
Autor:
Hao Sun, Michael O. Frederick, Roger Ryan Rothhaar, Amy C. DeBaillie, Brian Morgan Watson, Carlos Mateos, Leonard L. Winneroski, Carlos Jaramillo, Talbi Kaoudi, Matthew Johnson, Pablo Garcia-Losada, Srinivas Gangula, Peter J. Lindsay-Scott, Steven James Green, Dustin J. Mergott, Dajiang Jing, Marvin M. Hansen, José Eugenio de Diego, Juan A. Rincón, Kevin D. Seibert, Lei Zhang, Jiuyuan Li
Publikováno v:
Organic Process Research & Development. 24:306-314
Herein we report a summary of the synthetic development of LY3202626 from the initial discovery route to a final route that was scaled to make 150 kg. Key developments include the use of a [3 + 2] ...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bd409beaf54c99668ae6510bc63b7fdb
https://doi.org/10.1021/acs.oprd.9b00471
https://doi.org/10.1021/acs.oprd.9b00471
Autor:
Brian A. Willis, Stephen L. Lowe, Scott A. Monk, Patrick J. Cocke, Christopher D. Aluise, Leonard N. Boggs, Anthony R. Borders, Richard A. Brier, Robert A. Dean, Steven J. Green, Douglas E. James, Stanford S. Jhee, Qun Lin, Albert C. Lo, Patrick C. May, Brian M. Watson, Leonard L. Winneroski, Zhixiang Yang, Jennifer A. Zimmer, David L. McKinzie, Dustin J. Mergott
Publikováno v:
Journal of Alzheimer's disease reports. 6(1)
Background: The development of beta-site amyloid-beta precursor protein cleaving enzyme (BACE) 1 inhibitors for the treatment of Alzheimer’s disease requires optimization of inhibitor potency, selectivity, and brain penetration. Moreover, there is
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::912368ce5d97e52cb749b71026a53952
https://pubmed.ncbi.nlm.nih.gov/35243208
https://pubmed.ncbi.nlm.nih.gov/35243208
Autor:
Stephanie L. Stout, Leonard L. Winneroski, Jorg Hendle, Warren J. Porter, Patrick J. C. May, Leonard N. Boggs, Thomas K. Baker, James P. Beck, Steven James Green, Anthony R. Borders, Erik James Hembre, Stephen L. Lowe, Christopher D Aluise, David L. McKinzie, Brian Morgan Watson, Brian Michael Mathes, Jon A. Erickson, Zhixiang Yang, Patrick J Cocke, Dustin J. Mergott, Brian A. Willis, Scott A. Monk, Pablo Garcia-Losada, David E. Timm, Richard A. Brier, Jose Eduardo Lopez
Publikováno v:
Journal of medicinal chemistry. 64(12)
The beta-site APP cleaving enzyme 1, known as BACE1, has been a widely pursued Alzheimer's disease drug target owing to its critical role in the production of amyloid-beta. We have previously reported the clinical development of LY2811376 and LY28867
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::698057ee408d2f35c662510d099e51b3
https://pubmed.ncbi.nlm.nih.gov/34081466
https://pubmed.ncbi.nlm.nih.gov/34081466
Autor:
Leonard L. Winneroski, Dustin J. Mergott, Amy C. DeBaillie, Yuan Shi, Brian Morgan Watson, Francisco Martínez-Olid, Carolina Alhambra Jimenez, Mario Barberis, Chauncey D. Jones, Pablo Garcia-Losada, Erik James Hembre
Publikováno v:
Organic Process Research & Development. 22:650-654
Here we report an optimized protocol for the asymmetric introduction of a fluorine atom into a quaternary center facilitated by d-proline, Selectfluor®, and trifluoroethanol. The synthesis proceeds over four steps starting from a chiral amino alcoho
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::605c2844dfb8d56a6a2a8fae33d2b3e2
https://doi.org/10.1021/acs.oprd.8b00069
https://doi.org/10.1021/acs.oprd.8b00069
Autor:
David E. Timm, Leonard N. Boggs, Brian Michael Mathes, Yuan Shi, Mario Barberis, Zhixiang Yang, Dustin J. Mergott, Scott A. Monk, Pablo Garcia-Losada, Jose Miguel Minguez, Leonard L. Winneroski, Jon A. Erickson, Richard A. Brier, Anthony R. Borders, Stephanie L. Stout, Porter Warren J, Zoran Rankovic, Jose Eduardo Lopez, Erik James Hembre, James E. Audia, Jorg Hendle, James P. Beck, Steven James Green, Brian Morgan Watson, Patrick C. May, Robert D. Boyer
Publikováno v:
Bioorganic & Medicinal Chemistry. 28:115194
Inhibition of BACE1 has become an important strategy in the quest for disease modifying agents to slow the progression of Alzheimer's disease. We previously reported the fragment-based discovery of LY2811376, the first BACE1 inhibitor reported to dem
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::686975880a947f8f81325a11d876e66b
https://doi.org/10.1016/j.bmc.2019.115194
https://doi.org/10.1016/j.bmc.2019.115194
Autor:
Patrick C. May, Richard A. Brier, Leonard N. Boggs, David L. McKinzie, Leonard L. Winneroski, Anthony R. Borders, Steven James Green, Zhixiang Yang, Dustin J. Mergott, Scott A. Monk
Publikováno v:
Alzheimer's & Dementia. 12
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bb3fe393c7ae5674f4f9d6f9c640bd63
https://doi.org/10.1016/j.jalz.2016.06.1693
https://doi.org/10.1016/j.jalz.2016.06.1693
Autor:
Brian A. Willis, Zhixiang Yang, Dustin J. Mergott, Scott A. Monk, Richard A. Brier, Anthony R. Borders, Patrick J. C. May, Steven James Green, David L. McKinzie, Leonard L. Winneroski, Leonard N. Boggs
Publikováno v:
Alzheimer's & Dementia. 12
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ce9117800559ea83b6343abfc6cabbe1
https://doi.org/10.1016/j.jalz.2016.06.828
https://doi.org/10.1016/j.jalz.2016.06.828
Autor:
Yanping Xu, Nathan Bryan Mantlo, Fatima Iradier, Leonard L. Winneroski, Gary J. Etgen, Chahrzad Montrose-Rafizadeh, Carol L. Broderick, Jason Eric Lamar, Nathan Yumibe, Richard W. Zink, Brian A. Oldham, Jeremy Schulenburg York, Isabel C. Gonzalez
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1052-1055
The design and synthesis of dual PPAR γ/δ agonist (R)-3-{2-ethyl-4-[3-(4-ethyl-2-pyridin-2-yl-phenoxy)-butoxy]-phenyl}propionic acid is described. This compound dose-dependently lowered plasma glucose in hyperglycemic male Zucker diabetic fatty (ZD
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::15ce50b2bfd928c1d1472b197a929097
https://doi.org/10.1016/j.bmcl.2006.11.029
https://doi.org/10.1016/j.bmcl.2006.11.029
Autor:
Stephanie L. Stout, Patrick C. May, Brian Morgan Watson, Pablo Garcia Losada, Valentine J. Klimkowski, Brian Michael Mathes, David E. Timm, Dustin J. Mergott, Scott A. Monk, Leonard L. Winneroski, Leonard N. Boggs, James P. Beck, James E. Audia, Matthew Allen Schiffler, Richard A. Brier, Anthony R. Borders, Jon A. Erickson, Robert D. Boyer, Kevin John Hudziak
Publikováno v:
Bioorganicmedicinal chemistry. 23(13)
The BACE1 enzyme is a key target for Alzheimer’s disease. During our BACE1 research efforts, fragment screening revealed that bicyclic thiazine 3 had low millimolar activity against BACE1. Analysis of the co-crystal structure of 3 suggested that po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::01477228c3c9d6ec449c18a60008a90e
https://pubmed.ncbi.nlm.nih.gov/26001341
https://pubmed.ncbi.nlm.nih.gov/26001341
Autor:
Brian Michael Mathes, Zhixiang Yang, Dustin J. Mergott, Scott A. Monk, Hykop Gevorkyan, Larry Ereshefsky, Vaught Grant Matthews, Leonard L. Winneroski, Jon A. Erickson, Stephen L. Lowe, Celedon Gonzales, Scott Martin Sheehan, David E. Timm, Brian Morgan Watson, Ferenc Martenyi, David O. Calligaro, Stephanie L. Stout, Theresa A. Day, Richard A. Brier, Patrick J Cocke, Brian A. Willis, Stanford Jhee, Leonard N. Boggs, Robert A. Dean, James E. Audia, Steven F. Komjathy, Anthony R. Borders, Terry D. Lindstrom, Patrick C. May, Douglas E. James, Linglin Li
BACE1 is a key protease controlling the formation of amyloid β, a peptide hypothesized to play a significant role in the pathogenesis of Alzheimer's disease (AD). Therefore, the development of potent and selective inhibitors of BACE1 has been a focu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f78c69adc5fae76e66024d7197aeccfc
https://europepmc.org/articles/PMC6605527/
https://europepmc.org/articles/PMC6605527/
