Zobrazeno 1 - 10
of 36
pro vyhledávání: '"Dustin J. Mergott"'
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] ...
Autor:
Stephen L Lowe, Paul Goldsmith, Krista M Phipps, Donnelly B Kevin, Kevin Biglan, Michele Mancini, Hugh Norman Nuthall, Dustin J. Mergott, William Kielbasa
Publikováno v:
Alzheimer's & Dementia. 17
Autor:
William Kielbasa, Sergey Shcherbinin, Paul Goldsmith, Krista M Phipps, Kevin Biglan, Michele Mancini, David Russell, Cristian Constantinescu, Roger N Gunn, Hugh Norman Nuthall, Dustin J. Mergott, Stephen L Lowe, Emily C Collins
Publikováno v:
Alzheimer's & Dementia. 17
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
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
Autor:
Nicolas Dreyfus, James Tseng, Susan Warner, Emily C. Collins, Cristian Constantinescu, Hugh Nuthall, Sergey Shcherbinin, Fanni Natanegara, Roger N. Gunn, Krista M Phipps, Donnelly B. Kevin, Kevin Biglan, Mai Khanh Hawk, Stephen L. Lowe, Susan DuBois, David Russell, J.A. Gilmore, William Kielbasa, Peter J. Lindsay-Scott, Dustin J. Mergott, Xiaoyu Zhang, Nicholas McDonald
Publikováno v:
Alzheimer's & Dementia. 16
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
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
Autor:
Theresa A. Day, David L. McKinzie, Patricia Gonzalez-DeWhitt, Francis David Tingley, Ronald B. DeMattos, David R. Riddell, Dustin J. Mergott, Nicholas C. Reising, Mansuo L. Hayashi, Justin T. Hole
Publikováno v:
Alzheimer's & Dementia. 14
Publikováno v:
Organic Process Research & Development. 19:347-351
Here, we report a continuous flow protocol for the [3 + 2] cycloaddition of nitrones, in situ generated from oximes, into bicyclic isoxazolidines. This thermal process required very high temperatures to be efficient that were not easily reached in co