Loading…
Loading…
Discovery and clinical translation of ceperognastat, an O‐GlcNAcase (OGA) inhibitor, for the treatment of Alzheimer's disease
Kielbasa, William, Goldsmith, Paul, Donnelly, Kevin B., Nuthall, Hugh N., Shcherbinin, Sergey, Fleisher, Adam S., Hendle, Jörg, DuBois, Susan L., Lowe, Stephen L., Zhang, Feiyu Fred, Woerly, Eric M., Dreyfus, Nicolas J.‐F., Evans, David, Gilmore, Jeremy, Mancini, Michele, Constantinescu, Cristian C., Gunn, Roger N., Russell, David S., Collins, Emily C., Brys, Miroslaw, Hutton, Michael L., Mergott, Dustin J.
Published in Alzheimer's & dementia : translational research & clinical interventions (01.10.2024)
Published in Alzheimer's & dementia : translational research & clinical interventions (01.10.2024)
Get full text
Journal Article
Loading…
Total Synthesis of (-)-Spinosyn A
Mergott, Dustin J., Frank, Scott A., Roush, William R., Nicolaou, Kyriacos C.
Published in Proceedings of the National Academy of Sciences - PNAS (17.08.2004)
Published in Proceedings of the National Academy of Sciences - PNAS (17.08.2004)
Get full text
Journal Article
Loading…
Preparation and biological evaluation of conformationally constrained BACE1 inhibitors
Winneroski, Leonard L., Schiffler, Matthew A., Erickson, Jon A., May, Patrick C., Monk, Scott A., Timm, David E., Audia, James E., Beck, James P., Boggs, Leonard N., Borders, Anthony R., Boyer, Robert D., Brier, Richard A., Hudziak, Kevin J., Klimkowski, Valentine J., Garcia Losada, Pablo, Mathes, Brian M., Stout, Stephanie L., Watson, Brian M., Mergott, Dustin J.
Published in Bioorganic & medicinal chemistry (01.07.2015)
Published in Bioorganic & medicinal chemistry (01.07.2015)
Get full text
Journal Article
Loading…
Loading…
Robust Central Reduction of Amyloid-β in Humans with an Orally Available, Non-Peptidic β-Secretase Inhibitor
May, Patrick C., Dean, Robert A., Lowe, Stephen L., Martenyi, Ferenc, Sheehan, Scott M., Boggs, Leonard N., Monk, Scott A., Mathes, Brian M., Mergott, Dustin J., Watson, Brian M., Stout, Stephanie L., Timm, David E., Smith LaBell, Elizabeth, Gonzales, Celedon R., Nakano, Masako, Jhee, Stanford S., Yen, Mark, Ereshefsky, Larry, Lindstrom, Terry D., Calligaro, David O., Cocke, Patrick J., Greg Hall, D., Friedrich, Stuart, Citron, Martin, Audia, James E.
Published in The Journal of neuroscience (16.11.2011)
Published in The Journal of neuroscience (16.11.2011)
Get full text
Journal Article
Loading…
The Potent BACE1 Inhibitor LY2886721 Elicits Robust Central Aβ Pharmacodynamic Responses in Mice, Dogs, and Humans
May, Patrick C., Willis, Brian A., Lowe, Stephen L., Dean, Robert A., Monk, Scott A., Cocke, Patrick J., Audia, James E., Boggs, Leonard N., Borders, Anthony R., Brier, Richard A., Calligaro, David O., Day, Theresa A., Ereshefsky, Larry, Erickson, Jon A., Gevorkyan, Hykop, Gonzales, Celedon R., James, Douglas E., Jhee, Stanford S., Komjathy, Steven F., Li, Linglin, Lindstrom, Terry D., Mathes, Brian M., Martényi, Ferenc, Sheehan, Scott M., Stout, Stephanie L., Timm, David E., Vaught, Grant M., Watson, Brian M., Winneroski, Leonard L., Yang, Zhixiang, Mergott, Dustin J.
Published in The Journal of neuroscience (21.01.2015)
Published in The Journal of neuroscience (21.01.2015)
Get full text
Journal Article
Loading…
Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor
McKinzie, David L, Winneroski, Leonard L, Green, Steven J, Hembre, Erik J, Erickson, Jon A, Willis, Brian A, Monk, Scott A, Aluise, Christopher D, Baker, Thomas K, Lopez, Jose E, Hendle, Jörg, Beck, James P, Brier, Richard A, Boggs, Leonard N, Borders, Anthony R, Cocke, Patrick J, Garcia-Losada, Pablo, Lowe, Stephen L, Mathes, Brian M, May, Patrick C, Porter, Warren J, Stout, Stephanie L, Timm, David E, Watson, Brian M, Yang, Zhixiang, Mergott, Dustin J
Published in Journal of medicinal chemistry (24.06.2021)
Published in Journal of medicinal chemistry (24.06.2021)
Get full text
Journal Article
Loading…
Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints
Winneroski, Leonard L., Erickson, Jon A., Green, Steven J., Lopez, Jose E., Stout, Stephanie L., Porter, Warren J., Timm, David E., Audia, James E., Barberis, Mario, Beck, James P., Boggs, Leonard N., Borders, Anthony R., Boyer, Robert D., Brier, Richard A., Hembre, Erik J., Hendle, Jörg, Garcia-Losada, Pablo, Minguez, Jose Miguel, Mathes, Brian M., May, Patrick C., Monk, Scott A., Rankovic, Zoran, Shi, Yuan, Watson, Brian M., Yang, Zhixiang, Mergott, Dustin J.
Published in Bioorganic & medicinal chemistry (01.01.2020)
Published in Bioorganic & medicinal chemistry (01.01.2020)
Get full text
Journal Article
Loading…
Synthesis, Optimization, and Large-Scale Preparation of the Low-Dose Central Nervous System-Penetrant BACE1 Inhibitor LY3202626 via a [3 + 2] Nitrone Cycloaddition
Garcia-Losada, Pablo, DeBaillie, Amy C, Eugenio de Diego, Jose, Green, Steven J, Hansen, Marvin M, Jaramillo, Carlos, Johnson, Matt, Kaoudi, Talbi, Li, Jiuyuan, Lindsay-Scott, Peter J, Mateos, Carlos, Mergott, Dustin J, Rincon, Juan Antonio, Rothhaar, Roger R, Seibert, Kevin D, Watson, Brian M, Winneroski, Leonard L, Gangula, Srinivas, Jing, Dajiang, Sun, Hao, Zhang, Lei, Frederick, Michael O
Published in Organic process research & development (21.02.2020)
Published in Organic process research & development (21.02.2020)
Get full text
Journal Article
Loading…
Practical Asymmetric Fluorination Approach to the Scalable Synthesis of New Fluoroaminothiazine BACE Inhibitors
Garcia-Losada, Pablo, Barberis, Mario, Shi, Yuan, Hembre, Erik, Alhambra Jimenez, Carolina, Winneroski, Leonard L, Watson, Brian M, Jones, Chauncey, DeBaillie, Amy C, Martínez-Olid, Francisco, Mergott, Dustin J
Published in Organic process research & development (18.05.2018)
Published in Organic process research & development (18.05.2018)
Get full text
Journal Article
Loading…
Loading…
The Vinylogous Intramolecular Morita−Baylis−Hillman Reaction: Synthesis of Functionalized Cyclopentenes and Cyclohexenes with Trialkylphosphines as Nucleophilic Catalysts
Frank, Scott A, Mergott, Dustin J, Roush, William R
Published in Journal of the American Chemical Society (20.03.2002)
Published in Journal of the American Chemical Society (20.03.2002)
Get full text
Journal Article
Loading…
Robust Pharmacodynamic Effect of LY3202626, a Central Nervous System Penetrant, Low Dose BACE1 Inhibitor, in Humans and Nonclinical Species
Willis, Brian A., Lowe, Stephen L., Monk, Scott A., Cocke, Patrick J., Aluise, Christopher D., Boggs, Leonard N., Borders, Anthony R., Brier, Richard A., Dean, Robert A., Green, Steven J., James, Douglas E., Jhee, Stanford S., Lin, Qun, Lo, Albert C., May, Patrick C., Watson, Brian M., Winneroski, Leonard L., Yang, Zhixiang, Zimmer, Jennifer A., McKinzie, David L., Mergott, Dustin J.
Published in JAD reports (01.01.2022)
Published in JAD reports (01.01.2022)
Get full text
Journal Article
Loading…
A CORRELATIONAL ANALYSIS OF EXPOSURE AND PHARMACODYNAMIC EFFECTS OF THE BACE1 INHIBITOR LY3202626 IN PDAPP MICE FOLLOWING ACUTE ORAL DOSING
Boggs, Leonard N, May, Patrick C, Yang, Zhixiang, Brier, Richard A, Monk, Scott A, Borders, Anthony R, Winneroski, Leonard L, Green, Steven J, Mergott, Dustin J, McKinzie, David L
Published in Alzheimer's & dementia (01.07.2016)
Published in Alzheimer's & dementia (01.07.2016)
Get full text
Journal Article
Loading…
NONCLINICAL PHARMACOLOGICAL CHARACTERIZATION OF THE BACE1 INHIBITOR LY3202626
McKinzie, David L, May, Patrick C, Boggs, Leonard N, Yang, Zhixiang, Brier, Richard A, Monk, Scott A, Willis, Brian A, Borders, Anthony R, Winneroski, Leonard L, Green, Steven J, Mergott, Dustin J
Published in Alzheimer's & dementia (01.07.2016)
Published in Alzheimer's & dementia (01.07.2016)
Get full text
Journal Article
Loading…
COMBINATION THERAPY WITH A PLAQUE-SPECIFIC ABETA ANTIBODY AND A BACE INHIBITOR RESULTS IN DRAMATIC PLAQUE REDUCTION IN A DOSE-DEPENDENT MANNER IN AGED PDAPP TRANSGENIC MICE
Hole, Justin T, Racke, Margaret M, Tzaferis, John A, Liu, Feng, Oluoch, Herold, Ahmed, Zeshan, Fisher, Alice, Anderson, Wesley, Iversent, Philip, Gonzales, Celedon, Yang, Zhixiang, Boggs, Leonard N, Monk, Scott A, Mergott, Dustin J, Yang, Ying YT, Lu, Jirong, Irizarry, Michael C, Sims, John R, May, Patrick C, Hutton, Michael, Nordstedt, Christer, DeMattos, Ronald B
Published in Alzheimer's & dementia (01.07.2016)
Published in Alzheimer's & dementia (01.07.2016)
Get full text
Journal Article
Loading…
A COMPARISON OF IN VIVO POTENCY IN TWO BACE INHIBITORS AS DETERMINED IN HUMANS AND DOGS
Willis, Brian A, May, Patrick C, Monk, Scott A, Lowe, Stephen L, Friedrich, Stuart, Mergott, Dustin J, Boggs, Leonard, Gevorkyan, Hakop, Jhee, Stan, Dean, Robert A, Nakano, Masako, Gonzales, Celedon R
Published in Alzheimer's & dementia (01.07.2014)
Published in Alzheimer's & dementia (01.07.2014)
Get full text
Journal Article
Loading…
Investigation of dose-responses and longitudinal effects of combination therapy with a plaque-specific amyloid beta antibody and bace inhibitor in aged transgenic mice
DeMattos, Ronald B, Racke, Margaret M, Hole, Justin T, Tzaferis, John A, Liu, Feng, Ahmed, Zeshan, Fisher, Alice, Day, Theresa A, Anderson, Wesley, Iversent, Philip, Gonzales, Celedon, Yang, Zhixiang, Boggs, Leonard, Monk, Scott A, Mergott, Dustin J, Yang, Ying Y.T, Lu, Jirong, Irizarry, Michael C, Sims, John R, May, Patrick C, Hutton, Michael L, Nordstedt, Christer
Published in Alzheimer's & dementia (01.07.2015)
Published in Alzheimer's & dementia (01.07.2015)
Get full text
Journal Article