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)
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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)
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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)
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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)
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Synthesis and Preclinical Characterization of LY3154885, a Human Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Nonclinical Drug–Drug Interaction Risk Profile
Hao, Junliang, Beck, James, Zhou, Xin, Lackner, Gregory L, Johnston, Richard, Reinhard, Matt, Goldsmith, Paul, Hollinshead, Sean, Dehlinger, Veronique, Filla, Sandra A, Wang, Xu-shan, Richardson, Jeffery, Posada, Maria, Mohutsky, Mike, Schober, Doug, Katner, Jason S, Chen, Qi, Hu, Bingjie, Remick, David M, Coates, David A, Mathes, Brian M, Hawk, Mai K, Svensson, Kjell A, Hembre, Erik
Published in Journal of medicinal chemistry (10.03.2022)
Published in Journal of medicinal chemistry (10.03.2022)
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Two Prodrugs of Potent and Selective GluR5 Kainate Receptor Antagonists Actives in Three Animal Models of Pain
Dominguez, Esteban, Iyengar, Smriti, Shannon, Harlan E, Bleakman, David, Alt, Andrew, Arnold, Brian M, Bell, Michael G, Bleisch, Thomas J, Buckmaster, Jennifer L, Castano, Ana M, Del Prado, Miriam, Escribano, Ana, Filla, Sandra A, Ho, Ken H, Hudziak, Kevin J, Jones, Carrie K, Martinez-Perez, Jose A, Mateo, Ana, Mathes, Brian M, Mattiuz, Edward L, Ogden, Ann Marie L, Simmons, Rosa Maria A, Stack, Douglas R, Stratford, Robert E, Winter, Mark A, Wu, Zhipei, Ornstein, Paul L
Published in Journal of medicinal chemistry (30.06.2005)
Published in Journal of medicinal chemistry (30.06.2005)
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Defining Target Engagement Required for Efficacy In Vivo at the Retinoic Acid Receptor-Related Orphan Receptor C2 (RORγt)
Lugar, Charles W, Clarke, Christian A, Morphy, Richard, Rudyk, Helene, Sapmaz, Selma, Stites, Ryan E, Vaught, Grant M, Furness, Kelly, Broughton, Howard B, Durst, Greg L, Clawson, David K, Stout, Stephanie L, Guo, Sherry Y, Durbin, Jim D, Stayrook, Keith R, Edmondson, Denise D, Kikly, Kristy, New, Nicole E, Bina, Holly A, Chambers, Mark G, Shetler, Pamela, Chang, William Y, Chang, Veavi Ching-Yun, Barr, Rob, Gough, Wendy H, Steele, Jimmy P, Getman, Brian, Patel, Nita, Mathes, Brian M, Richardson, Timothy I
Published in Journal of medicinal chemistry (13.05.2021)
Published in Journal of medicinal chemistry (13.05.2021)
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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)
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Ethyl (3S,4aR,6S,8aR)-6-(4-Ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso- quinoline-3-carboxylic Ester: A Prodrug of a GluR5 Kainate Receptor Antagonist Active in Two Animal Models of Acute Migraine
Filla, Sandra A, Winter, Mark A, Johnson, Kirk W, Bleakman, David, Bell, Michael G, Bleisch, Thomas J, Castaño, Ana M, Clemens-Smith, Amy, del Prado, Miriam, Dieckman, Donna K, Dominguez, Esteban, Escribano, Ana, Ho, Ken H, Hudziak, Kevin J, Katofiasc, Mary A, Martinez-Perez, Jose A, Mateo, Ana, Mathes, Brian M, Mattiuz, Edward L, Ogden, Ann Marie L, Phebus, Lee A, Stack, Douglas R, Stratford, Robert E, Ornstein, Paul L
Published in Journal of medicinal chemistry (26.09.2002)
Published in Journal of medicinal chemistry (26.09.2002)
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GluK1 antagonists from 6-(tetrazolyl)phenyl decahydroisoquinoline derivatives: In vitro profile and in vivo analgesic efficacy
Martinez-Perez, Jose A., Iyengar, Smriti, Shannon, Harlan E., Bleakman, David, Alt, Andrew, Clawson, David K., Arnold, Brian M., Bell, Michael G., Bleisch, Thomas J., Castaño, Ana M., Del Prado, Miriam, Dominguez, Esteban, Escribano, Ana M., Filla, Sandra A., Ho, Ken H., Hudziak, Kevin J., Jones, Carrie K., Mateo, Ana, Mathes, Brian M., Mattiuz, Edward L., Ogden, Ann Marie L., Simmons, Rosa Maria A., Stack, Douglas R., Stratford, Robert E., Winter, Mark A., Wu, Zhipei, Ornstein, Paul L.
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
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GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models
Martinez-Perez, Jose A., Iyengar, Smriti, Shannon, Harlan E., Bleakman, David, Alt, Andrew, Arnold, Brian M., Bell, Michael G., Bleisch, Thomas J., Castaño, Ana M., Del Prado, Miriam, Dominguez, Esteban, Escribano, Ana M., Filla, Sandra A., Ho, Ken H., Hudziak, Kevin J., Jones, Carrie K., Mateo, Ana, Mathes, Brian M., Mattiuz, Edward L., Ogden, Ann Marie L., Simmons, Rosa Maria A., Stack, Douglas R., Stratford, Robert E., Winter, Mark A., Wu, Zhipei, Ornstein, Paul L.
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
Published in Bioorganic & medicinal chemistry letters (01.12.2013)
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Novel Potent 5-HT1F Receptor Agonists: Structure−Activity Studies of a Series of Substituted N-[3-(1-Methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides
Filla, Sandra A, Mathes, Brian M, Johnson, Kirk W, Phebus, Lee A, Cohen, Marlene L, Nelson, David L, Zgombick, John M, Erickson, Jon A, Schenck, Kathryn W, Wainscott, David B, Branchek, Theresa A, Schaus, John M
Published in Journal of medicinal chemistry (03.07.2003)
Published in Journal of medicinal chemistry (03.07.2003)
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Substituted furo[3,2-b]pyridines: novel bioisosteres of 5-HT1F receptor agonists
MATHES, Brian M, HUDZIAK, Kevin J, FILLA, Sandra A, SCHAUS, John M, XU, Yao-Chang, NELSON, David L, WAINSCOTT, David B, NUTTER, Suzanne E, GOUGH, Wendy H, BRANCHEK, Theresa A, ZGOMBICK, John M
Published in Bioorganic & medicinal chemistry letters (05.01.2004)
Published in Bioorganic & medicinal chemistry letters (05.01.2004)
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Substituted furo[3,2- b]pyridines: novel bioisosteres of 5-HT 1F receptor agonists
Mathes, Brian M., Hudziak, Kevin J., Schaus, John M., Xu, Yao-Chang, Nelson, David L., Wainscott, David B., Nutter, Suzanne E., Gough, Wendy H., Branchek, Theresa A., Zgombick, John M., Filla, Sandra A.
Published in Bioorganic & medicinal chemistry letters (05.01.2004)
Published in Bioorganic & medicinal chemistry letters (05.01.2004)
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Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT1F receptor agonists: Evolution from bicyclic to monocyclic cores
Zhang, Deyi, Blanco, Maria-Jesus, Ying, Bai-Ping, Kohlman, Daniel, Liang, Sidney X., Victor, Frantz, Chen, Qi, Krushinski, Joseph, Filla, Sandra A., Hudziak, Kevin J., Mathes, Brian M., Cohen, Michael P., Zacherl, DeAnna, Nelson, David L.G., Wainscott, David B., Nutter, Suzanne E., Gough, Wendy H., Schaus, John M., Xu, Yao-Chang
Published in Bioorganic & medicinal chemistry letters (01.10.2015)
Published in Bioorganic & medicinal chemistry letters (01.10.2015)
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Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT₁ F receptor agonists: Evolution from bicyclic to monocyclic cores
Zhang, Deyi, Blanco, Maria-Jesus, Ying, Bai-Ping, Kohlman, Daniel, Liang, Sidney X, Victor, Frantz, Chen, Qi, Krushinski, Joseph, Filla, Sandra A, Hudziak, Kevin J, Mathes, Brian M, Cohen, Michael P, Zacherl, DeAnna, Nelson, David L G, Wainscott, David B, Nutter, Suzanne E, Gough, Wendy H, Schaus, John M, Xu, Yao-Chang
Published in Bioorganic & medicinal chemistry letters (01.10.2015)
Published in Bioorganic & medicinal chemistry letters (01.10.2015)
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Journal Article
Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain : 2005 American Chemical Society Award for Computers in Chemical and Pharmaceutical Research
DOMINGUEZ, Esteban, IYENGAR, Smriti, DEL PRADO, Miriam, ESCRIBANO, Ana, FILLA, Sandra A, HO, Ken H, HUDZIAK, Kevin J, JONES, Carrie K, MARTINEZ-PEREZ, Jose A, MATEO, Ana, MATHES, Brian M, MATTIUZ, Edward L, SHANNON, Harlan E, OGDEN, Ann Marie L, SIMMONS, Rosa Maria A, STACK, Douglas R, STRATFORD, Robert E, WINTER, Mark A, ZHIPEI WU, ORNSTEIN, Paul L, BLEAKMAN, David, ALT, Andrew, ARNOLD, Brian M, BELL, Michael G, BLEISCH, Thomas J, BUCKMASTER, Jennifer L, CASTANO, Ana M
Published in Journal of medicinal chemistry (2005)
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Published in Journal of medicinal chemistry (2005)
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Novel potent 5-HT(1F) receptor agonists: structure-activity studies of a series of substituted N-[3-(1-methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides
Filla, Sandra A, Mathes, Brian M, Johnson, Kirk W, Phebus, Lee A, Cohen, Marlene L, Nelson, David L, Zgombick, John M, Erickson, Jon A, Schenck, Kathryn W, Wainscott, David B, Branchek, Theresa A, Schaus, John M
Published in Journal of medicinal chemistry (03.07.2003)
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Published in Journal of medicinal chemistry (03.07.2003)
Journal Article
Novel Potent 5-HT 1F Receptor Agonists: Structure−Activity Studies of a Series of Substituted N -[3-(1-Methyl-4-piperidinyl)-1 H -pyrrolo[3,2- b ]pyridin-5-yl]amides
Filla, Sandra A., Mathes, Brian M., Johnson, Kirk W., Phebus, Lee A., Cohen, Marlene L., Nelson, David L., Zgombick, John M., Erickson, Jon A., Schenck, Kathryn W., Wainscott, David B., Branchek, Theresa A., Schaus, John M.
Published in Journal of medicinal chemistry (01.07.2003)
Published in Journal of medicinal chemistry (01.07.2003)
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