Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase–Glucokinase Regulatory Protein (GK–GKRP) Binding: Strategic Use of a N → S (nN → σS–X) Interaction for Conformational Constraint
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Published in Journal of medicinal chemistry (24.12.2015)
Published in Journal of medicinal chemistry (24.12.2015)
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Design and Preparation of a Potent Series of Hydroxyethylamine Containing β-Secretase Inhibitors That Demonstrate Robust Reduction of Central β-Amyloid
Weiss, Matthew M, Williamson, Toni, Babu-Khan, Safura, Bartberger, Michael D, Brown, James, Chen, Kui, Cheng, Yuan, Citron, Martin, Croghan, Michael D, Dineen, Thomas A, Esmay, Joel, Graceffa, Russell F, Harried, Scott S, Hickman, Dean, Hitchcock, Stephen A, Horne, Daniel B, Huang, Hongbing, Imbeah-Ampiah, Ronke, Judd, Ted, Kaller, Matthew R, Kreiman, Charles R, La, Daniel S, Li, Vivian, Lopez, Patricia, Louie, Steven, Monenschein, Holger, Nguyen, Thomas T, Pennington, Lewis D, Rattan, Claire, San Miguel, Tisha, Sickmier, E.Allen, Wahl, Robert C, Wen, Paul H, Wood, Stephen, Xue, Qiufen, Yang, Bryant H, Patel, Vinod F, Zhong, Wenge
Published in Journal of medicinal chemistry (08.11.2012)
Published in Journal of medicinal chemistry (08.11.2012)
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Design and Synthesis of Potent, Orally Efficacious Hydroxyethylamine Derived β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors
Dineen, Thomas A, Weiss, Matthew M, Williamson, Toni, Acton, Paul, Babu-Khan, Safura, Bartberger, Michael D, Brown, James, Chen, Kui, Cheng, Yuan, Citron, Martin, Croghan, Michael D, Dunn, Robert T, Esmay, Joel, Graceffa, Russell F, Harried, Scott S, Hickman, Dean, Hitchcock, Stephen A, Horne, Daniel B, Huang, Hongbing, Imbeah-Ampiah, Ronke, Judd, Ted, Kaller, Matthew R, Kreiman, Charles R, La, Daniel S, Li, Vivian, Lopez, Patricia, Louie, Steven, Monenschein, Holger, Nguyen, Thomas T, Pennington, Lewis D, San Miguel, Tisha, Sickmier, E. Allen, Vargas, Hugo M, Wahl, Robert C, Wen, Paul H, Whittington, Douglas A, Wood, Stephen, Xue, Qiufen, Yang, Bryant H, Patel, Vinod F, Zhong, Wenge
Published in Journal of medicinal chemistry (08.11.2012)
Published in Journal of medicinal chemistry (08.11.2012)
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Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 1. Discovery of a Novel Tool Compound for in Vivo Proof-of-Concept
Ashton, Kate S., Andrews, Kristin L., Bryan, Marion C., Chen, Jie, Chen, Kui, Chen, Michelle, Chmait, Samer, Croghan, Michael, Cupples, Rod, Fotsch, Christopher, Helmering, Joan, Jordan, Steve R., Kurzeja, Robert J. M., Michelsen, Klaus, Pennington, Lewis D., Poon, Steve F., Sivits, Glenn, Van, Gwyneth, Vonderfecht, Steve L., Wahl, Robert C., Zhang, Jiandong, Lloyd, David J., Hale, Clarence, St. Jean, David J.
Published in Journal of medicinal chemistry (23.01.2014)
Published in Journal of medicinal chemistry (23.01.2014)
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Stereoselective Synthesis of anti-N-Protected 3-Amino-1,2-epoxides by Nucleophilic Addition to N-tert-Butanesulfinyl Imine of a Glyceraldehyde Synthon
Harried, Scott S, Croghan, Michael D, Kaller, Matthew R, Lopez, Patricia, Zhong, Wenge, Hungate, Randall, Reider, Paul J
Published in Journal of organic chemistry (21.08.2009)
Published in Journal of organic chemistry (21.08.2009)
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Quinolinone-based agonists of S1P1: Use of a N-scan SAR strategy to optimize in vitro and in vivo activity
Pennington, Lewis D., Croghan, Michael D., Sham, Kelvin K.C., Pickrell, Alexander J., Harrington, Paul E., Frohn, Michael J., Lanman, Brian A., Reed, Anthony B., Lee, Matthew R., Xu, Han, McElvain, Michele, Xu, Yang, Zhang, Xuxia, Fiorino, Michael, Horner, Michelle, Morrison, Henry G., Arnett, Heather A., Fotsch, Christopher, Tasker, Andrew S., Wong, Min, Cee, Victor J.
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
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A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of β-Secretase
Kaller, Matthew R, Harried, Scott S, Albrecht, Brian, Amarante, Patricia, Babu-Khan, Safura, Bartberger, Michael D, Brown, James, Brown, Ryan, Chen, Kui, Cheng, Yuan, Citron, Martin, Croghan, Michael D, Graceffa, Russell, Hickman, Dean, Judd, Ted, Kriemen, Chuck, La, Daniel, Li, Vivian, Lopez, Patricia, Luo, Yi, Masse, Craig, Monenschein, Holger, Nguyen, Thomas, Pennington, Lewis D, Miguel, Tisha San, Sickmier, E. Allen, Wahl, Robert C, Weiss, Matthew M, Wen, Paul H, Williamson, Toni, Wood, Stephen, Xue, May, Yang, Bryant, Zhang, Jianhua, Patel, Vinod, Zhong, Wenge, Hitchcock, Stephen
Published in ACS medicinal chemistry letters (08.11.2012)
Published in ACS medicinal chemistry letters (08.11.2012)
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Optimization of a Potent, Orally Active S1P1 Agonist Containing a Quinolinone Core
Harrington, Paul E, Croghan, Michael D, Fotsch, Christopher, Frohn, Mike, Lanman, Brian A, Pennington, Lewis D, Pickrell, Alexander J, Reed, Anthony B, Sham, Kelvin K. C, Tasker, Andrew, Arnett, Heather A, Fiorino, Michael, Lee, Matthew R, McElvain, Michele, Morrison, Henry G, Xu, Han, Xu, Yang, Zhang, Xuxia, Wong, Min, Cee, Victor J
Published in ACS medicinal chemistry letters (12.01.2012)
Published in ACS medicinal chemistry letters (12.01.2012)
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Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH2
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Published in Bioorganic & medicinal chemistry letters (21.07.2003)
Published in Bioorganic & medicinal chemistry letters (21.07.2003)
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4-Methoxy-N-[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide: A Potent and Selective Agonist of S1P1
Pennington, Lewis D, Sham, Kelvin K. C, Pickrell, Alexander J, Harrington, Paul E, Frohn, Michael J, Lanman, Brian A, Reed, Anthony B, Croghan, Michael D, Lee, Matthew R, Xu, Han, McElvain, Michele, Xu, Yang, Zhang, Xuxia, Fiorino, Michael, Horner, Michelle, Morrison, Henry G, Arnett, Heather A, Fotsch, Christopher, Wong, Min, Cee, Victor J
Published in ACS medicinal chemistry letters (13.10.2011)
Published in ACS medicinal chemistry letters (13.10.2011)
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Correction to Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 1. Discovery of a Novel Tool Compound for in Vivo Proof-of-Concept
Ashton, Kate S, Andrews, Kristin L, Bryan, Marian C, Chen, Jie, Chen, Kui, Chen, Michelle, Chmait, Samer, Croghan, Michael, Cupples, Rod, Fotsch, Christopher, Helmering, Joan, Jordan, Steve R, Kurzeja, Robert J. M, Michelsen, Klaus, Pennington, Lewis D, Poon, Steve F, Sivits, Glenn, Van, Gwyneth, Vonderfecht, Steve L, Wahl, Robert C, Zhang, Jiandong, Lloyd, David J, Hale, Clarence, St. Jean, David J
Published in Journal of medicinal chemistry (27.03.2014)
Published in Journal of medicinal chemistry (27.03.2014)
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4-Methoxy- N -[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide: A Potent and Selective Agonist of S1P 1
Pennington, Lewis D., Sham, Kelvin K. C., Pickrell, Alexander J., Harrington, Paul E., Frohn, Michael J., Lanman, Brian A., Reed, Anthony B., Croghan, Michael D., Lee, Matthew R., Xu, Han, McElvain, Michele, Xu, Yang, Zhang, Xuxia, Fiorino, Michael, Horner, Michelle, Morrison, Henry G., Arnett, Heather A., Fotsch, Christopher, Wong, Min, Cee, Victor J.
Published in ACS medicinal chemistry letters (13.10.2011)
Published in ACS medicinal chemistry letters (13.10.2011)
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The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core
Harrington, Paul E., St. Jean, David J., Clarine, Jeffrey, Coulter, Thomas S., Croghan, Michael, Davenport, Adam, Davis, James, Ghiron, Chiara, Hutchinson, Jonathan, Kelly, Michael G., Lott, Fred, Lu, Jenny Ying-Lin, Martin, David, Morony, Sean, Poon, Steve F., Portero-Larragueta, Elena, Reagan, Jeff D., Regal, Kelly A., Tasker, Andrew, Wang, Minghan, Yang, Yuhua, Yao, Guomin, Zeng, Qingping, Henley, Charles, Fotsch, Christopher
Published in Bioorganic & medicinal chemistry letters (15.09.2010)
Published in Bioorganic & medicinal chemistry letters (15.09.2010)
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Optimization of a Potent, Orally Active S1P 1 Agonist Containing a Quinolinone Core
Harrington, Paul E., Croghan, Michael D., Fotsch, Christopher, Frohn, Mike, Lanman, Brian A., Pennington, Lewis D., Pickrell, Alexander J., Reed, Anthony B., Sham, Kelvin K. C., Tasker, Andrew, Arnett, Heather A., Fiorino, Michael, Lee, Matthew R., McElvain, Michele, Morrison, Henry G., Xu, Han, Xu, Yang, Zhang, Xuxia, Wong, Min, Cee, Victor J.
Published in ACS medicinal chemistry letters (12.01.2012)
Published in ACS medicinal chemistry letters (12.01.2012)
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Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2)
Fotsch, Christopher, Smith, Duncan M, Adams, Jeffrey A, Cheetham, Janet, Croghan, Michael, Doherty, Elizabeth M, Hale, Clarence, Jarosinski, Mark A, Kelly, Michael G, Norman, Mark H, Tamayo, Nuria A, Xi, Ning, Baumgartner, James W
Published in Bioorganic & medicinal chemistry letters (21.07.2003)
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Published in Bioorganic & medicinal chemistry letters (21.07.2003)
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Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro- dPhe-Arg-Trp-Lys]-NH 2
Fotsch, Christopher, Smith, Duncan M, Adams, Jeffrey A, Cheetham, Janet, Croghan, Michael, Doherty, Elizabeth M, Hale, Clarence, Jarosinski, Mark A, Kelly, Michael G, Norman, Mark H, Tamayo, Nuria A, Xi, Ning, Baumgartner, James W
Published in Bioorganic & medicinal chemistry letters (2003)
Published in Bioorganic & medicinal chemistry letters (2003)
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Substituted hydroxyethyl amine compounds as beta-secretase modulators and methods of use
CROGHAN MICHAEL, YANG BRYANT, ZHONG WENGE, VINOD PATEL F, HITCHCOCK STEPHEN
Year of Publication 21.01.2014
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Year of Publication 21.01.2014
Patent
ChemInform Abstract: Stereoselective Synthesis of anti-N-Protected 3-Amino-1,2-epoxides by Nucleophilic Addition to N-tert-Butanesulfinyl Imine of a Glyceraldehyde Synthon
Harried, Scott S., Croghan, Michael D., Kaller, Matthew R., Lopez, Patricia, Zhong, Wenge, Hungate, Randall, Reider, Paul J.
Published in ChemInform (12.01.2010)
Published in ChemInform (12.01.2010)
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BENZODIOXEPINE AND BENZODIOXINE COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES
FOTSCH CHRISTOPHER H, TEGLEY CHRISTOPHER M, REICHELT ANDREAS, BARTBERGER MICHAEL DAVID, NORMAN MARK H, ST. JEAN, JR. DAVID J, CROGHAN MICHAEL D, PENNINGTON LEWIS DALE
Year of Publication 05.06.2014
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Year of Publication 05.06.2014
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