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Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11 beta-HSD1 inhibitors. 2009
Dustin L McMinn, and
Yosup Rew, and
Athena Sudom, and
Seb Caille, and
Michael Degraffenreid, and
Xiao He, and
Randall Hungate, and
Ben Jiang, and
Juan Jaen, and
Lisa D Julian, and
Jacob Kaizerman, and
Perry Novak, and
Daqing Sun, and
Hua Tu, and
Stefania Ursu, and
Nigel P C Walker, and
Xuelei Yan, and
Qiuping Ye, and
Zhulun Wang, and
Jay P Powers
Amgen, Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.
Novel 4,4-disubstituted cyclohexylbenzamide inhibitors of 11beta-HSD1 were optimized to account for liabilities relating to in vitro pharmacokinetics, cytotoxicity and protein-related shifts in potency. A representative compound showing favorable in vivo pharmacokinetics was found to be an efficacious inhibitor of 11beta-HSD1 in a rat pharmacodynamic model (ED(50)=10mg/kg).
Related Publications
Dustin L McMinn, and
Yosup Rew, and
Athena Sudom, and
Seb Caille, and
Michael Degraffenreid, and
Xiao He, and
Randall Hungate, and
Ben Jiang, and
Juan Jaen, and
Lisa D Julian, and
Jacob Kaizerman, and
Perry Novak, and
Daqing Sun, and
Hua Tu, and
Stefania Ursu, and
Nigel P C Walker, and
Xuelei Yan, and
Qiuping Ye, and
Zhulun Wang, and
Jay P Powers
March 2012,
Journal of medicinal chemistry,
Dustin L McMinn, and
Yosup Rew, and
Athena Sudom, and
Seb Caille, and
Michael Degraffenreid, and
Xiao He, and
Randall Hungate, and
Ben Jiang, and
Juan Jaen, and
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Jacob Kaizerman, and
Perry Novak, and
Daqing Sun, and
Hua Tu, and
Stefania Ursu, and
Nigel P C Walker, and
Xuelei Yan, and
Qiuping Ye, and
Zhulun Wang, and
Jay P Powers
March 2009,
Bioorganic & medicinal chemistry letters,
Dustin L McMinn, and
Yosup Rew, and
Athena Sudom, and
Seb Caille, and
Michael Degraffenreid, and
Xiao He, and
Randall Hungate, and
Ben Jiang, and
Juan Jaen, and
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Jacob Kaizerman, and
Perry Novak, and
Daqing Sun, and
Hua Tu, and
Stefania Ursu, and
Nigel P C Walker, and
Xuelei Yan, and
Qiuping Ye, and
Zhulun Wang, and
Jay P Powers
January 2007,
Bioorganic & medicinal chemistry letters,
Dustin L McMinn, and
Yosup Rew, and
Athena Sudom, and
Seb Caille, and
Michael Degraffenreid, and
Xiao He, and
Randall Hungate, and
Ben Jiang, and
Juan Jaen, and
Lisa D Julian, and
Jacob Kaizerman, and
Perry Novak, and
Daqing Sun, and
Hua Tu, and
Stefania Ursu, and
Nigel P C Walker, and
Xuelei Yan, and
Qiuping Ye, and
Zhulun Wang, and
Jay P Powers
January 2010,
Bioorganic & medicinal chemistry,
Dustin L McMinn, and
Yosup Rew, and
Athena Sudom, and
Seb Caille, and
Michael Degraffenreid, and
Xiao He, and
Randall Hungate, and
Ben Jiang, and
Juan Jaen, and
Lisa D Julian, and
Jacob Kaizerman, and
Perry Novak, and
Daqing Sun, and
Hua Tu, and
Stefania Ursu, and
Nigel P C Walker, and
Xuelei Yan, and
Qiuping Ye, and
Zhulun Wang, and
Jay P Powers
April 2022,
Bioorganic & medicinal chemistry,
Dustin L McMinn, and
Yosup Rew, and
Athena Sudom, and
Seb Caille, and
Michael Degraffenreid, and
Xiao He, and
Randall Hungate, and
Ben Jiang, and
Juan Jaen, and
Lisa D Julian, and
Jacob Kaizerman, and
Perry Novak, and
Daqing Sun, and
Hua Tu, and
Stefania Ursu, and
Nigel P C Walker, and
Xuelei Yan, and
Qiuping Ye, and
Zhulun Wang, and
Jay P Powers
March 2010,
Bioorganic & medicinal chemistry letters,
Dustin L McMinn, and
Yosup Rew, and
Athena Sudom, and
Seb Caille, and
Michael Degraffenreid, and
Xiao He, and
Randall Hungate, and
Ben Jiang, and
Juan Jaen, and
Lisa D Julian, and
Jacob Kaizerman, and
Perry Novak, and
Daqing Sun, and
Hua Tu, and
Stefania Ursu, and
Nigel P C Walker, and
Xuelei Yan, and
Qiuping Ye, and
Zhulun Wang, and
Jay P Powers
April 2015,
Bioorganic & medicinal chemistry letters,
Dustin L McMinn, and
Yosup Rew, and
Athena Sudom, and
Seb Caille, and
Michael Degraffenreid, and
Xiao He, and
Randall Hungate, and
Ben Jiang, and
Juan Jaen, and
Lisa D Julian, and
Jacob Kaizerman, and
Perry Novak, and
Daqing Sun, and
Hua Tu, and
Stefania Ursu, and
Nigel P C Walker, and
Xuelei Yan, and
Qiuping Ye, and
Zhulun Wang, and
Jay P Powers
July 2010,
ChemMedChem,
Dustin L McMinn, and
Yosup Rew, and
Athena Sudom, and
Seb Caille, and
Michael Degraffenreid, and
Xiao He, and
Randall Hungate, and
Ben Jiang, and
Juan Jaen, and
Lisa D Julian, and
Jacob Kaizerman, and
Perry Novak, and
Daqing Sun, and
Hua Tu, and
Stefania Ursu, and
Nigel P C Walker, and
Xuelei Yan, and
Qiuping Ye, and
Zhulun Wang, and
Jay P Powers
September 2007,
Bioorganic & medicinal chemistry letters,
Dustin L McMinn, and
Yosup Rew, and
Athena Sudom, and
Seb Caille, and
Michael Degraffenreid, and
Xiao He, and
Randall Hungate, and
Ben Jiang, and
Juan Jaen, and
Lisa D Julian, and
Jacob Kaizerman, and
Perry Novak, and
Daqing Sun, and
Hua Tu, and
Stefania Ursu, and
Nigel P C Walker, and
Xuelei Yan, and
Qiuping Ye, and
Zhulun Wang, and
Jay P Powers
October 2017,
Bioorganic chemistry,
