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Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors. 2009
Zhijian Zhao, and
William H Leister, and
Julie A O'Brien, and
Wei Lemaire, and
David L Williams, and
Marlene A Jacobson, and
Cyrille Sur, and
Gene G Kinney, and
Doug J Pettibone, and
Philip R Tiller, and
Sheri Smith, and
George D Hartman, and
Craig W Lindsley, and
Scott E Wolkenberg
Department of Medicinal Chemistry, Technology Enabled Synthesis Group, Merck & Co., Inc., WP-14-1, PO Box 4 Sumneytown Pike, West Point, PA 19486, USA.
Employing an iterative analogue library approach, novel potent and selective glycine transporter 1 (GlyT1) inhibitors containing a 4-pyridin-2-ylpiperidine sulfonamide have been discovered. These inhibitors are devoid of time-dependent CYP inhibition activity and exhibit improved aqueous solubility versus the corresponding 4-phenylpiperidine analogues.
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Zhijian Zhao, and
William H Leister, and
Julie A O'Brien, and
Wei Lemaire, and
David L Williams, and
Marlene A Jacobson, and
Cyrille Sur, and
Gene G Kinney, and
Doug J Pettibone, and
Philip R Tiller, and
Sheri Smith, and
George D Hartman, and
Craig W Lindsley, and
Scott E Wolkenberg
December 2006,
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Zhijian Zhao, and
William H Leister, and
Julie A O'Brien, and
Wei Lemaire, and
David L Williams, and
Marlene A Jacobson, and
Cyrille Sur, and
Gene G Kinney, and
Doug J Pettibone, and
Philip R Tiller, and
Sheri Smith, and
George D Hartman, and
Craig W Lindsley, and
Scott E Wolkenberg
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Julie A O'Brien, and
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Gene G Kinney, and
Doug J Pettibone, and
Philip R Tiller, and
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George D Hartman, and
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Zhijian Zhao, and
William H Leister, and
Julie A O'Brien, and
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Cyrille Sur, and
Gene G Kinney, and
Doug J Pettibone, and
Philip R Tiller, and
Sheri Smith, and
George D Hartman, and
Craig W Lindsley, and
Scott E Wolkenberg
January 2011,
Bioorganic & medicinal chemistry letters,
Zhijian Zhao, and
William H Leister, and
Julie A O'Brien, and
Wei Lemaire, and
David L Williams, and
Marlene A Jacobson, and
Cyrille Sur, and
Gene G Kinney, and
Doug J Pettibone, and
Philip R Tiller, and
Sheri Smith, and
George D Hartman, and
Craig W Lindsley, and
Scott E Wolkenberg
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Bioorganic & medicinal chemistry letters,
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William H Leister, and
Julie A O'Brien, and
Wei Lemaire, and
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Marlene A Jacobson, and
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Gene G Kinney, and
Doug J Pettibone, and
Philip R Tiller, and
Sheri Smith, and
George D Hartman, and
Craig W Lindsley, and
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April 2018,
Bioorganic & medicinal chemistry letters,
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William H Leister, and
Julie A O'Brien, and
Wei Lemaire, and
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Marlene A Jacobson, and
Cyrille Sur, and
Gene G Kinney, and
Doug J Pettibone, and
Philip R Tiller, and
Sheri Smith, and
George D Hartman, and
Craig W Lindsley, and
Scott E Wolkenberg
September 2008,
Bioorganic & medicinal chemistry letters,
Zhijian Zhao, and
William H Leister, and
Julie A O'Brien, and
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David L Williams, and
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Cyrille Sur, and
Gene G Kinney, and
Doug J Pettibone, and
Philip R Tiller, and
Sheri Smith, and
George D Hartman, and
Craig W Lindsley, and
Scott E Wolkenberg
January 2016,
Chemical & pharmaceutical bulletin,
Zhijian Zhao, and
William H Leister, and
Julie A O'Brien, and
Wei Lemaire, and
David L Williams, and
Marlene A Jacobson, and
Cyrille Sur, and
Gene G Kinney, and
Doug J Pettibone, and
Philip R Tiller, and
Sheri Smith, and
George D Hartman, and
Craig W Lindsley, and
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September 2017,
Future medicinal chemistry,
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William H Leister, and
Julie A O'Brien, and
Wei Lemaire, and
David L Williams, and
Marlene A Jacobson, and
Cyrille Sur, and
Gene G Kinney, and
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Philip R Tiller, and
Sheri Smith, and
George D Hartman, and
Craig W Lindsley, and
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