Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors
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.
Zhao, Zhijian,Leister, William H.,O'Brien, Julie A.,Lemaire, Wei,Williams Jr., David L.,Jacobson, Marlene A.,Sur, Cyrille,Kinney, Gene G.,Pettibone, Doug J.,Tiller, Philip R.,Smith, Sheri,Hartman, George D.,Lindsley, Craig W.,Wolkenberg, Scott E.
scheme or table
p. 1488 - 1491
(2009/11/30)
RADIOLABELED GLYCINE TRANSPORTER INHIBITORS
The present invention is directed to radiolabeled glycine transporter inhibitors which are useful for the labeling and diagnostic imaging of glycine transporters in mammals.
The present invention is directed to pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergi
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Page/Page column 15
(2010/11/28)
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