The present invention is directed to morpholinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
Craig W. Lindsley - Schwenksville PA, US David D. Wisnoski - Quakertown PA, US Scott E. Wolkenberg - Jenkintown PA, US
Assignee:
Merck Sharp & Dohme Corp. - Rahway NJ
International Classification:
A61K 31/445 C07D 211/96
US Classification:
514331, 514233, 546184
Abstract:
The present invention is directed to cyclopropyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neuro-transmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
Wesley Blackaby - Harlow, GB Mark E. Duggan - Wellesley MA, US David Hallett - Harlow, GB George D. Hartman - Landsdale PA, US Andrew S. Jennings - Harlow, GB William H. Leister - Quakertown PA, US Richard T. Lewis - Harlow, GB Craig W. Lindsley - Schwenksville PA, US Elizabeth Naylor - Harlow, GB Leslie J. Street - Harlow, GB Yi Wang - North Wales PA, US David D. Wisnoski - Quakertown PA, US Scott E. Wolkenberg - Jenkintown PA, US Zhijian Zhao - Wilimington DE, US
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 glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
David Hallett - Buckinghamshire, GB Craig W. Lindsley - Brentwood TN, US Elizabeth M. Naylor - Needham MA, US Zhijian Zhao - Wilmington DE, US Cory R. Theberge - Elkins Park PA, US Scott E. Wolkenberg - Jenkintown PA, US M. Brad Nolt - Gilbertsville PA, US
Assignee:
Merck, Sharp & Dohme Corp. - Rahway NJ
International Classification:
A61K 31/445 C07D 211/32
US Classification:
514331, 546233, 546234
Abstract:
The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
B. Wesley Trotter - Glenside PA, US Kausik K. Nanda - Norristown PA, US Scott Wolkenberg - Jenkintown PA, US M. Brad Nolt - Blue Bell PA, US Peter Manley - Harleysville PA, US Nathan R. Kett - Perkiomenville PA, US Mark T. Bilodeau - Lansdale PA, US
B. Wesley Trotter - Glenside PA, US Kausik K. Nanda - Norristown PA, US Scott E. Wolkenberg - Jenkintown PA, US M. Brad Nolt - Bluebell PA, US David Wisnoski - Quakertown PA, US
James C. Barrow - Arnold MD, US Scott Harrison - Etkins Park PA, US James Mulhearn - Saint Davids PA, US Cyrille Sur - Harleysville PA, US David L. Williams - Telford PA, US Scott Wolkenberg - Jenkintown PA, US Eric Hostetler - Collegeville PA, US
The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH.
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