- Identification of an orally bioavailable, potent, and selective inhibitor of GlyT1
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Amalgamation of the structure-activity relationship of two series of GlyT1 inhibitors developed at Merck led to the discovery of a clinical candidate, compound 16 (DCCCyB), which demonstrated excellent in vivo occupancy of GlyT1 transporters in rhesus mon
- Blackaby, Wesley P.,Lewis, Richard T.,Thomson, Joanne L.,Jennings, Andrew S. R.,Goodacre, Simon C.,Street, Leslie J.,MacLeod, Angus M.,Pike, Andrew,Wood, Suzanne,Thomas, Steve,Brown, Terry A.,Smith, Alison,Pillai, Gopalan,Almond, Sarah,Guscott, Martin R.,Burns, H. Donald,Eng, Waisi,Ryan, Christine,Cook, Jacquelynn,Hamill, Terence G.
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scheme or table
p. 350 - 354
(2010/11/18)
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- Cyclohexanesulfonyl derivatives as GlyT1 inhibitors to treat schizophrenia
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The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3
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Page/Page column 17
(2008/06/13)
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