- Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: Development of a [3.3.0]-based series and other piperidine bioisosteres
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This Letter describes the development and SAR of a novel series of GlyT1 inhibitors derived from a scaffold hopping approach, in lieu of an HTS campaign, which provided intellectual property position. Members within this new [3.3.0]-based series displayed excellent GlyT1 potency, selectivity, free fraction, and modest CNS penetration. Moreover, enantioselective GlyT1 inhibition was observed, within this novel series and a number of other piperidine bioisosteric cores.
- Sheffler, Douglas J.,Nedelovych, Michael T.,Williams, Richard,Turner, Stephen C.,Duerk, Brittany B.,Robbins, Megan R.,Jadhav, Sataya B.,Niswender, Colleen M.,Jones, Carrie K.,Conn, P. Jeffrey,Daniels, R. Nathan,Lindsley, Craig W.
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p. 1062 - 1066
(2014/03/21)
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- 3.3.0 BICYCLIC GLYT1 INHIBITORS AND METHODS OF MAKING AND USING SAME
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In one aspect, the invention relates to compounds which are useful as inhibitors of glycine type 1 transporter (GIyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GIyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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Page/Page column 62
(2010/07/02)
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- TRICYCLIC HETEROARYL PIPERAZINES, PYRROLIDINES AND AZETIDINES AS SEROTONIN RECEPTOR MODULATORS
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The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are hexahydro
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Page/Page column 25
(2008/06/13)
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- Azabicyclic compounds are central nervous system active agents
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Compounds of formula (I) are novel CNS active agents that are useful for treating pain and for treating other disorders associated with the cholinergic system.
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