130658-14-9Relevant academic research and scientific papers
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: Development of a [3.3.0]-based series and other piperidine bioisosteres
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.
, p. 1062 - 1066 (2014/03/21)
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.
3.3.0 BICYCLIC GLYT1 INHIBITORS AND METHODS OF MAKING AND USING SAME
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Page/Page column 62, (2010/07/02)
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.
TRICYCLIC HETEROARYL PIPERAZINES, PYRROLIDINES AND AZETIDINES AS SEROTONIN RECEPTOR MODULATORS
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Page/Page column 25, (2008/06/13)
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
Azabicyclic compounds are central nervous system active agents
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Page 81; 52, (2010/02/05)
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.
