39124-19-1Relevant articles and documents
SUBSTITUTED-PYRIDINYL COMPOUNDS AND USES THEREOF
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Page/Page column 60-61, (2020/01/10)
The present application relates generally to compounds useful for the treatment and/or enhancement of cognitive dysfunction and negative symptoms associated with CNS disorders where the circuitry involving fast spiking PV+ interneurons and the production of cortical gamma oscillations is disrupted. The subject disclosure enables the manufacture of medicaments as well as compositions containing same for use in methods of therapy and prophylaxis of cognitive dysfunction and negative symptoms.
Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space
Prevet, Hugues,Flipo, Marion,Roussel, Pascal,Deprez, Benoit,Willand, Nicolas
supporting information, p. 2888 - 2894 (2016/06/14)
Fragment-based drug design has been successfully applied to a large set of proteins, however in order to expand this concept to the most demanding targets, such as protein-protein interactions, it is required to enrich current fragment libraries with new and original 3D privileged fragments. Our goal was to develop a rapid microwave-assisted synthesis of 27 new privileged spirohydantoin fragments. Among them 24 compounds showed a high water solubility. These molecules were plotted according to the normalized principal moments of inertia of their minimized conformers, and most of the compounds were prone to occupy under-populated regions of the triangular plot. Finally we demonstrated that the hydantoin ring can be selectively N-monoalkylated providing the access to rapid functionalization for further elaboration.
PEPTIDYL NITRIL COMPOUNDS AS DIPEPTIDYL PEPTIDASE I INHIBITORS
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Page/Page column 26; 28, (2015/03/28)
The invention relates to compounds of Formula (I) and their use as selective dipeptidyl peptidase I inhibitors, as well as pharmaceutical compositions comprising said compounds, and methods of treatment involving said compounds.