59227-67-7Relevant articles and documents
Pyrrole inhibitors of S-nitrosoglutathione reductase as therapeutic agents
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Page/Page column 296, (2015/11/16)
The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
Discovery of an orally available, brain penetrant BACE1 inhibitor that affords robust CNS Aβ reduction
Stamford, Andrew W.,Scott, Jack D.,Li, Sarah W.,Babu, Suresh,Tadesse, Dawit,Hunter, Rachael,Wu, Yusheng,Misiaszek, Jeffrey,Cumming, Jared N.,Gilbert, Eric J.,Huang, Chunli,McKittrick, Brian A.,Hong, Liwu,Guo, Tao,Zhu, Zhaoning,Strickland, Corey,Orth, Peter,Voigt, Johannes H.,Kennedy, Matthew E.,Chen, Xia,Kuvelkar, Reshma,Hodgson, Robert,Hyde, Lynn A.,Cox, Kathleen,Favreau, Leonard,Parker, Eric M.,Greenlee, William J.
supporting information, p. 897 - 902 (2013/01/15)
Inhibition of BACE1 to prevent brain Aβ peptide formation is a potential disease-modifying approach to the treatment of Alzheimer's disease. Despite over a decade of drug discovery efforts, the identification of brain-penetrant BACE1 inhibitors that substantially lower CNS Aβ levels following systemic administration remains challenging. In this report we describe structure-based optimization of a series of brain-penetrant BACE1 inhibitors derived from an iminopyrimidinone scaffold. Application of structure-based design in tandem with control of physicochemical properties culminated in the discovery of compound 16, which potently reduced cortex and CSF Aβ40 levels when administered orally to rats.
Antibacterial agents
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, (2008/06/13)
The present invention provides compounds of formula (I): wherein R1-R6 and J and K have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful as antibacterial agents. Also disclosed are pharmaceutical compositions comprising one or more compounds of formula I, processes for preparing compounds of formula I, and intermediates useful for preparing compounds of formula I.