82938-49-6Relevant articles and documents
OBTENTION D'UN α-AMINO ALDEHYDE PTIQUEMENT ACTIF EN SERIE β-LACTAME
Labia, Roger,Morin, Christophe
, p. 1007 - 1008 (1984)
Oxidation of a suitable protected L-aspartic acid derived azetdione gives rise to a chiral β-lactam carboxaldehyde without significant racemization.
The discovery and optimization of benzimidazoles as selective NaV1.8 blockers for the treatment of pain
Brown, Alan D.,Bagal, Sharan K.,Blackwell, Paul,Blakemore, David C.,Brown, Bruce,Bungay, Peter J.,Corless, Martin,Crawforth, James,Fengas, David,Fenwick, David R.,Gray, Victoria,Kemp, Mark,Klute, Wolfgang,Malet Sanz, Laia,Miller, Duncan,Murata, Yoshihisa,Payne, C. Elizabeth,Skerratt, Sarah,Stevens, Edward B.,Warmus, Joseph S.
, p. 230 - 239 (2018/12/11)
The voltage gated sodium channel NaV1.8 has been postulated to play a key role in the transmission of pain signals. Core hopping from our previously reported phenylimidazole leads has allowed the identification of a novel series of benzimidazole NaV1.8 blockers. Subsequent optimization allowed the identification of compound 9, PF-06305591, as a potent, highly selective blocker with an excellent preclinical in vitro ADME and safety profile.
Cyclic dipeptides and azetidinone compounds and their use in treating CNS injury and neurodegenerative disorders
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Page/Page column 46, (2010/11/26)
The present invention provides 4-substituted-2-azetidinone compounds, bicyclic 2-5-diketopiperazine compounds, and pharmaceutical compositions thereof that are potent, safe and effective neuroprotective agents. Due to their strong central nervous system (CNS) activity, the compounds can be used to enhance memory and to treat a variety of neurological disorders. The compounds are particularly useful for treating neurological disorders caused by, or associated with, CNS trauma.