887338-57-0Relevant academic research and scientific papers
Design, Synthesis, and Biological Evaluation of Novel Indoles Targeting the Influenza PB2 Cap Binding Region
Mcgowan, David C.,Balemans, Wendy,Embrechts, Werner,Motte, Magali,Keown, Jeremy R.,Buyck, Christophe,Corbera, Jordi,Funes, Mario,Moreno, Laura,Cooymans, Ludwig,Tahri, Abdellah,Eymard, Julien,Stoops, Bart,Strijbos, Rudy,Van Den Berg, Joke,Fodor, Ervin,Grimes, Jonathan M.,Koul, Anil,Jonckers, Tim H. M.,Raboisson, Pierre,Guillemont, Jér?me
, p. 9680 - 9690 (2019)
In the search for novel influenza inhibitors we evaluated 7-fluoro-substituted indoles as bioisosteric replacements for the 7-azaindole scaffold of Pimodivir, a PB2 (polymerase basic protein 2) inhibitor currently in clinical development. Specifically, a 5,7-difluoroindole derivative 11a was identified as a potent and metabolically stable influenza inhibitor. 11a demonstrated a favorable oral pharmacokinetic profile and in vivo efficacy in mice. In addition, it was found that 11a was not at risk of metabolism via aldehyde oxidase, an advantage over previously described inhibitors of this class. The crystal structure of 11a bound to influenza A PB2 cap region is disclosed here and deposited to the PDB.
INDOLES FOR USE IN INFLUENZA VIRUS INFECTION
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Page/Page column 34-36, (2016/04/19)
The invention relates to compounds having the structure of formula (I) which can be used for the treatment of or against influenza infections.
1-SUBSTITUTED-3- BETA-D-GLUCOPYRANOSYLATED NITROGENOUS HETERO- CYCLIC COMPOUNDS AND MEDICINES CONTAINING THE SAME
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Page/Page column 16, (2008/06/13)
A compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity, etc. It is a 1-substituted-3-(β-D
