1246639-94-0Relevant academic research and scientific papers
Development of autotaxin inhibitors: A series of zinc binding triazoles
Thomson, Christopher G.,Le Grand, Darren,Dowling, Mark,Brocklehurst, Cara E.,Chinn, Colin,Elphick, Lucy,Faller, Michael,Freeman, Mark,Furminger, Vikki,Gasser, Cornelia,Hamadi, Ahmed,Hardaker, Elizabeth,Head, Victoria,Hill, Johan C.,Janus, Diana I.,Pearce, David,Poulaud, Anne-Sophie,Stanley, Emily,Sviridenko, Lilya
supporting information, p. 2279 - 2284 (2018/05/24)
A series of inhibitors of Autotaxin (ATX) has been developed using the binding mode of known inhibitor, PF-8380, as a template. Replacement of the benzoxazolone with a triazole zinc-binding motif reduced crystallinity and improved solubility relative to PF-8380. Modification of the linker region removed hERG activity and led to compound 12 – a selective, high affinity, orally-bioavailable inhibitor of ATX. Compound 12 concentration-dependently inhibits autotaxin and formation of LPA in vivo, as shown in pharmacokinetic-pharmacodynamic experiments.
Autotaxin inhibitors
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Page/Page column, (2014/06/25)
The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.
HETEROCYCLIC COMPOUNDS AS AUTOTAXIN INHIBITORS
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Page/Page column 20, (2012/02/01)
Compounds of the formula (I), in which Het, R, X, Y, R1 and p have the meanings indicated in claim 1, are autotaxin inhibitors and can be employed for the treatment of tumours.
