17289-25-7Relevant academic research and scientific papers
BIARYL PYRAZOLES AS NRF2 REGULATORS
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Page/Page column 474; 475, (2017/08/01)
The present invention relates to biaryl pyrazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
New asymmetric synthesis of protein farnesyltransferase inhibitors via palladium-catalyzed cross-coupling reactions of 2-iodo-imidazoles
Kerherve, Jennifer,Botuha, Candice,Dubois, Joelle
experimental part, p. 2214 - 2222 (2009/09/04)
Palladium catalyzed cross-coupling reactions of 2-iodoimidazole have been studied to synthesize imidazole-containing protein farnesyltransferase inhibitors. The Suzuki coupling reaction proved to be very efficient to introduce functionalized alkyl chains at the 2-position of the imidazole ring and a new synthesis of the required alkenylboronates was realised by a reaction of cross metathesis. Asymmetric synthesis of allyl succinic derivatives allowed us to synthesize chiral protein farnesyltransferase inhibitors through Suzuki coupling and to determine the influence of the stereochemistry of our inhibitors on the enzymatic activity.
2-PHENYLPYRIDIN-4-YL DERIVATIVES AS ALK5 INHIBITORS
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Page 47, (2010/02/06)
This invention relates to novel 2-phenylpyridin-4-yl heterocyclyl derivatives which are inhibitors of the transforming growth factor, ("TGF")-? signalling pathway, in particular, the phosphorylation of smad2 or smad3 by the TGF-β type I or activin-like kinase ("ALK")-5 receptor, methods for their preparation and their use in medicine, specifically in the treatment and prevention of a disease state mediated by this pathway.
PYRAZOLE INHIBITORS OF THE TRANSFORMING GROWTH FACTOR
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Page 30, (2010/02/06)
The invention relates to novel pyrazole derivatives of formula (I), which are inhibitors of the transforming growth factor, ("TGF")-? signalling pathway, in particular, the phosphorylation of smad2 or smad3 by the TGF-β type I or activin-like kinase ("ALK")-5 receptor, methods for their preparation and their use in medicine, specifically in the treatment and prevention of a disease state mediated by this pathway.
Substituted triazolo-pyridazine derivatives as ligands for GABA receptors
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, (2008/06/13)
Substituted triazolo-pyridazine derivative compounds represented by wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the α2 and/or α3 subunits.
