84400-99-7Relevant articles and documents
HETEROCYCLIC SULFONAMIDE DERIVATIVE AND MEDICINE COMPRISING SAME
-
Paragraph 0350; 0351, (2016/12/01)
The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. The compound has a superior TRPA1 antagonist activity, and can provide a medicament useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.
Discovery and optimization of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1
Hornberger, Keith R.,Berger, Dan M.,Crew, Andrew P.,Dong, Hanqing,Kleinberg, Andrew,Li, An-Hu,Medeiros, Matthew R.,Mulvihill, Mark J.,Siu, Kam,Tarrant, James,Wang, Jing,Weng, Felix,Wilde, Victoria L.,Albertella, Mark,Bittner, Mark,Cooke, Andrew,Gray, Michael J.,Maresca, Paul,May, Earl,Meyn, Peter,Peick Jr., William,Romashko, Darlene,Tanowitz, Michael,Tokar, Brianna
, p. 4517 - 4522 (2013/08/23)
The discovery and potency optimization of a series of 7-aminofuro[2,3-c] pyridine inhibitors of TAK1 is described. Micromolar hits taken from high-throughput screening were optimized for biochemical and cellular mechanistic potency to ~10 nM, as exemplified by compound 12az. Application of structure-based drug design aided by co-crystal structures of TAK1 with inhibitors significantly shortened the number of iterations required for the optimization.
7-AMINOFUROPYRIDINE DERIVATIVES
-
Page/Page column 23, (2011/09/15)
Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.