84400-98-6Relevant articles and documents
HETEROCYCLIC SULFONAMIDE DERIVATIVE AND MEDICINE COMPRISING SAME
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Paragraph 0349, (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.
Synthesis of highly substituted cyclobutane fused-ring systems from n-vinyl β-lactams through a one-pot domino process
Cheung, Lawrence L. W.,Yudin, Andrei K.
supporting information; experimental part, p. 4100 - 4109 (2010/07/05)
In this contribution, aminocyclobutanes, as well as eight-membered enamide rings, have been made from N-vinyl β-lactams. The eightmembered products have been formed by a [3,3]-sigmatropic rearrangement, whereas the aminocyclobutanes have been derived from a domino [3,3]-rearrangement/6π- electrocyclisation process. The aminocyclobutanes have been obtained in a highly diastereoselective fashion. The cyclobutane ring system tolerates fusion even if adjacent quaternary centres are present. Systems containing up to four fused rings are readily accessible. The reaction profile has been investigated by using Gaussian 03. This study suggests that two reaction pathways for aminocyclobutane formation are possible. In one pathway the [3,3]-sigmatropic rearrangement is the rate-limiting step and in the second pathway the electrocyclisation is rate limiting. Taken together, these reactions should facilitate the construction of fused heterocycles.
