944950-51-0Relevant academic research and scientific papers
SAR of tricyclic sulfones as γ-secretase inhibitors
Xu, Ruo,Cole, David,Asberom, Ted,Bara, Tom,Bennett, Chad,Burnett, Duane A.,Clader, John,Domalski, Martin,Greenlee, William J.,Hyde, Lynn,Josien, Hubert,Li, Hongmei,McBriar, Mark,McKittrick, Brian,Pissarnitski, Dmitri,Qiang, Li,Rajagopalan, Murali,Sasikumar, Thavalakulamgara,Su, Jing,Tang, Haiqun,Wu, Wen-Lian,Zhang, Lili,Zhao, Zhiqiang
, p. 1688 - 1701 (2012/05/19)
Novel tricyclic sulfones as γ-secretase inhibitors have been reported by this laboratory for the treatment of Alzheimers disease. Compounds in this series have comparable or better in vitro activities and in vivo efficacies than sulfonamide analogues reported previously by this laboratory. Based on the previously reported tricyclic sulfone scaffold, additional SAR studies of C ring were carried out. Various C-ring structures including cyclohexane, pyran, and piperidine were tolerated. Additionally, the 7- and 8- positions of the C-ring were identified as the best sites to introduce substituent for modulating the pharmacokinetic properties of compounds from this series.
BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS
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Page/Page column 107; 108, (2010/11/28)
This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl
