1243204-92-3Relevant articles and documents
Anilinotriazoles as potent gamma secretase modulators
Velter, Adriana I.,Bischoff, Franois P.,Berthelot, Didier,De Cleyn, Michel,Oehlrich, Daniel,Jaroskova, Libuse,Macdonald, Gregor,Minne, Garrett,Pieters, Serge,Rombouts, Frederik,Van Brandt, Sven,Van Roosbroeck, Yves,Surkyn, Michel,Trabanco, Andrs A.,Tresadern, Gary,Wu, Tongfei,Borghys, Herman,Mercken, Marc,Masungi, Chantal,Gijsen, Harrie
, p. 5805 - 5813 (2015/01/08)
The design and synthesis of a novel series of potent gamma secretase modulators is described. Exploration of various spacer groups between the triazole ring and the aromatic appendix in 2 has led to anilinotriazole 28, which combined high in vitro and in
Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators
Pettersson, Martin,Johnson, Douglas S.,Subramanyam, Chakrapani,Bales, Kelly R.,Am Ende, Christopher W.,Fish, Benjamin A.,Green, Michael E.,Kauffman, Gregory W.,Lira, Ricardo,Mullins, Patrick B.,Navaratnam, Thayalan,Sakya, Subas M.,Stiff, Cory M.,Tran, Tuan P.,Vetelino, Beth C.,Xie, Longfei,Zhang, Liming,Pustilnik, Leslie R.,Wood, Kathleen M.,O'Donnell, Christopher J.
scheme or table, p. 2906 - 2911 (2012/06/04)
We report the discovery and optimization of a novel series of dihydrobenzofuran amides as γ-secretase modulators (GSMs). Strategies for aligning in vitro potency with drug-like physicochemical properties and good microsomal stability while avoiding P-gp mediated efflux are discussed. Lead compounds such as 35 and 43 have moderate to good in vitro potency and excellent selectivity against Notch. Good oral bioavailability was achieved as well as robust brain Aβ42 lowering activity at 100 mg/kg po dose.
SUBSTITUTED TRIAZOLE AND IMIDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
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Page/Page column 116, (2011/02/24)
The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.