944951-67-1Relevant academic research and scientific papers
Tricyclic sulfones as orally active γ-secretase inhibitors: Synthesis and structure-activity relationship studies
Sasikumar,Qiang, Li,Burnett, Duane A.,Cole, David,Xu, Ruo,Li, Hongmei,Greenlee, William J.,Clader, John,Zhang, Lili,Hyde, Lynn
scheme or table, p. 3632 - 3635 (2010/09/06)
Tricyclic sulfones were designed as γ-secretase inhibitors and found to have excellent potency. Extensive SAR shows that a large number of sulfonamides at position 7 of the tricycle are very well tolerated. Compounds such as 15a and 15c showed remarkable in vivo potency.
TETRAHYDROPYRANOCHROMENE GAMMA SECRETASE INHIBITORS
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Page/Page column 231; 233, (2009/03/07)
Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)-O-C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)-O-C(O)-heteroaryl and a basic tertiary amine.
