1100362-33-1Relevant articles and documents
Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors
Wu, Wen-Lian,Asberom, Theodros,Bara, Thomas,Bennett, Chad,Burnett, Duane A.,Clader, John,Domalski, Martin,Greenlee, William J.,Josien, Hubert,McBriar, Mark,Rajagopalan, Murali,Vicarel, Monica,Xu, Ruo,Hyde, Lynn A.,Del Vecchio, Robert A.,Cohen-Williams, Mary E.,Song, Lixin,Lee, Julie,Terracina, Giuseppe,Zhang, Qi,Nomeir, Amin,Parker, Eric M.,Zhang, Lili
, p. 844 - 849 (2013/02/25)
An investigation is detailed of the structure activity relationships (SAR) of two sulfone side chains of compound (-)-1a (SCH 900229), a potent, PS1-selective γ-secretase inhibitor and clinical candidate for the treatment of Alzheimer's disease. Specifically, 4-CF3 and 4-Br substituted arylsulfone analogs, (-)-1b and (-)-1c, are equipotent to compound (-)-1a. On the right hand side chain, linker size and terminal substituents of the pendant sulfone group are also investigated.
TETRAHYDROPYRANOCHROMENE GAMMA SECRETASE INHIBITORS
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Page/Page column 249; 251, (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.
