944950-53-2Relevant academic research and scientific papers
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.
Design and synthesis of tricyclic sulfones as γ-secretase inhibitors with greatly reduced Notch toxicity
Xu, Ruo,Cole, David,Asberom, Ted,Bara, Tom,Bennett, Chad,Burnett, Duane A.,Clader, John,Domalski, Martin,Greenlee, William,Hyde, Lynn,Josien, Hubert,Li, Hongmei,McBriar, Mark,McKittrick, Brian,McPhail, Andrew T.,Pissarnitski, Dmitri,Qiang, Li,Rajagopalan, Murali,Sasikumar, Thavalakulamgar,Su, Jing,Tang, Haiqun,Wu, Wen-Lian,Zhang, Lili,Zhao, Zhiqiang
body text, p. 2591 - 2596 (2010/07/05)
A novel series of tricyclic γ-secretase inhibitors was designed and synthesized via a conformational analysis of literature compounds. The preliminary results have shown that compounds in this new series have much improved in vitro potency and in vivo pro
TETRAHYDROPYRANOCHROMENE GAMMA SECRETASE INHIBITORS
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Page/Page column 194; 196, (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.
BENZENESULFONYL-CHROMANE, THIOCHROMANE, TETRAHYDRONAPHTHALENE AND RELATED GAMMA SECRETASE INHIBITORS
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Page/Page column 111, (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
