845546-60-3Relevant academic research and scientific papers
Piperazine sulfonamide BACE1 inhibitors: Design, synthesis, and in vivo characterization
Cumming, Jared,Babu, Suresh,Huang, Ying,Carrol, Carolyn,Chen, Xia,Favreau, Leonard,Greenlee, William,Guo, Tao,Kennedy, Matthew,Kuvelkar, Reshma,Le, Thuy,Li, Guoqing,McHugh, Nansie,Orth, Peter,Ozgur, Lynne,Parker, Eric,Saionz, Kurt,Stamford, Andrew,Strickland, Corey,Tadesse, Dawit,Voigt, Johannes,Zhang, Lili,Zhang, Qi
scheme or table, p. 2837 - 2842 (2010/08/04)
With collaboration between chemistry, X-ray crystallography, and molecular modeling, we designed and synthesized a series of novel piperazine sulfonamide BACE1 inhibitors. Iterative exploration of the non-prime side and S2′ sub-pocket of the enzyme culmin
CYCLIC AMINE BASE-1 INHIBITORS HAVING A HETEROCYCLIC SUBSTITUENT
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Page/Page column 87, (2008/06/13)
Disclosed are novel compounds of the formula (I)or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is formula (I) X is -0-, -C(R14)2- or -N(R)-; Z is -C(R14)2- or -N(R)-; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, -CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, -OR35, -N(R24)(R25)or -SR35; R41 is alkyl, cycloalkyl, -S02(alkyl), -C(O)-alkyl, -C(O)-cycloalkyl or -alkyl-NH-C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula (I). Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.
