Amino-5,5-diphenylimidazolone derivatives for the inhibition of beta-secretase
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated β-amyloid deposits or β-amyloid levels in a patient.
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Page/Page column 8
(2008/06/13)
Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase
A non-methionine FT inhibitor lead structure (1) was designed through computer modeling of the peptidomimetic FT inhibitor ABT839. Optimization of this lead resulted in compounds 2e and 2g, with FT IC50 values of 1.3 and 1.8 nM, GGT IC50 of 1400 nM, and EC50 (Ras processing) values of 13 and 11 nM, respectively.
Wang, Gary T.,Wang, Xilu,Wang, Weibo,Hasvold, Lisa A.,Sullivan, Gerry,Hutchins, Charles W.,O'Conner, Steve,Gentiles, Robert,Sowin, Thomas,Cohen, Jerry,Gu, Wen-Zhen,Zhang, Haiying,Rosenberg, Saul H.,Sham, Hing L.
p. 153 - 158
(2007/10/03)
Substituted phenyl farnesyltransferase inhibitors
Compounds of formula (I) or pharmaceutically acceptable salts thereof, inhibit farnesyltransferase. Methods for making the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.
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(2012/09/25)
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