2-Amino-3,4-dihydroquinazolines as inhibitors of BACE-1 (β-site APP cleaving enzyme): Use of structure based design to convert a micromolar hit into a nanomolar lead
A new aspartic protease inhibitory chemotype bearing a 2-amino-3,4- dihydroquinazoline ring was identified by high-throughput screening for the inhibition of BACE-1. X-ray crystallography revealed that the exocyclic amino group participated in a hydrogen
Baxter, Ellen W.,Conway, Kelly A.,Kennis, Ludo,Bischoff, Fran?ois,Mercken, Marc H.,De Winter, Hans L.,Reynolds, Charles H.,Tounge, Brett A.,Luo, Chi,Scott, Malcolm K.,Huang, Yifang,Braeken, Mirielle,Pieters, Serge M. A.,Berthelot, Didier J. C.,Masure, Stefan,Bruinzeel, Wouter D.,Jordan, Alfonzo D.,Parker, Michael H.,Boyd, Robert E.,Qu, Junya,Alexander, Richard S.,Brenneman, Douglas E.,Reitz, Allen B.
p. 4261 - 4264
(2008/03/11)
NOVEL 2-AMINO-QUINAZOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
The present invention is directed to novel 2-amino-3, 4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of P-secretase, also known as n-site cleaving enzyme and BACE.
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Page/Page column 163
(2010/10/20)
NOVEL 2-AMINO-QUINAZOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer’s disease (AD) and related disorders. The compounds of the invention are inhibitors of β-secretase, also known as β-site cleaving enzyme and BACE.
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Page/Page column 163
(2010/10/20)
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