883889-24-5Relevant academic research and scientific papers
Application of fragment-based lead generation to the discovery of novel, cyclic amidine β-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency
Edwards, Philip D.,Albert, Jeffrey S.,Sylvester, Mark,Aharony, David,Andisik, Donald,Callaghan, Owen,Campbell, James B.,Carr, Robin A.,Chessari, Gianni,Congreve, Miles,Frederickson, Martyn,Folmer, Rutger H. A.,Geschwindner, Stefan,Koether, Gerard,Kolmodin, Karin,Krumrine, Jennifer,Mauger, Russell C.,Murray, Christopher W.,Olsson, Lise-Lotte,Patel, Sahil,Spear, Nate,Tian, Gaochao
, p. 5912 - 5925 (2007)
Fragment-based lead generation has led to the discovery of a novel series of cyclic amidine-based inhibitors of β-secretase (BACE-1). Initial fragment hits with an isocytosine core having millimolar potency were identified via NMR affinity screening. Stru
SUBSTITUTED 2-AMINOPYRIMIDINE-4-ONES, THEIR PHARMACEUTICAL COMPOSITIONS AND THEIR USE IN THE TREATMENT AND/OR PREVENTION OF A?-RELATED PATHOLOGIES
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Page/Page column 43-44, (2008/06/13)
This invention relates to novel compounds having the structural formula (I) below: [Chemical formula should be inserted here. Please see paper copy] and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds prov
2-AMINOPYRIMIDIN-4-ONES AND THEIR USE FOR TREATING OR PREVENTING Aβ-RELATED PATHOLOGIES
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Page/Page column 21-22, (2008/06/13)
This invention relates to novel compounds having the structural formula (I) below: [Chemical formula should be inserted here. Please see paper copy] and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds prov
SUBSTITUTED AMINO-COMPOUNDS AND USES THEREOF
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Page/Page column 47, (2008/06/13)
This invention relates to novel compounds having the structural formula Ia or formula Ib: Ia Ib and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provi
SUBSTITUTED AMINO-PYRIMIDONES AND USES THEREOF
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Page/Page column 56; 61, (2008/06/13)
This invention relates to novel compounds having the structural formula Ia or formula Ib below: (Ia,Ib), and their phatmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Abeta related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
