-
1
-
-
34247876141
-
Therapies for Alzheimer's disease
-
DOI 10.1038/nrd2314, PII NRD2314
-
Melnikova I. Therapies for Alzheimer's disease. Nat Rev Drug Disc 2007;6:341-342. (Pubitemid 46696548)
-
(2007)
Nature Reviews Drug Discovery
, vol.6
, Issue.5
, pp. 341-342
-
-
Melnikova, I.1
-
2
-
-
4344580888
-
Strategies for disease modification in Alzheimer's disease
-
DOI 10.1038/nrn1495
-
Citron M. Strategies for disease modification in Alzheimer's disease. Nat Rev Neur 2004;5:677-685. (Pubitemid 39150139)
-
(2004)
Nature Reviews Neuroscience
, vol.5
, Issue.9
, pp. 677-685
-
-
Citron, M.1
-
4
-
-
33947179945
-
Social cognition: An early impairment in dementia of the Alzheimer type
-
Verdon C-M, Fossati P, Verny M, Dieudonne B, Teillet L, Nadel J. Social cognition: An early impairment in dementia of the Alzheimer type. Alzh Dis Ass Dis 2007;21:25-30.
-
(2007)
Alzh Dis Ass Dis
, vol.21
, pp. 25-30
-
-
Verdon, C.-M.1
Fossati, P.2
Verny, M.3
Dieudonne, B.4
Teillet, L.5
Nadel, J.6
-
5
-
-
0019972810
-
The cholinergic hypothesis of geriatric memory dysfunction
-
Bartus RT, Dean RL III, Beer B, Lippa AS. The cholinergic hypothesis of geriatric memory dysfunction. Science 1982;217:408-417. (Pubitemid 12048290)
-
(1982)
Science
, vol.217
, Issue.4558
, pp. 408-417
-
-
Bartus, R.T.1
Dean III, R.L.2
Beer, B.3
Lippa, A.S.4
-
6
-
-
0037135111
-
The amyloid hypothesis of Alzheimer's disease: Progress and problems on the road to therapeutics
-
Hardy J, Selkoe DJ. The amyloid hypothesis of Alzheimer's disease: Progress and problems on the road to therapeutics. Science 2002;297:353-357.
-
(2002)
Science
, vol.297
, pp. 353-357
-
-
Hardy, J.1
Selkoe, D.J.2
-
7
-
-
33750874958
-
Views on amyloid hypothesis and secretase inhibitors for treating Alzheimer's disease: Progress and problems
-
Nguyen J-T, Yamani A, Kiso Y. Views on amyloid hypothesis and secretase inhibitors for treating Alzheimer's disease: Progress and problems. Curr Pharm Des 2006;12:4295-4312.
-
(2006)
Curr Pharm Des
, vol.12
, pp. 4295-4312
-
-
Nguyen, J.-T.1
Yamani, A.2
Kiso, Y.3
-
8
-
-
0038176528
-
In vitro characterization of conditions for amyloid-beta peptide oligomerization and fibrillogenesis
-
Stine WB Jr, Dahlgren KN, Krafft GA, LaDu MJ. In vitro characterization of conditions for amyloid-beta peptide oligomerization and fibrillogenesis. J Biol Chem 2003;278:11612-11622.
-
(2003)
J Biol Chem
, vol.278
, pp. 11612-11622
-
-
Stine Jr., W.B.1
Dahlgren, K.N.2
Krafft, G.A.3
LaDu, M.J.4
-
9
-
-
24044493604
-
Compounds that bind APP and inhibit Aβ processing in vitro suggest a novel approach to Alzheimer disease therapeutics
-
DOI 10.1074/jbc.M414331200
-
Espeseth AS, Xu M, Huang Q, Coburn CA, Jones KLG, Ferrer M, Zuck PD, Strulovici B, Price EA, Wu G, Wolfe AL, Lineberger JE, Sardana M, Tugusheva K, Pietrak BL, Crouthamel M-C, Lai M-T, Dodson EC, Bazzo R, Shi X-P, Simon AJ, Li Y, Hazuda DJ. Compounds that bind APP and inhibit a processing in vitro suggest a novel approach to Alzheimer's disease therapeutics. J Biol Chem 2005;280:17792-17797. (Pubitemid 41389018)
-
(2005)
Journal of Biological Chemistry
, vol.280
, Issue.18
, pp. 17792-17797
-
-
Espeseth, A.S.1
Xu, M.2
Huang, Q.3
Coburn, C.A.4
Jones, K.L.G.5
Ferrer, M.6
Zuck, P.D.7
Strulovici, B.8
Price, E.A.9
Wu, G.10
Wolfe, A.L.11
Lineberger, J.E.12
Sardana, M.13
Tugusheva, K.14
Pietrak, B.L.15
Crouthamel, M.-C.16
Lai, M.-T.17
Dodson, E.C.18
Bazzo, R.19
Shi, X.-P.20
Simon, A.J.21
Li, Y.22
Hazuda, D.J.23
more..
-
10
-
-
0027258525
-
The carboxy terminus of the β-amyloid protein is critical for the seeding of amyloid formation: Implications for the pathogenesis of Alzheimer's disease
-
Jarrett JT, Berger EP, Lansbury PT Jr. The carboxy terminus of the β-amyloid protein is critical for the seeding of amyloid formation: Implications for the pathogenesis of Alzheimer's disease. Biochemistry 1993;32:4693-4697.
-
(1993)
Biochemistry
, vol.32
, pp. 4693-4697
-
-
Jarrett, J.T.1
Berger, E.P.2
Lansbury Jr., P.T.3
-
11
-
-
33845946933
-
Effect of acetylcholine on tau phosphorylation in human neuroblastoma cells
-
DOI 10.1385/JMN:30:1:185, PII JMN301185
-
Rubio A, Avila J, Pérez M. Effect of acetylcholine on tau phosphorylation in human neuroblastoma cells. J Mol Neurosci 2006;30:185-188. (Pubitemid 46035364)
-
(2006)
Journal of Molecular Neuroscience
, vol.30
, Issue.1-2
, pp. 185-188
-
-
Rubio, A.1
Avila, J.2
Perez, M.3
-
12
-
-
0031003233
-
The Alzheimer family of diseases: Many etiologies, one pathogenesis?
-
Hardy J. The Alzheimer family of diseases: Many etiologies, one pathogenesis? Proc Natl Acad Sci USA 1997;94:2095-2097.
-
(1997)
Proc Natl Acad Sci USA
, vol.94
, pp. 2095-2097
-
-
Hardy, J.1
-
13
-
-
20844458090
-
Synaptic targeting by Alzheimer's-related amyloid β oligomers
-
DOI 10.1523/JNEUROSCI.3432-04.2004
-
Lacor PN, Buniel MC, Chang L, Fernandez SJ, Gong Y, Viola KL, Lambert MP, Velasco PT, Bigio EB, Finch CE, Krafft GA, Klein WL. Synaptic targeting by Alzheimer's-related amyloid b oligomers. J Neurosci 2004;24:10191-10200. (Pubitemid 39492046)
-
(2004)
Journal of Neuroscience
, vol.24
, Issue.45
, pp. 10191-10200
-
-
Lacor, P.N.1
Buniel, M.C.2
Chang, L.3
Fernandez, S.J.4
Gong, Y.5
Viola, K.L.6
Lambert, M.P.7
Velasco, P.T.8
Bigio, E.H.9
Finch, C.E.10
Krafft, G.A.11
Klein, W.L.12
-
14
-
-
33846633336
-
Aβ oligomer-induced aberrations in synapse composition, shape, and density provide a molecular basis for loss of connectivity in Alzheimer's disease
-
DOI 10.1523/JNEUROSCI.3501-06.2007
-
Lacor PN, Buniel MC, Furlow PW, Clemente AS, Velasco PT, Wood M, Viola KL, Klein WL. Ab oligomer-induced aberrations in synapse composition, shape, and density provide a molecular basis for loss of connectivity in Alzheimer's disease. J Neurosci 2007;27:796-807. (Pubitemid 46174498)
-
(2007)
Journal of Neuroscience
, vol.27
, Issue.4
, pp. 796-807
-
-
Lacor, P.N.1
Buniel, M.C.2
Furlow, P.W.3
Clemente, A.S.4
Velasco, P.T.5
Wood, M.6
Viola, K.L.7
Klein, W.L.8
-
15
-
-
12844273354
-
The fetal basis of amyloidogenesis: Exposure to lead and latent overexpression of amyloid precursor protein and amyloid in the aging brain
-
Basha MR, Wei W, Bakheet SA, Benitez N, Siddiqi HK, Ge Y-W, Lahiri DK, Zawia NH. The fetal basis of amyloidogenesis: Exposure to lead and latent overexpression of amyloid precursor protein and amyloid in the aging brain. J Neurosci 2005;25:823-829.
-
(2005)
J Neurosci
, vol.25
, pp. 823-829
-
-
Basha, M.R.1
Wei, W.2
Bakheet, S.A.3
Benitez, N.4
Siddiqi, H.K.5
Ge, Y.-W.6
Lahiri, D.K.7
Zawia, N.H.8
-
16
-
-
23944444806
-
Molecular, structural, and functional characterization of Alzheimer's disease: Evidence for a relationship between default activity, amyloid, and memory
-
Buckner RL, Snyder AZ, Shannon BJ, LaRossa G, Sachs R, Fotenos AF, Sheline YI, Klunk WE, Mathis CA, Morris JC, Mintun MA. Molecular, structural, and functional characterization of Alzheimer's disease: Evidence for a relationship between default activity, amyloid, and memory. J Neurosci 2005;25:7709-7717.
-
(2005)
J Neurosci
, vol.25
, pp. 7709-7717
-
-
Buckner, R.L.1
Snyder, A.Z.2
Shannon, B.J.3
LaRossa, G.4
Sachs, R.5
Fotenos, A.F.6
Sheline, Y.I.7
Klunk, W.E.8
Mathis, C.A.9
Morris, J.C.10
Mintun, M.A.11
-
17
-
-
33947314641
-
Natural oligomers of the Alzheimer amyloid-β protein induce reversible synapse loss by modulating an NMDA-type glutamate receptor-dependent signaling pathway
-
DOI 10.1523/JNEUROSCI.4970-06.2007
-
Shankar GM, Bloodgood BL, Townsend M, Walsh DM, Selkoe DJ, Sabatini BL. Natural oligomers of the Alzheimer amyloid-β protein induce reversible synapse loss by modulating an NMDA-type glutamate receptor-dependent signaling pathway. J Neurosci 2007;27:2866-2875. (Pubitemid 46438992)
-
(2007)
Journal of Neuroscience
, vol.27
, Issue.11
, pp. 2866-2875
-
-
Shankar, G.M.1
Bloodgood, B.L.2
Townsend, M.3
Walsh, D.M.4
Selkoe, D.J.5
Sabatini, B.L.6
-
18
-
-
0025753852
-
The molecular pathology of Alzheimer's disease
-
Selkoe DJ. The molecular pathology of Alzheimer's disease. Neuron 1991;6:487-498.
-
(1991)
Neuron
, vol.6
, pp. 487-498
-
-
Selkoe, D.J.1
-
19
-
-
34247611095
-
Fibrillar and oligomeric β-amyloid as distinct local biomarkers for Alzheimer's disease
-
DOI 10.1196/annals.1379.023, Imaging and the Aging Brain
-
Montalto MC, Farrar G, Hehir CT. Fibrillar and oligomeric β-amyloid as distinct local biomarkers for Alzheimer's disease. Ann New York Acad Sci 2007;1097:239-258. (Pubitemid 47084898)
-
(2007)
Annals of the New York Academy of Sciences
, vol.1097
, pp. 239-258
-
-
Montalto, M.C.1
Farrar, G.2
Hehir, C.T.3
-
20
-
-
0031587286
-
Acetylcholinesterase promotes the aggregation of amyloid-β-peptide fragments by forming a complex with the growing fibrils
-
DOI 10.1006/jmbi.1997.1245
-
Alvarez A, Opazo C, Alarcon R, Garrido J, Inestrosa NC. Acetylcholinesterase promotes the aggregation of amyloid-beta-peptide fragments by forming a complex with the growing fibrils. J Mol Biol 1997;272:348-361. (Pubitemid 27410049)
-
(1997)
Journal of Molecular Biology
, vol.272
, Issue.3
, pp. 348-361
-
-
Alvarez, A.1
Opazo, C.2
Alarcon, R.3
Garrido, J.4
Inestrosa, N.C.5
-
21
-
-
33750883640
-
Targeting beta-amyloid pathogenesis through acetylcholinesterase inhibitors
-
Castro A, Martinez A. Targeting beta-amyloid pathogenesis through acetylcholinesterase inhibitors. Curr Pharm Des 2006;12:4377-4387.
-
(2006)
Curr Pharm Des
, vol.12
, pp. 4377-4387
-
-
Castro, A.1
Martinez, A.2
-
22
-
-
4544297127
-
Development of bivalent acetylcholinesterase inhibitors as potential therapeutic drugs for Alzheimer's disease
-
DOI 10.2174/1381612043383412
-
Du D-M, Carlier PR. Development of bivalent acetylcholinesterase inhibitors as potential therapeutic drugs for Alzheimer's disease. Curr Pharm Design 2004;10:3141-3156. (Pubitemid 39242909)
-
(2004)
Current Pharmaceutical Design
, vol.10
, Issue.25
, pp. 3141-3156
-
-
Du, D.-M.1
Carlier, P.R.2
-
23
-
-
15944386029
-
Ab initio molecular structure study of alkyl substitute analogues of Alzheimer drug phenserine: Structure-activity relationships for acetyl- and butyrylcholinesterase inhibitory action
-
Tezer N. Ab initio molecular structure study of alkyl substitute analogues of Alzheimer drug phenserine: Structure-activity relationships for acetyl- and butyrylcholinesterase inhibitory action. Theochem 2005;714:133-136.
-
(2005)
Theochem
, vol.714
, pp. 133-136
-
-
Tezer, N.1
-
24
-
-
33845918390
-
Dual binding site acetylcholinesterase inhibitors: Potential new disease-modifying agents for AD
-
Del Monte-Millán M, Gracía-Palomero E, Valenzuela R, Usán P, de Austria C, Muñoz-Rulz P, Rubio L, Dorronsoro I, Martínez A, Medina M. Dual binding site acetylcholinesterase inhibitors: Potential new disease-modifying agents for AD. J Mol Neurosci 2006;30:85-88.
-
(2006)
J Mol Neurosci
, vol.30
, pp. 85-88
-
-
Del Monte-Millán, M.1
Gracía-Palomero, E.2
Valenzuela, R.3
Usán, P.4
De Austria, C.5
Muñoz-Rulz, P.6
Rubio, L.7
Dorronsoro, I.8
Martínez, A.9
Medina, M.10
-
25
-
-
34247581682
-
Development of huperzine A and B for treatment of Alzheimer's disease
-
Bai D. Development of huperzine A and B for treatment of Alzheimer's disease. Pure Appl Chem 2007;79:469-479.
-
(2007)
Pure Appl Chem
, vol.79
, pp. 469-479
-
-
Bai, D.1
-
26
-
-
0029863697
-
Acetylcholinesterase accelerates assembly of amyloid-beta-peptides into Alzheimer's fibrils: Possible role of the peripheral site of the enzyme
-
Inestrosa NC, Alvarez A, Perez CA, Moreno RD, Vicente M, Linker C, Casanueva OI, Soto C, Garrido J. Acetylcholinesterase accelerates assembly of amyloid-beta-peptides into Alzheimer's fibrils: Possible role of the peripheral site of the enzyme. Neuron 1996;16:881-891.
-
(1996)
Neuron
, vol.16
, pp. 881-891
-
-
Inestrosa, N.C.1
Alvarez, A.2
Perez, C.A.3
Moreno, R.D.4
Vicente, M.5
Linker, C.6
Casanueva, O.I.7
Soto, C.8
Garrido, J.9
-
27
-
-
0035807054
-
A structural motif of acetylcholinesterase that promotes amyloid β-peptide fibril formation
-
DOI 10.1021/bi0101392
-
De Ferrari GV, Canales MA, Shin I, Weiner LM, Silman I, Inestrosa NC. A structural motif of acetylcholinesterase that promotes amyloid-peptide fibril formation. Biochemistry 2001;40:10447-10457. (Pubitemid 32816655)
-
(2001)
Biochemistry
, vol.40
, Issue.35
, pp. 10447-10457
-
-
De Ferrari, G.V.1
Canales, M.A.2
Shin, I.3
Weiner, L.M.4
Silman, I.5
Inestrosa, N.C.6
-
28
-
-
0034304034
-
Cholinesterase inhibitors stabilize Alzheimer's disease
-
Giacobini E. Cholinesterase inhibitors stabilize Alzheimer's disease. Neurochem Res 2000;25:1185-1190.
-
(2000)
Neurochem Res
, vol.25
, pp. 1185-1190
-
-
Giacobini, E.1
-
29
-
-
0028197477
-
Tacrine alters the secretion of the beta-amyloid precursor protein in cell lines
-
Lahiri DK, Lewis S, Farlow MR. Tacrine alters the secretion of beta-amyloid precursor protein in cell lines. J Neurosci Res 1994;37:777-787. (Pubitemid 24125794)
-
(1994)
Journal of Neuroscience Research
, vol.37
, Issue.6
, pp. 777-787
-
-
Lahiri, D.K.1
Lewis, S.2
Farlow, M.R.3
-
30
-
-
0037234423
-
The role of acetylcholinesterase in the pathogenesis of Alzheimer's disease
-
DOI 10.1358/dot.2003.39.1.740206
-
Rees TM, Brimijoin S. The role of acetylcholinesterase in the pathogenesis of Alzheimer's disease. Drugs Today 2003;39:75-83. (Pubitemid 36378463)
-
(2003)
Drugs of Today
, vol.39
, Issue.1
, pp. 75-83
-
-
Rees, T.M.1
Brimijoin, S.2
-
31
-
-
0036928604
-
Tau as a drug target in Alzheimer's disease
-
DOI 10.1385/JMN:19:3:337
-
Gozes I. Tau as a drug target in Alzheimer's disease. J Mol Neurosci 2002;19:337-338. (Pubitemid 36051526)
-
(2002)
Journal of Molecular Neuroscience
, vol.19
, Issue.3
, pp. 337-338
-
-
Gozes, I.1
-
32
-
-
0036860349
-
Metal complexing agents as therapies for Alzheimer's disease
-
DOI 10.1016/S0197-4580(02)00120-3, PII S0197458002001203
-
Bush AI. Metal complexing agents as therapies for Alzheimer's disease. Neur Aging 2002;23:1031-1038. (Pubitemid 35447784)
-
(2002)
Neurobiology of Aging
, vol.23
, Issue.6
, pp. 1031-1038
-
-
Bush, A.I.1
-
33
-
-
33750582961
-
Therapeutic approaches to Alzheimer's disease
-
DOI 10.1093/brain/awl280
-
Klafki H-W, Staufenbiel M, Kornhuber J, Wiltfang J. Therapeutic approaches to Alzheimer's disease. Brain 2006;129:2840-2855. (Pubitemid 44684507)
-
(2006)
Brain
, vol.129
, Issue.11
, pp. 2840-2855
-
-
Klafki, H.-W.1
Staufenbiel, M.2
Kornhuber, J.3
Wiltfang, J.4
-
34
-
-
33750858044
-
In vivo disrupting of amyloid deposition after injection of β-sheet breaker peptide into cerebral ventricle
-
Permanne BM, Saborio GP, Soto C. In vivo disrupting of amyloid deposition after injection of β-sheet breaker peptide into cerebral ventricle. Neur Aging 2000;21(S1):S87.
-
(2000)
Neur Aging
, vol.21
, Issue.S1
-
-
Permanne, B.M.1
Saborio, G.P.2
Soto, C.3
-
35
-
-
33745922350
-
Cyclohexanehexol inhibitors of Aβ aggregation prevent and reverse Alzheimer phenotype in a mouse model
-
DOI 10.1038/nm1423, PII NM1423
-
McLaurin J, Kierstead ME, Brown ME, Hawkes CA, Lambermon MHL, Phinney AL, Darabie AA, Cousins JE, French JE, Lan MF, Chen F, Wong SSN, Mount HTJ, Fraser PE, Westaway D, StGeorge-Hyslop P. Cyclohexanehexol inhibitors of A aggregation prevent and reverse Alzheimer phenotype in a mouse model. Nature Med 2006;12:801-808. (Pubitemid 44050070)
-
(2006)
Nature Medicine
, vol.12
, Issue.7
, pp. 801-808
-
-
McLaurin, J.1
Kierstead, M.E.2
Brown, M.E.3
Hawkes, C.A.4
Lambermon, M.H.L.5
Phinney, A.L.6
Darabie, A.A.7
Cousins, J.E.8
French, J.E.9
Lan, M.F.10
Chen, F.11
Wong, S.S.N.12
Mount, H.T.J.13
Fraser, P.E.14
Westaway, D.15
George-Hyslop, P.S.16
-
36
-
-
0035902619
-
Peripheral anti-Aβ antibody alters CNS and plasma Aβ clearance and decreases brain Aβ burden in a mouse model of Alzheimer's disease
-
DOI 10.1073/pnas.151261398
-
de Mattos RB, Bales KR, Cummins DJ, Dodart JC, Paul SM, Holtzman DM. Peripheral anti-Aβ antibody alters CNS and plasma Aβ clearance and decreases brain Aβ burden in a mouse model of Alzheimer's disease. Proc Natl Acad Sci USA 2001;98:8850-8855. (Pubitemid 32678116)
-
(2001)
Proceedings of the National Academy of Sciences of the United States of America
, vol.98
, Issue.15
, pp. 8850-8855
-
-
Demattos, R.B.1
Bales, K.R.2
Cummins, D.J.3
Dodart, J.-C.4
Paul, S.M.5
Holtzman, D.M.6
-
37
-
-
33748774150
-
Tramiprosate: Antiamyloidogenic agent treatment of Alzheimer's disease treatment of hemorrhagic stroke
-
DOI 10.1358/dof.2006.031.06.1001606
-
(a)Revill P, Serradell N, Bolos J. Tramiprosate: Antiamyloidogenic agent for treatment of Alzheimer's disease and hemorrhagic stroke. Drugs Fut 2006;31:498-501;37. (Pubitemid 44406097)
-
(2006)
Drugs of the Future
, vol.31
, Issue.6
, pp. 498-501
-
-
Revill, P.1
Serradell, N.2
Bolos, J.3
-
38
-
-
33745562109
-
Tramiprosate
-
(b)Wright TM. Tramiprosate. Drugs Today 2006;42:291-298.
-
(2006)
Drugs Today
, vol.42
, pp. 291-298
-
-
Wright, T.M.1
-
39
-
-
0029013727
-
Staging of Alzheimer's disease-related neurofibrillary changes
-
Braak H, Braak E. Staging of Alzheimer's disease-related neurofibrillary changes. Neur Aging 1995;16:271-278.
-
(1995)
Neur Aging
, vol.16
, pp. 271-278
-
-
Braak, H.1
Braak, E.2
-
40
-
-
0027453490
-
Activation of protein kinase C inhibits cellular production of the amyloid β-protein
-
Hung AY, Haass C, Nitsch RM, Qiu WQ, Citron M, Wurtman PJ, Growdon JH, Selkoe DJ. Activation of protein kinase C inhibits cellular production of the amyloid beta-protein. J Biol Chem 1993;268:22959-22962. (Pubitemid 23327996)
-
(1993)
Journal of Biological Chemistry
, vol.268
, Issue.31
, pp. 22959-22962
-
-
Hung, A.Y.1
Haass, C.2
Nitsch, R.M.3
Wei Qiao, Q.4
Citron, M.5
Wurtman, R.J.6
Growdon, J.H.7
Selkoe, D.J.8
-
41
-
-
0026476297
-
Release of Alzheimer amyloid precursor derivatives stimulated by activation of muscarinic acetylcholine receptors
-
Nitsch RM, Slack BE, Wurtman RJ, Growdon JH. Release of Alzheimer amyloid precursor derivatives stimulated by activation of muscarinic acetylcholine receptors. Science 1992;258:304-307.
-
(1992)
Science
, vol.258
, pp. 304-307
-
-
Nitsch, R.M.1
Slack, B.E.2
Wurtman, R.J.3
Growdon, J.H.4
-
42
-
-
85047690140
-
A disintegrin-metalloproteinase prevents amyloid plaque formation and hippocampal defects in an Alheizmer disease mouse model
-
DOI 10.1172/JCI200420864
-
Postina R, Schroeder A, Dewachter I, Bohl J, Schmitt U, Kojiro E. A disintegrin-metalloproteinase prevents amyloid plaque formation and hippocampal defects in an Alzheimer's disease mouse model. J Clin Invest 2004;113:1456-1464. (Pubitemid 39071701)
-
(2004)
Journal of Clinical Investigation
, vol.113
, Issue.10
, pp. 1456-1464
-
-
Postina, R.1
Schroeder, A.2
Dewachter, I.3
Bohl, J.4
Schmitt, U.5
Kojro, E.6
Prinzen, C.7
Endres, K.8
Hiemke, C.9
Blessing, M.10
Flamez, P.11
Dequenne, A.12
Godaux, E.13
Van Leuven, F.14
Fahrenholz, F.15
-
43
-
-
0001504829
-
Simvastatin strongly reduces levels of Alzheimer's disease β-amyloid peptides Aβ42 and Aβ40 in vitro and in vivo
-
DOI 10.1073/pnas.081620098
-
Fassbender K, Simons M, Bergmann C, Stroick M, Lutjohann D, Keller P, Runz H, Kuhl S, Bertsch T, Von Bergmann K, Hennerici M, Beyreuther K, Hartmann T. Simvastatin strongly reduces levels of Alzheimer's disease β-amyloid peptides Aβ42 and Aβ40 in vitro and in vivo. Proc Natl Acad Sci USA 2001;98:5856-5861. (Pubitemid 32435732)
-
(2001)
Proceedings of the National Academy of Sciences of the United States of America
, vol.98
, Issue.10
, pp. 5856-5861
-
-
Fassbender, K.1
Simons, M.2
Bergmann, C.3
Stroick, M.4
Lutjohann, D.5
Keller, P.6
Runz, H.7
Kuhl, S.8
Bertsch, T.9
Von Bergmann, K.10
Hennerici, M.11
Beyreuther, K.12
Hartmann, T.13
-
44
-
-
0035826909
-
Low cholesterol stimulates the nonamyloidogenic pathway by its effect on the α-secretase ADAM 10
-
DOI 10.1073/pnas.081612998
-
Kojiro E, Gimpl G, Lammich S, Marz W, Fahrenholz F. Low cholesterol stimulates the nonamyloidogenic pathway by its effect on the α-secretase ADAM10. Proc Natl Acad Sci USA 2001;98:5815-5820. (Pubitemid 32435725)
-
(2001)
Proceedings of the National Academy of Sciences of the United States of America
, vol.98
, Issue.10
, pp. 5815-5820
-
-
Kojro, E.1
Gimpl, G.2
Lammich, S.3
Marz, W.4
Fahrenholz, F.5
-
45
-
-
5744225747
-
Secretases as therapeutic targets in Alzheimer's disease: Patents 2000-2004
-
Larner AJ. Secretases as therapeutic targets in Alzheimer's disease: Patents 2000-2004. Expert Opin Ther Pat 2004;14:1403-1420.
-
(2004)
Expert Opin Ther Pat
, vol.14
, pp. 1403-1420
-
-
Larner, A.J.1
-
46
-
-
0032556859
-
Deficiency of presenilin-1 inhibits the normal cleavage of amyloid precursor protein
-
DOI 10.1038/34910
-
De Strooper B, Saftig P, Craessaerts K, Vanderstichele H, Guhde G, Annaert W, Von Figura K, Van Leuven F. Deficiency of presenilin-1 inhibits the normal cleavage of amyloid precursor protein. Nature 1998;391:387-390. (Pubitemid 28093512)
-
(1998)
Nature
, vol.391
, Issue.6665
, pp. 387-390
-
-
De Strooper, B.1
Saftig, P.2
Craessaerts, K.3
Vanderstichele, H.4
Guhde, G.5
Annaert, W.6
Von Figura, K.7
Van Leuven, F.8
-
47
-
-
0035005101
-
New protease inhibitors prevent gamma-secretase-mediated production of Aβ40/42 without affecting Notch cleavage
-
Petit A, Bihel F, Alves da Costa C, Pourquie O, Checler F, Kraus JL. New protease inhibitors prevent gamma-secretase-mediated production of Aβ40/42 without affecting Notch cleavage. Nat Cell Biol 2001;3:507-511.
-
(2001)
Nat Cell Biol
, vol.3
, pp. 507-511
-
-
Petit, A.1
Bihel, F.2
Alves Da Costa, C.3
Pourquie, O.4
Checler, F.5
Kraus, J.L.6
-
48
-
-
0037795653
-
Presenilin endoproteolysis mediated by an aspartyl protease activity pharmacologically distinct from γ-secretase
-
DOI 10.1046/j.1471-4159.2003.01799.x
-
Campbell WA, Reed ML, Strahle J,Wolfe MS, Xia W. Presenilin endoproteolysis mediated by an aspartyl protease activity pharmacologically distinct from gamma-secretase. J Neurochem 2003;85:1563-1574. (Pubitemid 36702568)
-
(2003)
Journal of Neurochemistry
, vol.85
, Issue.6
, pp. 1563-1574
-
-
Campbell, W.A.1
Reed, M.L.O.2
Strahle, J.3
Wolfe, M.S.4
Xia, W.5
-
49
-
-
0036833437
-
Therapeutic strategies for Alzheimer's disease
-
Wolfe MS. Therapeutic strategies for Alzheimer's disease. Nat Rev Drug Disc 2002;1:859-865.
-
(2002)
Nat Rev Drug Disc
, vol.1
, pp. 859-865
-
-
Wolfe, M.S.1
-
50
-
-
20944443757
-
Aryl sulfones: A new class of γ-secretase inhibitors
-
Teall M, Oakley P, Harrison T, Shaw D, Kay E, Elliott J, Gerhard U, Castro JL, Shearman M, Ball RG, Tsou NN. Aryl sulfones: A new class of γ-secretase inhibitors. Bioorg Med Chem Lett 2005;15:2685-2688.
-
(2005)
Bioorg Med Chem Lett
, vol.15
, pp. 2685-2688
-
-
Teall, M.1
Oakley, P.2
Harrison, T.3
Shaw, D.4
Kay, E.5
Elliott, J.6
Gerhard, U.7
Castro, J.L.8
Shearman, M.9
Ball, R.G.10
Tsou, N.N.11
-
51
-
-
24944439990
-
γ-Secretase as a therapeutic target for the treatment of Alzheimer's disease
-
DOI 10.2174/138161205774370771
-
Churcher I, Beher D. γ-Secretase as a therapeutic target for the treatment of Alzheimer's disease. Curr Pharm Des 2005;11:3363-3382. (Pubitemid 41300765)
-
(2005)
Current Pharmaceutical Design
, vol.11
, Issue.26
, pp. 3363-3382
-
-
Churcher, I.1
Beher, D.2
-
52
-
-
0035112647
-
BACE1 is the major β-secretase for generation of Aβ peptides by neurons
-
DOI 10.1038/85064
-
Cai H, Wang Y, McCarthy D, Wen H, Borchelt DR, Price DL, Donald L, Wong PC. BACE1 is the major β-secretase for generation of Aβ peptides by neurons. Nature Neurosci 2001;4:233-234. (Pubitemid 32194867)
-
(2001)
Nature Neuroscience
, vol.4
, Issue.3
, pp. 233-234
-
-
Cai, H.1
Wang, Y.2
McCarthy, D.3
Wen, H.4
Borchelt, D.R.5
Price, D.L.6
Wong, P.C.7
-
53
-
-
17944368176
-
The 'Arctic' APP mutation (E693G) causes Alzheimer's disease by enhanced Aβ protofibril formation
-
Nilsberth C, Westlind-Danielsson A, Eckman CB, Condron MM, Axelman K, Forsell C, Stenh C, Luthman J, Teplow DB, Younkin SG, Naeslund J, Lannfelt L. The 'Arctic' APP mutation (E693G) causes Alzheimer's disease by enhanced Aβ protofibril formation. Nature Neurosci 2001;4:887-893.
-
(2001)
Nature Neurosci
, vol.4
, pp. 887-893
-
-
Nilsberth, C.1
Westlind-Danielsson, A.2
Eckman, C.B.3
Condron, M.M.4
Axelman, K.5
Forsell, C.6
Stenh, C.7
Luthman, J.8
Teplow, D.B.9
Younkin, S.G.10
Naeslund, J.11
Lannfelt, L.12
-
54
-
-
0033518251
-
Purification and cloning of amyloid precursor protein beta-secretase from human brain
-
Sinha S, Anderson JP, Barbour R, Basi GS, Caccavello R, Davis D, Doan M, Dovey HF, Frigon N, Hong J, Jacobson-Croak K, Jewett N, Keim P, Knops J, Lieberburg I, Power M, Tan H, Tatsuno G, Tung J, Schenk D, Seubert P, Suomensaari SM, Wang S, Walker D, Zhao J, McConlogue L, John V. Purification and cloning of amyloid precursor protein beta-secretase from human brain. Nature 1999;402:537-540.
-
(1999)
Nature
, vol.402
, pp. 537-540
-
-
Sinha, S.1
Anderson, J.P.2
Barbour, R.3
Basi, G.S.4
Caccavello, R.5
Davis, D.6
Doan, M.7
Dovey, H.F.8
Frigon, N.9
Hong, J.10
Jacobson-Croak, K.11
Jewett, N.12
Keim, P.13
Knops, J.14
Lieberburg, I.15
Power, M.16
Tan, H.17
Tatsuno, G.18
Tung, J.19
Schenk, D.20
Seubert, P.21
Suomensaari, S.M.22
Wang, S.23
Walker, D.24
Zhao, J.25
McConlogue, L.26
John, V.27
more..
-
55
-
-
0034613320
-
Structure of the protease domain of memapsin 2 (β-secretase) complexed with inhibitor
-
Hong L, Koelsch G, Lin X, Wu S, Terzyan S, Ghosh AK, Zhang XC, Tang J. Structure of the protease domain of memapsin 2 (β-secretase) complexed with inhibitor. Science 2000;290:150-153.
-
(2000)
Science
, vol.290
, pp. 150-153
-
-
Hong, L.1
Koelsch, G.2
Lin, X.3
Wu, S.4
Terzyan, S.5
Ghosh, A.K.6
Zhang, X.C.7
Tang, J.8
-
56
-
-
0035974650
-
Structure-based design: Potent inhibitors of human brain memapsin 2 (β-secretase)
-
Ghosh AK, Bilcer G, Harwood C, Kawahama R, Shin D, Hussain KA, Hong L, Loy JA, Nguyen C, Koelsh G, Ermolieff J, Tang J. Structure-based design: Potent inhibitors of human brain memapsin 2 (β-secretase). J Med Chem 2001;44:2865-2868.
-
(2001)
J Med Chem
, vol.44
, pp. 2865-2868
-
-
Ghosh, A.K.1
Bilcer, G.2
Harwood, C.3
Kawahama, R.4
Shin, D.5
Hussain, K.A.6
Hong, L.7
Loy, J.A.8
Nguyen, C.9
Koelsh, G.10
Ermolieff, J.11
Tang, J.12
-
57
-
-
33750891503
-
β-Secretase inhibitors and methods of use
-
PCT Int Appl; WO03039454
-
Ghosh AK, Tang J, Bilcer G, Chang W, Hong L, Koelsch G, Loy J, Turner RT III. β-Secretase inhibitors and methods of use. PCT Int Appl 2003; WO03039454.
-
(2003)
-
-
Ghosh, A.K.1
Tang, J.2
Bilcer, G.3
Chang, W.4
Hong, L.5
Koelsch, G.6
Loy, J.7
Turner III, R.T.8
-
58
-
-
9644254194
-
Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (β-secretase)
-
DOI 10.1016/j.bmcl.2004.10.084, PII S0960894X04013241
-
Ghosh AK, Devasamudram T, Hong L, Dezuter C, Xu X, Weerasena V, Koelsch G, Bilcer G, Tang J. Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 β-secretase. Bioorg Med Chem Lett 2005;15:15-20. (Pubitemid 39575774)
-
(2005)
Bioorganic and Medicinal Chemistry Letters
, vol.15
, Issue.1
, pp. 15-20
-
-
Ghosh, A.K.1
Devasamudram, T.2
Hong, L.3
Dezutter, C.4
Xu, X.5
Weerasena, V.6
Koelsch, G.7
Bilcer, G.8
Tang, J.9
-
59
-
-
0344927114
-
KMI-008, a novel beta-secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-state mimic: Design and synthesis of substrate-based octapeptides
-
Shuto D, Kasai S, Kimura T, Liu P, Hidaka K, Hamada T, Shibakawa S, Hayashi Y, Hattori C, Szabo B, Ishiura S, Kiso Y. KMI-008, a novel beta-secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-state mimic: Design and synthesis of substrate-based octapeptides. Bioorg Med Chem Lett 2003;13:4273-4276.
-
(2003)
Bioorg Med Chem Lett
, vol.13
, pp. 4273-4276
-
-
Shuto, D.1
Kasai, S.2
Kimura, T.3
Liu, P.4
Hidaka, K.5
Hamada, T.6
Shibakawa, S.7
Hayashi, Y.8
Hattori, C.9
Szabo, B.10
Ishiura, S.11
Kiso, Y.12
-
60
-
-
10744219775
-
KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine
-
DOI 10.1016/j.bmcl.2003.12.088, PII S0960894X04000150
-
Kimura T, Shuto D, Kasai S, Liu P, Hidaka K, Hamada T, Hayashi Y, Hattori C, Asai M, Kitazume S, Saido TC, Ishiura S, Kiso Y. KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine. Bioorg Med Chem Lett 2004;14:1527-1531. (Pubitemid 38299443)
-
(2004)
Bioorganic and Medicinal Chemistry Letters
, vol.14
, Issue.6
, pp. 1527-1531
-
-
Kimura, T.1
Shuto, D.2
Kasai, S.3
Liu, P.4
Hidaka, K.5
Hamada, T.6
Hayashi, Y.7
Hattori, C.8
Asai, M.9
Kitazume, S.10
Saido, T.C.11
Ishiura, S.12
Kiso, Y.13
-
61
-
-
34247647440
-
Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human β-secretase (BACE1)
-
DOI 10.1016/j.bmc.2007.03.072, PII S0968089607002726
-
Manzenrieder F, Frank AO, Huber T, Dorner-Ciossek C, Kessler H. Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human β-secretase (BACE1). Bioorg Med Chem 2007;15:4136-4143. (Pubitemid 46678841)
-
(2007)
Bioorganic and Medicinal Chemistry
, vol.15
, Issue.12
, pp. 4136-4143
-
-
Manzenrieder, F.1
Frank, A.O.2
Huber, T.3
Dorner-Ciossek, C.4
Kessler, H.5
-
62
-
-
9644266667
-
Design and synthesis of highly active Alzheimer's β-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability
-
DOI 10.1016/j.bmcl.2004.09.090, PII S0960894X04012387
-
Kimura T, Shuto D, Hamada Y, Igawa N, Kasai S, Liu P, Hidaka K, Hamada T, Hayashi Y, Kiso Y. Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability. Bioorg Med Chem Lett 2005;15:211-215. (Pubitemid 39575813)
-
(2005)
Bioorganic and Medicinal Chemistry Letters
, vol.15
, Issue.1
, pp. 211-215
-
-
Kimura, T.1
Shuto, D.2
Hamada, Y.3
Igawa, N.4
Kasai, S.5
Liu, P.6
Hidaka, K.7
Hamada, T.8
Hayashi, Y.9
Kiso, Y.10
-
63
-
-
33644878338
-
The novel β-secretase inhibitor KMI-429 reduces amyloid b peptide production in amyloid precursor protein transgenic and wild-type mice
-
Asai M, Hattori C, Iwata N, Saido TC, Sasagawa N, Szabò B, Hashimoto Y, Maruyama K, Tanuma S, Kiso Y, Ishiura S. The novel β-secretase inhibitor KMI-429 reduces amyloid b peptide production in amyloid precursor protein transgenic and wild-type mice. J Neurochem 2006;96:533-540.
-
(2006)
J Neurochem
, vol.96
, pp. 533-540
-
-
Asai, M.1
Hattori, C.2
Iwata, N.3
Saido, T.C.4
Sasagawa, N.5
Szabò, B.6
Hashimoto, Y.7
Maruyama, K.8
Tanuma, S.9
Kiso, Y.10
Ishiura, S.11
-
64
-
-
33644988047
-
Design and synthesis of β-secretase (BACE1) inhibitors with P1′ carboxylic acid bioisosteres
-
Kimura T, Hamada Y, Stochaj M, Ikari H, Nagamine A, Abdel-Rahman H, Igawa N, Hidaka K, Nguyen J-T, Saito K, Hayashi Y, Kiso Y. Design and synthesis of β-secretase (BACE1) inhibitors with P1′ carboxylic acid bioisosteres. Bioorg Med Chem Lett 2006;16:2380-2386.
-
(2006)
Bioorg Med Chem Lett
, vol.16
, pp. 2380-2386
-
-
Kimura, T.1
Hamada, Y.2
Stochaj, M.3
Ikari, H.4
Nagamine, A.5
Abdel-Rahman, H.6
Igawa, N.7
Hidaka, K.8
Nguyen, J.-T.9
Saito, K.10
Hayashi, Y.11
Kiso, Y.12
-
65
-
-
33750877824
-
Novel inhibitor of β-amyloid cleavage enzyme
-
US Pat Appl; US2002115616
-
Boyd JG, Singleton DH. Novel inhibitor of β-amyloid cleavage enzyme. US Pat Appl 2002;US2002115616.
-
(2002)
-
-
Boyd, J.G.1
Singleton, D.H.2
-
66
-
-
0348147637
-
P3 cap modified Phe*-Ala series BACE inhibitors
-
DOI 10.1016/j.bmcl.2003.09.085
-
Chen S-H, Lamar J, Guo D, Kohn T, Yang H-C, McGee J, Timm D, Erickson J, Yip Y, May P, McCarthy J. P3 cap modified Phe*-Ala series BACE inhibitors. Bioorg Med Chem Lett 2004;14:245-250. (Pubitemid 38010226)
-
(2004)
Bioorganic and Medicinal Chemistry Letters
, vol.14
, Issue.1
, pp. 245-250
-
-
Chen, S.-H.1
Lamar, J.2
Guo, D.3
Kohn, T.4
Yang, H.-C.5
McGee, J.6
Timm, D.7
Erickson, J.8
Yip, Y.9
May, P.10
McCarthy, J.11
-
67
-
-
0037122704
-
Design of substrate-based inhibitors of human β-secretase
-
DOI 10.1021/jm0155695
-
Tung JS, Davis DL, Anderson JP,Walker DE, Mamo S, Jewett N, Hom RK, Sinha S, Thorsett ED, John V. Design of substrate-based inhibitors of human β-secretase. J Med Chem 2002;45:259-262. (Pubitemid 34073445)
-
(2002)
Journal of Medicinal Chemistry
, vol.45
, Issue.2
, pp. 259-262
-
-
Tung, J.S.1
Davis, D.L.2
Anderson, J.P.3
Walker, D.E.4
Mamo, S.5
Jewett, N.6
Hom, R.K.7
Sinha, S.8
Thorsett, E.D.9
John, V.10
-
68
-
-
1642477688
-
Rational design and synthesis of selective BACE-1 inhibitors
-
DOI 10.1016/j.bmcl.2003.11.061
-
Bradly F, Singh S, Crouthamel MC, Holloway MK, Coburn CA, Grasky VM, Bogusky M, Pennington MW, Vacca JP, Hazuda D, Lai M-T. Rational design and synthesis of selective BACE1 inhibitors. Bioorg Med Chem Lett 2004;14:601-614. (Pubitemid 38120278)
-
(2004)
Bioorganic and Medicinal Chemistry Letters
, vol.14
, Issue.3
, pp. 601-604
-
-
Brady, S.F.1
Singh, S.2
Crouthamel, M.-C.3
Holloway, M.K.4
Coburn, C.A.5
Garsky, V.M.6
Bogusky, M.7
Pennington, M.W.8
Vacca, J.P.9
Hazuda, D.10
Lai, M.-T.11
-
70
-
-
33745052352
-
Development of BACE1 inhibitors for Alzheimer's disease
-
DOI 10.2174/092986706777452489
-
Guo T, Hobbs DW. Development of BACE1 inhibitors for Alzheimer's disease. Curr Med Chem 2006;13:1811-1829. (Pubitemid 43871758)
-
(2006)
Current Medicinal Chemistry
, vol.13
, Issue.15
, pp. 1811-1829
-
-
Guo, T.1
Hobbs, D.W.2
-
71
-
-
33645544750
-
Small-sized BACE1 inhibitors
-
Ziora Z, Kimura T, Kiso Y. Small-sized BACE1 inhibitors. Drug Fut 2006;31:53-63.
-
(2006)
Drug Fut
, vol.31
, pp. 53-63
-
-
Ziora, Z.1
Kimura, T.2
Kiso, Y.3
-
72
-
-
34548392290
-
Ensemble-docking approach on BACE1: Pharmacophore perception and guidelines for drug design
-
Limongelli V, Marinelli L, Cosconati S, Braun HA, Schmidt B, Novellino E. Ensemble-docking approach on BACE1: Pharmacophore perception and guidelines for drug design. Chem Med Chem 2007;2:667-678.
-
(2007)
Chem Med Chem
, vol.2
, pp. 667-678
-
-
Limongelli, V.1
Marinelli, L.2
Cosconati, S.3
Braun, H.A.4
Schmidt, B.5
Novellino, E.6
-
73
-
-
33846160571
-
Aspartic proteases in drug discovery
-
DOI 10.2174/138161207779313560
-
Eder J, Hommel U, Cumin F, Martoglio B, Gerhartz B. Aspartic proteases in drug discovery. Curr Pharm Des 2007;11:271-285. (Pubitemid 46085279)
-
(2007)
Current Pharmaceutical Design
, vol.13
, Issue.3
, pp. 271-285
-
-
Eder, J.1
Hommel, U.2
Cumin, F.3
Martoglio, B.4
Gerhartz, B.5
-
74
-
-
0034881503
-
Transport characteristics of peptides and peptidomimetics: II. Hydroxyethylamine bioisostere-containing peptidomimetics as substrates for the oligopeptide transporter and P-glycoprotein in the intestinal mucosa
-
Gao J, Winslow SL, Vander Velde D, Aube J, Borchardt RT. Transport characteristics of peptides and peptidomimetics: II. Hydroxyethylamine bioisostere-containing peptidomimetics as substrates for the oligopeptide transporter and P-glycoprotein in the intestinal mucosa. J Pept Res 2001;57:361-371.
-
(2001)
J Pept Res
, vol.57
, pp. 361-371
-
-
Gao, J.1
Winslow, S.L.2
Vander Velde, D.3
Aube, J.4
Borchardt, R.T.5
-
75
-
-
21244449721
-
Preparation of 2-[2-amino- or 2-(N-heterocyclyl)ethyl]-6-(4- biphenylylmethoxy)tetralin derivatives as β-secretase inhibitors
-
Takeda Chem Ind. PCT Int Appl; WO2001087293
-
Miyamoto M, Matsui J, Fukumoto H, Tarui N. (Takeda Chem Ind) Preparation of 2-[2-amino- or 2-(N-heterocyclyl)ethyl]-6-(4-biphenylylmethoxy)tetralin derivatives as β-secretase inhibitors. PCT Int Appl 2001; WO2001087293.
-
(2001)
-
-
Miyamoto, M.1
Matsui, J.2
Fukumoto, H.3
Tarui, N.4
-
76
-
-
33750850737
-
Beta-secretase inhibitors
-
Takeda Chem Ind. Jpn Pat Appl; JP2002037731
-
Miyamoto M, Matsui J, Fukumoto H, Tarui N. (Takeda Chem Ind) Beta-secretase inhibitors. Jpn Pat Appl 2002; JP2002037731.
-
(2002)
-
-
Miyamoto, M.1
Matsui, J.2
Fukumoto, H.3
Tarui, N.4
-
77
-
-
66249115782
-
Secretase inhibitors
-
Takeda Chem Ind. Eur Pat Appl; EP1283039
-
Miyamoto M, Matsui J, Fukumoto H,Tarui N. (Takeda Chem Ind)-Secretase inhibitors. Eur Pat Appl 2003;EP1283039.
-
(2003)
-
-
Miyamoto, M.1
Matsui, J.2
Fukumoto, H.3
Tarui, N.4
-
78
-
-
21244460130
-
Preparation of benzamide derivatives as β-secretase inhibitors
-
Takeda Chem Ind. PCT Int Appl; WO 2004014843
-
Uchikawa O, Aso K, Koike T, Tarui N, Hirai K. (Takeda Chem Ind) Preparation of benzamide derivatives as β-secretase inhibitors. PCT Int Appl 2004; WO 2004014843.
-
(2004)
-
-
Uchikawa, O.1
Aso, K.2
Koike, T.3
Tarui, N.4
Hirai, K.5
-
79
-
-
66249093639
-
Preparation of indoles as inhibitors against aspartate protease, β-secretase, and amyloid β protein for treatment of nerve disorders and myopathy
-
Takeda Chem Ind. Jpn Pat Appl; JP2004149429
-
Watanabe H, Kurasawa O, Tarui N, Yorimoto T, Hirai K. (Takeda Chem Ind) Preparation of indoles as inhibitors against aspartate protease, β-secretase, and amyloid β protein for treatment of nerve disorders and myopathy. Jpn Pat Appl 2004; JP2004149429.
-
(2004)
-
-
Watanabe, H.1
Kurasawa, O.2
Tarui, N.3
Yorimoto, T.4
Hirai, K.5
-
80
-
-
21244504417
-
Preparation of phosphinylmethyl and phosphorylmethyl succinic and glutaric acid analogs as β-secretase inhibitors useful in the treatment of Alzheimer's disease
-
Neurologic Inc. PCT Int Appl; WO2002096897
-
Qiao L, Etchenberrigaray R. (Neurologic Inc.) Preparation of phosphinylmethyl and phosphorylmethyl succinic and glutaric acid analogs as β-secretase inhibitors useful in the treatment of Alzheimer's disease. PCT Int Appl 2002; WO2002096897.
-
(2002)
-
-
Qiao, L.1
Etchenberrigaray, R.2
-
81
-
-
66249140763
-
Phosphinylmethyl and phosphorylmethyl succinic and glutaric acid analogs as β-secretase inhibitors
-
Neurologic Inc. PCT Int Appl; US2003078240
-
Etchenberrigaray R, Qiao L. (Neurologic Inc.) Phosphinylmethyl and phosphorylmethyl succinic and glutaric acid analogs as β-secretase inhibitors. PCT Int Appl 2003; US2003078240.
-
(2003)
-
-
Etchenberrigaray, R.1
Qiao, L.2
-
82
-
-
21244484843
-
Preparation of β-carbolines and other inhibitors of BACE1 aspartic proteinase useful against Alzheimer's and other BACE-mediated diseases
-
Vertex Pharm. Inc. PCT Int Appl; WO2002088101
-
Bhisetti GR, Saunders JO, Murcko MA, Lepre CA, Britt SD, Come JH, Deninger DD, Wang T. (Vertex Pharm. Inc.) Preparation of β-carbolines and other inhibitors of BACE1 aspartic proteinase useful against Alzheimer's and other BACE-mediated diseases. PCT Int Appl 2002; WO2002088101.
-
(2002)
-
-
Bhisetti, G.R.1
Saunders, J.O.2
Murcko, M.A.3
Lepre, C.A.4
Britt, S.D.5
Come, J.H.6
Deninger, D.D.7
Wang, T.8
-
83
-
-
0142092495
-
Human β-Secretase (BACE) and BACE Inhibitors
-
DOI 10.1021/jm030247h
-
John V, Beck JP, Bienkowski MJ, Sinha S, Heinrikson RL. Human β-secretase (BACE) and BACE inhibitors. J Med Chem 2003;46:4625-4630. (Pubitemid 37271610)
-
(2003)
Journal of Medicinal Chemistry
, vol.46
, Issue.22
, pp. 4625-4630
-
-
John, V.1
Beck, J.P.2
Bienkowski, M.J.3
Sinha, S.4
Heinrikson, R.L.5
-
84
-
-
0034965645
-
Statine-derived tetrapeptide inhibitors of β-secretase
-
Elan Pharm, Inc.
-
Elan Pharm, Inc. Statine-derived tetrapeptide inhibitors of β-secretase. Exp Opin Ther Pat 2001;11:1047-1050.
-
(2001)
Exp Opin Ther Pat
, vol.11
, pp. 1047-1050
-
-
-
85
-
-
66249116829
-
Preparation of statine-derived tetrapeptides as inhibitors of β-secretase
-
Elan Pharm. Inc. PCT Int Appl; WO2000077030
-
John V, Tung J, Fang L, Mamo SS. (Elan Pharm. Inc.) Preparation of statine-derived tetrapeptides as inhibitors of β-secretase. PCT Int Appl 2000; WO2000077030.
-
(2000)
-
-
John, V.1
Tung, J.2
Fang, L.3
Mamo, S.S.4
-
86
-
-
9144267815
-
Design and Synthesis of Hydroxyethylene-Based Peptidomimetic Inhibitors of Human β-Secretase
-
DOI 10.1021/jm0304008
-
Hom RK, Gailunas AF, Mamo S, Fang LY, Tung JS,Walker DE, Davis D, Thorsett ED, Jewett NE, Moon JB, John V. Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human bsecretase. J Med Chem 2004;47:158-164. (Pubitemid 38040499)
-
(2004)
Journal of Medicinal Chemistry
, vol.47
, Issue.1
, pp. 158-164
-
-
Hom, R.K.1
Gailunas, A.F.2
Mamo, S.3
Fang, L.Y.4
Tung, J.S.5
Walker, D.E.6
Davis, D.7
Thorsett, E.D.8
Jewett, N.E.9
Moon, J.B.10
John, V.11
-
87
-
-
0037122704
-
Design of substrate-based inhibitors of human β-secretase
-
DOI 10.1021/jm0155695
-
Tung JS, Davis DL, Anderson JP,Walker DE, Mamo S, Jewett N, Hom RK, Sinha S, Thorsett ED, John V. Design of substrate-based inhibitors of human β-secretase. J Med Chem 2002;45:259-262. (Pubitemid 34073445)
-
(2002)
Journal of Medicinal Chemistry
, vol.45
, Issue.2
, pp. 259-262
-
-
Tung, J.S.1
Davis, D.L.2
Anderson, J.P.3
Walker, D.E.4
Mamo, S.5
Jewett, N.6
Hom, R.K.7
Sinha, S.8
Thorsett, E.D.9
John, V.10
-
88
-
-
33847368052
-
Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human β-secretase
-
DOI 10.1021/jm061242y
-
Maillard MC, Hom RK, Benson TE, Moon JB, Mamo S, Bienkowski M, Tomasselli AG, Woods DD, Prince DB, Paddock DJ, Emmons TL, Tucker JA, Dappen MS, Brogley L, Thorsett ED, Jewett N, Sinha S, John V. Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human β-secretase. J Med Chem 2007;50:776-781. (Pubitemid 46332990)
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, Issue.4
, pp. 776-781
-
-
Maillard, M.C.1
Hom, R.K.2
Benson, T.E.3
Moon, J.B.4
Mamo, S.5
Bienkowski, M.6
Tomasselli, A.G.7
Woods, D.D.8
Prince, D.B.9
Paddock, D.J.10
Emmons, T.L.11
Tucker, J.A.12
Dappen, M.S.13
Brogley, L.14
Thorsett, E.D.15
Jewett, N.16
Sinha, S.17
John, V.18
-
89
-
-
66249115457
-
Preparation of hydroxyethylenes with peptide subunits for pharmaceutical use in the treatment of Alzheimer's disease
-
Elan Pharm. Inc. PCT Int Appl; WO2001070672
-
Hom R, Mamo S, Tung J, Gailunas A, John V, Fang LY. (Elan Pharm. Inc.) Preparation of hydroxyethylenes with peptide subunits for pharmaceutical use in the treatment of Alzheimer's disease. PCT Int Appl 2001; WO2001070672.
-
(2001)
-
-
Hom, R.1
Mamo, S.2
Tung, J.3
Gailunas, A.4
John, V.5
Fang, L.Y.6
-
90
-
-
21244466127
-
Preparation of substituted amines for the treatment of Alzheimer's disease
-
Elan Pharm. Inc. PCT Int Appl; WO2002002505
-
Fang LY, Hom R, John V, Maillaird M. (Elan Pharm. Inc.) Preparation of substituted amines for the treatment of Alzheimer's disease. PCT Int Appl 2002; WO2002002505.
-
(2002)
-
-
Fang, L.Y.1
Hom, R.2
John, V.3
Maillaird, M.4
-
91
-
-
21244501518
-
Preparation of substituted amines to treat Alzheimer's disease
-
Elan Pharm. Inc. PCT Int Appl; WO2002002512
-
Maillard M, Hom C, Gailunas A, Jagodzinska B, Fang LY, John V, Freskos JN, Pulley SR, Beck JP, Tenbrink RE. (Elan Pharm. Inc.) Preparation of substituted amines to treat Alzheimer's disease. PCT Int Appl 2002; WO2002002512.
-
(2002)
-
-
Maillard, M.1
Hom, C.2
Gailunas, A.3
Jagodzinska, B.4
Fang, L.Y.5
John, V.6
Freskos, J.N.7
Pulley, S.R.8
Beck, J.P.9
Tenbrink, R.E.10
-
92
-
-
33646140305
-
Preparation of disubstituted amines for treating Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. Eur Pat Appl; EP1586556. PCT Int Appl 2002; WO2002002518
-
Beck JP, Gailunas A,Hom R, Jagodzinska B, John V, Maillaird M. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of disubstituted amines for treating Alzheimer's disease. Eur Pat Appl 2001; EP1586556. PCT Int Appl 2002; WO2002002518.
-
(2001)
-
-
Beck, J.P.1
Gailunas, A.2
Hom, R.3
Jagodzinska, B.4
John, V.5
Maillaird, M.6
-
93
-
-
66249148232
-
Preparation of β-hydroxyamine derivatives for the treatment of Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2003002122
-
John V, Hom R, Tucker J. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of β-hydroxyamine derivatives for the treatment of Alzheimer's disease. PCT Int Appl 2003; WO2003002122.
-
(2003)
-
-
John, V.1
Hom, R.2
Tucker, J.3
-
94
-
-
66249116473
-
Preparation of peptide isosteres containing a heterocycle useful in the treatment of Alzheimer's disease
-
Elan Pharm. Inc. PCT Int Appl; WO2003047576
-
John V. (Elan Pharm. Inc.) Preparation of peptide isosteres containing a heterocycle useful in the treatment of Alzheimer's disease. PCT Int Appl 2003; WO2003047576.
-
(2003)
-
-
John, V.1
-
95
-
-
33646124669
-
Preparation of hydroxyethylamines as aspartyl protease inhibitors for treatment of amyloidosis
-
Elan Pharm. Inc. PCT Int Appl; WO2005087751. and 2005; WO2005087752
-
John V, Maillard M, Tucker J, Aquino J, Jagodzinska B, Brogley L, Tung J, Bowers S, Dressen D, Probst G, Shah N. (Elan Pharm. Inc.) Preparation of hydroxyethylamines as aspartyl protease inhibitors for treatment of amyloidosis. PCT Int Appl 2005; WO2005087751. and 2005; WO2005087752.
-
(2005)
-
-
John, V.1
Maillard, M.2
Tucker, J.3
Aquino, J.4
Jagodzinska, B.5
Brogley, L.6
Tung, J.7
Bowers, S.8
Dressen, D.9
Probst, G.10
Shah, N.11
-
96
-
-
64349111983
-
Methods of treatment of amyloidosis using bi-aryl aspartyl protease inhibitors
-
US Pat Appl; US20060014737
-
John V, Hom R, Tucker J. Methods of treatment of amyloidosis using bi-aryl aspartyl protease inhibitors. US Pat Appl 2006; US20060014737.
-
(2006)
-
-
John, V.1
Hom, R.2
Tucker, J.3
-
97
-
-
66249146740
-
Methods of treating or preventing Alzheimer's disease using 4-aryl-3-aralkoxypipiperidines and azabicyclooctanes
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2002076440
-
Nieman JA, Fang L, Jagodzinska B. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Methods of treating or preventing Alzheimer's disease using 4-aryl-3-aralkoxypipiperidines and azabicyclooctanes. PCT Int Appl 2002; WO2002076440.
-
(2002)
-
-
Nieman, J.A.1
Fang, L.2
Jagodzinska, B.3
-
98
-
-
66249099704
-
Acylaminopropylhydrazines as β-secretase inhibitors
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2002094768
-
Schostarez H, Chrusciel RA, Cenko RS. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Acylaminopropylhydrazines as β-secretase inhibitors. PCT Int Appl 2002; WO2002094768.
-
(2002)
-
-
Schostarez, H.1
Chrusciel, R.A.2
Cenko, R.S.3
-
99
-
-
33750883752
-
Preparation of macrocycles useful in the treatment of Alzheimer's disease
-
Elan Pharm. Inc. Pharmacia & Upjohn Comp. PCT Int Appl; WO2002100399
-
Pulley SR, Beck JP, Tenbrink RE, Jacobs JS. (Elan Pharm. Inc. Pharmacia & Upjohn Comp.) Preparation of macrocycles useful in the treatment of Alzheimer's disease. PCT Int Appl 2002; WO2002100399.
-
(2002)
-
-
Pulley, S.R.1
Beck, J.P.2
Tenbrink, R.E.3
Jacobs, J.S.4
-
100
-
-
33750883752
-
Macrocycles useful in the treatment of Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2002100856
-
Pulley SR, Beck JP, Tenbrink RE. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Macrocycles useful in the treatment of Alzheimer's disease. PCT Int Appl 2002; WO2002100856.
-
(2002)
-
-
Pulley, S.R.1
Beck, J.P.2
Tenbrink, R.E.3
-
101
-
-
66249126129
-
Preparation of aminediols as β-secretase inhibitors for the treatment of Alzheimer's and other diseases characterized by deposition of Aβ peptide
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2002100818
-
Schostarez HJ, Chrusciel RA. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of aminediols as β-secretase inhibitors for the treatment of Alzheimer's and other diseases characterized by deposition of Aβ peptide. PCT Int Appl 2002; WO2002100818.
-
(2002)
-
-
Schostarez, H.J.1
Chrusciel, R.A.2
-
102
-
-
66249089992
-
Aminodiols useful in the treatment of Alzheimer's disease and similar diseases
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2003043618
-
Schostarez HJ, Hanson GJ. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Aminodiols useful in the treatment of Alzheimer's disease and similar diseases. PCT Int Appl 2003; WO2003043618.
-
(2003)
-
-
Schostarez, H.J.1
Hanson, G.J.2
-
103
-
-
66249145220
-
Preparation of amine 1,2- and 1,3-diol alditols and their use for treatment of Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2003043975
-
Romero AG, Schostarez H, Roels CM. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of amine 1,2- and 1,3-diol alditols and their use for treatment of Alzheimer's disease. PCT Int Appl 2003; WO2003043975.
-
(2003)
-
-
Romero, A.G.1
Schostarez, H.2
Roels, C.M.3
-
104
-
-
33750410586
-
Preparation and use of aza-bicyclononanes for the treatment of Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2003000261
-
Beck JP. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation and use of aza-bicyclononanes for the treatment of Alzheimer's disease. PCT Int Appl 2003; WO2003000261.
-
(2003)
-
-
Beck, J.P.1
-
105
-
-
66249121554
-
Preparation of diamine diols as β-secretase inhibitors for the treatment of Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2003006013
-
Schostarez HJ, Chrusciel RA. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of diamine diols as β-secretase inhibitors for the treatment of Alzheimer's disease. PCT Int Appl 2003; WO2003006013.
-
(2003)
-
-
Schostarez, H.J.1
Chrusciel, R.A.2
-
106
-
-
66249121554
-
Preparation of diamine diols as β-secretase inhibitors for the treatment of Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2003006453
-
Schostarez HJ, Chrusciel RA. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of diamine diols as β-secretase inhibitors for the treatment of Alzheimer's disease. PCT Int Appl 2003; WO2003006453.
-
(2003)
-
-
Schostarez, H.J.1
Chrusciel, R.A.2
-
107
-
-
66249143923
-
Preparation of N-(3-amino-2-hydroxypropyl) substituted alkanamides as inhibitors of the beta secretase enzyme for treating Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2003006423
-
Gailunas A, Hom R, John V, Mailard M, Chrusciel RA, Fisher J, Jacobs J, Freskos JN, Brown DL, Fobian YM. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of N-(3-amino-2-hydroxypropyl) substituted alkanamides as inhibitors of the beta secretase enzyme for treating Alzheimer's disease. PCT Int Appl 2003; WO2003006423.
-
(2003)
-
-
Gailunas, A.1
Hom, R.2
John, V.3
Mailard, M.4
Chrusciel, R.A.5
Fisher, J.6
Jacobs, J.7
Freskos, J.N.8
Brown, D.L.9
Fobian, Y.M.10
-
108
-
-
33646131803
-
Preparation of 2-hydroxy-3-aminoalkylbenzamides as β-secretase inhibitors for the treatment of Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2004094384
-
Aquino J, John V, Tucker JA, Hom R, Pulley S, Tenbrink R. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of 2-hydroxy-3- aminoalkylbenzamides as β-secretase inhibitors for the treatment of Alzheimer's disease. PCT Int Appl 2004; WO2004094384.
-
(2004)
-
-
Aquino, J.1
John, V.2
Tucker, J.A.3
Hom, R.4
Pulley, S.5
Tenbrink, R.6
-
109
-
-
66249095805
-
Preparation of phenethylamines for the treatment of Alzheimer's disease
-
(Elan Pharm. Inc.). PCT Int Appl; WO2003027068
-
Gailunas AT, Tucker JA, John V. Preparation of phenethylamines for the treatment of Alzheimer's disease. (Elan Pharm. Inc.). PCT Int Appl 2003; WO2003027068.
-
(2003)
-
-
Gailunas, A.T.1
Tucker, J.A.2
John, V.3
-
110
-
-
66249102141
-
Preparation of arylhydroxypropylamines used for treatment of Alzheimer's disease and to reduce amyloid beta peptide formation
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2003029169
-
Fisher JF, Jacobs JS, Scherer BA. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of arylhydroxypropylamines used for treatment of Alzheimer's disease and to reduce amyloid beta peptide formation. PCT Int Appl 2003; WO2003029169.
-
(2003)
-
-
Fisher, J.F.1
Jacobs, J.S.2
Scherer, B.A.3
-
111
-
-
66249115113
-
Preparation of allylamides useful in the treatment of Alzheimer's disease
-
Elan Pharm. Inc. PCT Int Appl; WO2003030886
-
Roy H. (Elan Pharm. Inc.) Preparation of allylamides useful in the treatment of Alzheimer's disease. PCT Int Appl 2003; WO2003030886.
-
(2003)
-
-
Roy, H.1
-
112
-
-
66249137950
-
Preparation of hydroxy substituted indanylamides for the treatment of Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2003037325
-
Beck JP. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of hydroxy substituted indanylamides for the treatment of Alzheimer's disease. PCT Int Appl 2003; WO2003037325.
-
(2003)
-
-
Beck, J.P.1
-
113
-
-
33646135511
-
Preparation of N0, N′-susbstituted-1,3-diamino-2-hydroxypropanes for treating Alzheimer's disease
-
(Elan Pharm. Inc., Pharmacia & Upjohn Comp.) PCT Int Appl; WO2003040096
-
John V, Maillard M, Jagodzinska B, Beck JP, Gailunas A, Fang L, Sealy J, Tenbrink R, Freskos J, Mickelson J, Samala L, Hom R. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of N0, N′-susbstituted-1,3- diamino-2-hydroxypropanes for treating Alzheimer's disease. PCT Int Appl 2003; WO2003040096.
-
(2003)
-
-
John, V.1
Maillard, M.2
Jagodzinska, B.3
Beck, J.P.4
Gailunas, A.5
Fang, L.6
Sealy, J.7
Tenbrink, R.8
Freskos, J.9
Mickelson, J.10
Samala, L.11
Hom, R.12
-
114
-
-
66249125511
-
Preparation of substituted amine as prodrugs useful in treating Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2003072535
-
Jagodzinska B, Maillard M, Beck JP, Tenbrink R, Getman D. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of substituted amine as prodrugs useful in treating Alzheimer's disease. PCT Int Appl 2003; WO2003072535.
-
(2003)
-
-
Jagodzinska, B.1
Maillard, M.2
Beck, J.P.3
Tenbrink, R.4
Getman, D.5
-
115
-
-
21244494587
-
A preparation of 1,3-diamino-2-hydroxypropane derivatives as beta-secretase enzyme inhibitors
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2004022523
-
Fobian YM, Freskos JN, Jagodzinska B. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) A preparation of 1,3-diamino-2-hydroxypropane derivatives as beta-secretase enzyme inhibitors. PCT Int Appl 2004; WO2004022523.
-
(2004)
-
-
Fobian, Y.M.1
Freskos, J.N.2
Jagodzinska, B.3
-
116
-
-
66249126444
-
Preparation of ring-containing N-acetyl 2-hydroxy-1,3-diamonoalkanes as β-secretase inhibitors for treating Alzheimer's disease and other diseases characterized by deposition of Aβ-peptide
-
Elan Pharm. Inc., Pfizer, Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2004024081
-
Maillard M, Baldwin ET, Beck JT, Hughesm R, John V, Pulley SR, Tenbrink R. (Elan Pharm. Inc., Pfizer, Inc., Pharmacia & Upjohn Comp.) Preparation of ring-containing N-acetyl 2-hydroxy-1,3-diamonoalkanes as β-secretase inhibitors for treating Alzheimer's disease and other diseases characterized by deposition of Aβ-peptide. PCT Int Appl 2004; WO2004024081.
-
(2004)
-
-
Maillard, M.1
Baldwin, E.T.2
Beck, J.T.3
Hughesm, R.4
John, V.5
Pulley, S.R.6
Tenbrink, R.7
-
117
-
-
33646149339
-
Preparation of phenacyl-substituted 2-hydroxy-3-diaminoalkanes as inhibitors of β-secretase
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2004094413
-
Aquino J, John V, Tucker JA, Hom R, Pulley S, Tenbrink R. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of phenacyl-substituted 2-hydroxy-3-diaminoalkanes as inhibitors of β-secretase. PCT Int Appl 2004; WO2004094413.
-
(2004)
-
-
Aquino, J.1
John, V.2
Tucker, J.A.3
Hom, R.4
Pulley, S.5
Tenbrink, R.6
-
118
-
-
66249091384
-
Preparation of substituted piperidines and piperazines useful as β-secretase inhibitors against Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2003043987
-
John V, Moon JB, Pulley SR, Rich DH, Brown D. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of substituted piperidines and piperazines useful as β-secretase inhibitors against Alzheimer's disease. PCT Int Appl 2003; WO2003043987.
-
(2003)
-
-
John, V.1
Moon, J.B.2
Pulley, S.R.3
Rich, D.H.4
Brown, D.5
-
119
-
-
21244431743
-
Preparation of substituted hydroxyethylamines as β-secretase inhibitors
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2003050073
-
Tenbrink R, Maillard M, Warpehoski M. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of substituted hydroxyethylamines as β-secretase inhibitors. PCT Int Appl 2003; WO2003050073.
-
(2003)
-
-
Tenbrink, R.1
Maillard, M.2
Warpehoski, M.3
-
120
-
-
66249125511
-
Preparation of substituted amino carboxamides for the treatment of Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2003057721
-
Jagodzinska B, Warpehoski MA. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of substituted amino carboxamides for the treatment of Alzheimer's disease. PCT Int Appl 2003; WO2003057721.
-
(2003)
-
-
Jagodzinska, B.1
Warpehoski, M.A.2
-
121
-
-
33750885583
-
Methods of treating Alzheimer's disease using aromatically substituted ω-aminoalkanoic acid amides and alkanoic acid diamides
-
Elan Pharm. Inc. PCT Int Appl; WO2003103652
-
Maillard M, Varghese J. (Elan Pharm. Inc) Methods of treating Alzheimer's disease using aromatically substituted ω-aminoalkanoic acid amides and alkanoic acid diamides. PCT Int Appl 2003; WO2003103652.
-
(2003)
-
-
Maillard, M.1
Varghese, J.2
-
122
-
-
66249106201
-
Methods of treating Alzheimer's disease and methods of preparing δ-amino-γ-hydroxy-ω-arylalkanoic acid amides
-
Elan Pharm. Inc. PCT Int Appl; WO2003103653
-
John V, Maillard M. (Elan Pharm. Inc) Methods of treating Alzheimer's disease and methods of preparing δ-amino-γ-hydroxy-ω- arylalkanoic acid amides. PCT Int Appl 2003; WO2003103653.
-
(2003)
-
-
John, V.1
Maillard, M.2
-
123
-
-
66249116470
-
Preparation of hydroxyaminopropyl benzamides for the treatment of Alzheimer's disease
-
Elan Pharm. Inc. PCT Int Appl; WO2004029019
-
Hom R, Varghese J. (Elan Pharm. Inc.) Preparation of hydroxyaminopropyl benzamides for the treatment of Alzheimer's disease. PCT Int Appl 2004; WO2004029019.
-
(2004)
-
-
Hom, R.1
Varghese, J.2
-
124
-
-
33646139612
-
Preparation of hydroxypropyl amide peptide analogs for the treatment of Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2005042472
-
Tucker JA. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of hydroxypropyl amide peptide analogs for the treatment of Alzheimer's disease. PCT Int Appl 2005; WO2005042472.
-
(2005)
-
-
Tucker, J.A.1
-
125
-
-
66249139032
-
Preparation of peptide-related substituted ureas and carbamates for the treatment of Alzheimer's disease
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2004050609
-
Pulley SR, Tucker JA. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of peptide-related substituted ureas and carbamates for the treatment of Alzheimer's disease. PCT Int Appl 2004; WO2004050609.
-
(2004)
-
-
Pulley, S.R.1
Tucker, J.A.2
-
126
-
-
33646135969
-
Preparation of substituted ureas and carbamates, phenacyl-2-hydroxy-3- diaminoalkane and benzamide-2- hydroxy-3-diaminoalkane aspartyl protease and β-secretase inhibitors for treating conditions associated with amyloidosis such Alzheimer's disease
-
Elan Pharm. Inc. PCT Int Appl; WO2005087215
-
John V, Maillard M, Tucker J, Aquino J, Hom R, Tung J, Dressen D, Shah N, Neitz RJ. (Elan Pharm. Inc.) Preparation of substituted ureas and carbamates, phenacyl-2-hydroxy-3-diaminoalkane and benzamide-2- hydroxy-3-diaminoalkane aspartyl protease and β-secretase inhibitors for treating conditions associated with amyloidosis such Alzheimer's disease. PCT Int Appl 2005; WO2005087215.
-
(2005)
-
-
John, V.1
Maillard, M.2
Tucker, J.3
Aquino, J.4
Hom, R.5
Tung, J.6
Dressen, D.7
Shah, N.8
Neitz, R.J.9
-
127
-
-
33646155289
-
Preparation of N-(3-amino- 2-hydroxypropyl)acetamides as aspartyl protease and beta-secretase inhibitors for treating conditions associated with amyloidosis such Alzheimer's disease
-
Elan Pharm. Inc. PCT Int Appl; WO2005070407
-
John V, Hom R, Saely J, Aquino J, Probst G, Tung J, Fang L. (Elan Pharm. Inc.) Preparation of N-(3-amino- 2-hydroxypropyl)acetamides as aspartyl protease and beta-secretase inhibitors for treating conditions associated with amyloidosis such Alzheimer's disease. PCT Int Appl 2005; WO2005070407.
-
(2005)
-
-
John, V.1
Hom, R.2
Saely, J.3
Aquino, J.4
Probst, G.5
Tung, J.6
Fang, L.7
-
128
-
-
33646155289
-
Preparation of bicyclic compounds as aspartyl protease and beta-secretase inhibitors for treating conditions associated with amyloidosis such Alzheimer's disease
-
Elan Pharm. Inc. PCT Int Appl; WO2005087714
-
John V, Maillard M, Fang L, Tucker J, Brogley L, Aquino J, Bowers S, Probst G, Tung J. (Elan Pharm. Inc.) Preparation of bicyclic compounds as aspartyl protease and beta-secretase inhibitors for treating conditions associated with amyloidosis such Alzheimer's disease. PCT Int Appl 2005; WO2005087714.
-
(2005)
-
-
John, V.1
Maillard, M.2
Fang, L.3
Tucker, J.4
Brogley, L.5
Aquino, J.6
Bowers, S.7
Probst, G.8
Tung, J.9
-
129
-
-
66249145567
-
Preparation of 2-amino- and 2-thio-substituted 1,3-diaminopropanes as β-secretase inhibitors for treating Alzheimer's disease and other diseases characterized by deposition of Aβ-peptide
-
Elan Pharm. Inc., Pharmacia & Upjohn Comp. PCT Int Appl; WO2005095326
-
Hom R, Tucker J, John V, Shah N. (Elan Pharm. Inc., Pharmacia & Upjohn Comp.) Preparation of 2-amino- and 2-thio-substituted 1,3-diaminopropanes as β-secretase inhibitors for treating Alzheimer's disease and other diseases characterized by deposition of Aβ-peptide. PCT Int Appl 2005; WO2005095326.
-
(2005)
-
-
Hom, R.1
Tucker, J.2
John, V.3
Shah, N.4
-
130
-
-
66249117825
-
Preparation of oxime, hydrazone and other derivative substituted hydroxyethylamine selective β-secretase inhibitors for treating amyloidosis
-
Elan Pharm. Inc. PCT Int Appl; WO2006010095
-
John V, Maillard M, Jagodzinska B, Aquino J, Probst G, Tung JS. (Elan Pharm. Inc.) Preparation of oxime, hydrazone and other derivative substituted hydroxyethylamine selective β-secretase inhibitors for treating amyloidosis. PCT Int Appl 2006; WO2006010095.
-
(2006)
-
-
John, V.1
Maillard, M.2
Jagodzinska, B.3
Aquino, J.4
Probst, G.5
Tung, J.S.6
-
131
-
-
66249129552
-
Preparation of oxime-containing N-(3-amino-1-arylmethyl-2-hydroxypropyl) carboxamides and related selective β-secretase inhibitors for treating amyloidosis
-
Elan Pharm. Inc. PCT Int Appl; WO2006010094
-
Sealy J, Hom R, John V, Probst G, Tung JS. (Elan Pharm. Inc.) Preparation of oxime-containing N-(3-amino-1-arylmethyl-2-hydroxypropyl) carboxamides and related selective β-secretase inhibitors for treating amyloidosis. PCT Int Appl 2006; WO2006010094.
-
(2006)
-
-
Sealy, J.1
Hom, R.2
John, V.3
Probst, G.4
Tung, J.S.5
-
132
-
-
66249138304
-
Preparation of ethanolcyclicamines selective β-secretase inhibitors for treatment of amyloidosis
-
Elan Pharm. Inc. PCT Int Appl; WO2006026533 and 2006; WO2006026532
-
Hom R, Fang L, John V. (Elan Pharm. Inc.) Preparation of ethanolcyclicamines selective β-secretase inhibitors for treatment of amyloidosis. PCT Int Appl 2006; WO2006026533 and 2006; WO2006026532.
-
(2006)
-
-
Hom, R.1
Fang, L.2
John, V.3
-
133
-
-
66249100713
-
Preparation of aryl cyclopropyl(heterocyclyl)aminohydroxybutylamides as aspartyl protease inhibitors for treatment of amyloidosis
-
Elan Pharm. Inc. PCT Int Appl; WO2007047306 and 2007; WO2007047305
-
Hom R, Toth G, Probst G, Bowers S, Truong A, Tung JS. (Elan Pharm. Inc.) Preparation of aryl cyclopropyl(heterocyclyl)aminohydroxybutylamides as aspartyl protease inhibitors for treatment of amyloidosis. PCT Int Appl 2007; WO2007047306 and 2007; WO2007047305.
-
(2007)
-
-
Hom, R.1
Toth, G.2
Probst, G.3
Bowers, S.4
Truong, A.5
Tung, J.S.6
-
134
-
-
9744221865
-
Identification of a small molecule nonpeptide active site β-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases
-
DOI 10.1021/jm049388p
-
Coburn CA, Stachel SJ, Li Y-M, Rush DM, Steele TG, Chen-Dodson E, Holloway MK, Xu M, Huang Q, Lai M-T, Di Muzio J, Crouthamel M-C, Shi X-P, Sardana V, Chen Z, Munshi S, Kuo L, Makara GM, Annis DA, Tadikinda PK, Nash HM, Vacca JP, Wang T. Identification of a small molecule nonpeptide active site β-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases. J Med Chem 2004;47:6117-6119. (Pubitemid 39587236)
-
(2004)
Journal of Medicinal Chemistry
, vol.47
, Issue.25
, pp. 6117-6119
-
-
Coburn, C.A.1
Stachel, S.J.2
Li, Y.-M.3
Rush, D.M.4
Steele, T.G.5
Chen-Dodson, E.6
Holloway, M.K.7
Xu, M.8
Huang, Q.9
Lai, M.-T.10
Dimuzio, J.11
Crouthamel, M.-C.12
Shi, X.-P.13
Sardana, V.14
Chen, Z.15
Munshi, S.16
Kuo, L.17
Makara, G.M.18
Annis, D.A.19
Tadikonda, P.K.20
Nash, H.M.21
Vacca, J.P.22
Wang, T.23
more..
-
135
-
-
66249089669
-
Preparation of aminopently-aminooxoethylphenylcarboxamides as β-secretase inhibitors for treatment of Alzheimer's disease
-
Merck & Co. PCT Int Appl; WO2005113484
-
Coburn CA, Steele TG, Vacca JP, Annis DA Jr, Makara GM, Nash HM, Tadikonda PK, Praveen K, Wang T. (Merck & Co.) Preparation of aminopently-aminooxoethylphenylcarboxamides as β-secretase inhibitors for treatment of Alzheimer's disease. PCT Int Appl 2005; WO2005113484.
-
(2005)
-
-
Coburn, C.A.1
Steele, T.G.2
Vacca, J.P.3
Annis Jr., D.A.4
Makara, G.M.5
Nash, H.M.6
Tadikonda, P.K.7
Praveen, K.8
Wang, T.9
-
136
-
-
10644249886
-
Structure-based design of potent and selective cell-permeable inhibitors of human β-secretase (BACE-1)
-
DOI 10.1021/jm049379g
-
Stachel SJ, Coburn CA, Steele TG, Jones KG, Loutzenhiser EF, Gregro AR, Rajapakse HA, Lai M-T, Crouthamel M-C, Xu M, Tugusheva K, Lineberger JE, Pietrak BL, Espeseth AS, Shi X-P, Chen-Dodson E, Holloway M-K, Munshi S, Simon AJ, Kuo L, Vacca JP. Structure-based design of potent and selective cell-permeable inhibitors of human β-secretase (BACE1). J Med Chem 2004;47:6447-6450. (Pubitemid 39657304)
-
(2004)
Journal of Medicinal Chemistry
, vol.47
, Issue.26
, pp. 6447-6450
-
-
Stachel, S.J.1
Coburn, C.A.2
Steele, T.G.3
Jones, K.G.4
Loutzenhiser, E.F.5
Gregro, A.R.6
Rajapakse, H.A.7
Lai, M.-T.8
Crouthamel, M.-C.9
Xu, M.10
Tugusheva, K.11
Lineberger, J.E.12
Pietrak, B.L.13
Espeseth, A.S.14
Shi, X.-P.15
Chen-Dodson, E.16
Holloway, M.K.17
Munshi, S.18
Simon, A.J.19
Kuo, L.20
Vacca, J.P.21
more..
-
137
-
-
21244479168
-
Preparation of phenylcarboxamide derivatives as β-secretase inhibitors for treatment of Alzheimer's disease
-
PCT Int Appl; WO2004043916
-
Coburn CA, Stachel SJ, Vacca JP. Preparation of phenylcarboxamide derivatives as β-secretase inhibitors for treatment of Alzheimer's disease. PCT Int Appl 2004; WO2004043916.
-
(2004)
-
-
Coburn, C.A.1
Stachel, S.J.2
Vacca, J.P.3
-
138
-
-
29544449814
-
Conformationally biased P3 amide replacements of β-secretase inhibitors
-
DOI 10.1016/j.bmcl.2005.10.032, PII S0960894X0501317X
-
Stachel SJ, Coburn CA, Steele TG, Crouthamel M-C, Pietrak BL, Lai M-T, Holloway MK, Munshi SK, Graham SL, Vacca JP. Conformationally biased P3 amide replacements of β-secretase inhibitors. Bioorg Med Chem Lett 2006;16:641-644. (Pubitemid 43014850)
-
(2006)
Bioorganic and Medicinal Chemistry Letters
, vol.16
, Issue.3
, pp. 641-644
-
-
Stachel, S.J.1
Coburn, C.A.2
Steele, T.G.3
Crouthamel, M.-C.4
Pietrak, B.L.5
Lai, M.-T.6
Holloway, M.K.7
Munshi, S.K.8
Graham, S.L.9
Vacca, J.P.10
-
139
-
-
33746509102
-
2NH] reduced amide isosteres
-
2NH] reduced amide isosteres. Bioorg Med Chem Lett 2006;16:3635-3638.
-
(2006)
Bioorg Med Chem Lett
, vol.16
, pp. 3635-3638
-
-
Coburn, C.A.1
Stachel, S.J.2
Jones, K.J.3
Steele, T.J.4
Rush, D.M.5
Di Muzio, J.6
Pietrak, B.L.7
Lai, M.-T.8
Huang, Q.9
Lineberger, J.10
Jin, L.11
Munshi, S.12
Holloway, M.K.13
Espeseth, A.14
Simon, A.15
Hazuda, D.16
Graham, S.L.17
Vacca, J.P.18
-
140
-
-
33646152294
-
N-alkyl phenylacetamides beta-secretase inhibitors for treatment of Alzheimer's disease
-
Merck & Co. PCT Int Appl; WO2005004802
-
Coburn CA, Stachel SJ, Vacca JP. (Merck & Co.) N-alkyl phenylacetamides beta-secretase inhibitors for treatment of Alzheimer's disease. PCT Int Appl 2005; WO2005004802.
-
(2005)
-
-
Coburn, C.A.1
Stachel, S.J.2
Vacca, J.P.3
-
141
-
-
33750128392
-
Macrocyclic inhibitors of β-secretase: Functional activity in an animal model
-
Stachel SJ, Coburn CA, Sankaranarayanan S, Price EA, Pietrak BL, Huang Q, Lineberger J, Espeseth AS, Jin L, Ellis J, Holloway MK, Munshi S, Allison T, Hazuda D, Simon AJ, Graham SL, Vacca JP. Macrocyclic inhibitors of β-secretase: Functional activity in an animal model. J Med Chem 2006;49:6147-6150.
-
(2006)
J Med Chem
, vol.49
, pp. 6147-6150
-
-
Stachel, S.J.1
Coburn, C.A.2
Sankaranarayanan, S.3
Price, E.A.4
Pietrak, B.L.5
Huang, Q.6
Lineberger, J.7
Espeseth, A.S.8
Jin, L.9
Ellis, J.10
Holloway, M.K.11
Munshi, S.12
Allison, T.13
Hazuda, D.14
Simon, A.J.15
Graham, S.L.16
Vacca, J.P.17
-
142
-
-
33646153249
-
Preparation of macrocyclic β-secretase inhibitors for the treatment of Alzheimer's disease
-
Merck & Co. PCT Int Appl; WO2005018545
-
Coburn CA, Stachel SJ, Vacca JP. (Merck & Co.) Preparation of macrocyclic β-secretase inhibitors for the treatment of Alzheimer's disease. PCT Int Appl 2005; WO2005018545.
-
(2005)
-
-
Coburn, C.A.1
Stachel, S.J.2
Vacca, J.P.3
-
143
-
-
33846193320
-
Evaluating scoring functions for docking and designing β-secretase inhibitors
-
DOI 10.1016/j.bmcl.2006.10.051, PII S0960894X06012303
-
Holloway MK, McGaughey GB, Coburn CA, Stachel SJ, Jones KG, Stanton EL, Gregro AR, Lai M-T, Crouthamel M-C, Pietrak BL, Munshi SK. Evaluating scoring functions for docking and designing β-secretase inhibitors. Bioorg Med Chem
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.3
, pp. 823-827
-
-
Katharine Holloway, M.1
McGaughey, G.B.2
Coburn, C.A.3
Stachel, S.J.4
Jones, K.G.5
Stanton, E.L.6
Gregro, A.R.7
Lai, M.-T.8
Crouthamel, M.-C.9
Pietrak, B.L.10
Munshi, S.K.11
-
144
-
-
33847029846
-
Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind β-secretase in a N-terminal 10s-loop down conformation
-
DOI 10.1016/j.bmcl.2006.12.051, PII S0960894X06014478
-
Stauffer SR, Stanton MG, Gregro AG, Steinbeiser MA, Shaffer JR, Nantermet PG, Barrow JC, Rittle KE, Collusi D, Espeseth AS, Lai M-T, Pietrak BL, Holloway MK, McGaughey GB, Munshi SK, Hochman JH, Simon AJ, Selnick HG, Graham SL, Vacca JP. Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind β-secretase in a N-terminal 10s-loop down conformation. Bioorg Med Chem Lett 2007;17:1788-1792. (Pubitemid 46274326)
-
(2007)
Bioorganic and Medicinal Chemistry Letters
, vol.17
, Issue.6
, pp. 1788-1792
-
-
Stauffer, S.R.1
Stanton, M.G.2
Gregro, A.R.3
Steinbeiser, M.A.4
Shaffer, J.R.5
Nantermet, P.G.6
Barrow, J.C.7
Rittle, K.E.8
Collusi, D.9
Espeseth, A.S.10
Lai, M.-T.11
Pietrak, B.L.12
Holloway, M.K.13
McGaughey, G.B.14
Munshi, S.K.15
Hochman, J.H.16
Simon, A.J.17
Selnick, H.G.18
Graham, S.L.19
Vacca, J.P.20
more..
-
145
-
-
34547566031
-
Discovery of isonicotinamide derived β-secretase inhibitors: In vivo reduction of β-amyloid
-
DOI 10.1021/jm070272d
-
Stanton MG, Stauffer SR, Gregro AR, Steinbeiser M, Nantermet P, Sankaranarayanan S, Price EA, Wu G, Crouthamel M-C, Ellis J, Lai M-T, Espeseth AS, Shi X-P, Jin L, Colussi D, Pietrak B, Huang Q, Xu M, Simon AJ, Graham SL, Vacca JP, Selnick H. Discovery of isonicotinamide derived β-secretase inhibitors: in vivo reduction of β-amyloid. J Med Chem 2007;50:3431-3433. (Pubitemid 47195452)
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, Issue.15
, pp. 3431-3433
-
-
Stanton, M.G.1
Stauffer, S.R.2
Gregro, A.R.3
Steinbeiser, M.4
Nantermet, P.5
Sankaranarayanan, S.6
Price, E.A.7
Wu, G.8
Crouthamel, M.-C.9
Ellis, J.10
Lai, M.-T.11
Espeseth, A.S.12
Shi, X.-P.13
Jin, L.14
Colussi, D.15
Pietrak, B.16
Huang, Q.17
Xu, M.18
Simon, A.J.19
Graham, S.L.20
Vacca, J.P.21
Selnick, H.22
more..
-
146
-
-
66249101379
-
Preparation of 1,3,5-substituted phenyl derivatives containing five-membered heterocycles useful as β-secretase inhibitors for treatment of Alzheimer's disease
-
Merck & Co. PCT Int Appl; WO2005103020
-
Barrow JC, McGaughey GB, Nantermet PG, Rajapakse HA, Selnick HG, Stauffer SR, Coburn CA. (Merck & Co.) Preparation of 1,3,5-substituted phenyl derivatives containing five-membered heterocycles useful as β-secretase inhibitors for treatment of Alzheimer's disease. PCT Int Appl 2005; WO2005103020.
-
(2005)
-
-
Barrow, J.C.1
McGaughey, G.B.2
Nantermet, P.G.3
Rajapakse, H.A.4
Selnick, H.G.5
Stauffer, S.R.6
Coburn, C.A.7
-
147
-
-
66249092951
-
Preparation of amino oxadiazolyl pyridinil sulfonamides as β-secretase inhibitors for treatment of Alzheimer's disease
-
Merck & Co. PCT Int Appl; WO2005103043
-
Barrow JC, McGaughey GB, Nantermet PG, Rajapakse HA, Selnick HG, Stauffer SR, Shaun R, Vacca JP, Stachel SJ, Coburn CA, Stanton MG. (Merck & Co.) Preparation of amino oxadiazolyl pyridinil sulfonamides as β-secretase inhibitors for treatment of Alzheimer's disease. PCT Int Appl 2005; WO2005103043.
-
(2005)
-
-
Barrow, J.C.1
McGaughey, G.B.2
Nantermet, P.G.3
Rajapakse, H.A.4
Selnick, H.G.5
Stauffer, S.R.6
Shaun, R.7
Vacca, J.P.8
Stachel, S.J.9
Coburn, C.A.10
Stanton, M.G.11
-
148
-
-
66249106203
-
Preparation of 2-aminothiazole compounds as aspartyl protease inhibitors
-
Merck & Co. PCT Int Appl; WO200597767
-
Coburn CA, Espeseth AS, Stachel SJ, Olsen DB, Hazuda D, Holloway MK. (Merck & Co.) Preparation of 2-aminothiazole compounds as aspartyl protease inhibitors. PCT Int Appl 2005; WO200597767.
-
(2005)
-
-
Coburn, C.A.1
Espeseth, A.S.2
Stachel, S.J.3
Olsen, D.B.4
Hazuda, D.5
Holloway, M.K.6
-
149
-
-
33750187712
-
Preparation of phenylamides and pyridylamides as β-secretase inhibitors
-
Merck & Co. PCT Int Appl; WO2005065195
-
Barrow JC, Coburns CA, Nantermet PG, Selnick HG, Stachel SJ, Shawn J, Stanton MG, Stauffer SR, Zhuang L, Davis JR. (Merck & Co.) Preparation of phenylamides and pyridylamides as β-secretase inhibitors. PCT Int Appl 2005; WO2005065195.
-
(2005)
-
-
Barrow, J.C.1
Coburns, C.A.2
Nantermet, P.G.3
Selnick, H.G.4
Stachel, S.J.5
Shawn, J.6
Stanton, M.G.7
Stauffer, S.R.8
Zhuang, L.9
Davis, J.R.10
-
150
-
-
66249118850
-
Pyrrolidin-3-yl compounds, synthesis, pharmaceutical compositions and their use as β-secretase inhibitors for treatment of Alzheimer's disease
-
Merck&Co. PCT Int Appl; WO2006002004
-
Coburn CA. (Merck&Co.) Pyrrolidin-3-yl compounds, synthesis, pharmaceutical compositions and their use as β-secretase inhibitors for treatment of Alzheimer's disease. PCT Int Appl 2006; WO2006002004.
-
(2006)
-
-
Coburn, C.A.1
-
151
-
-
66249118850
-
Preparation of spiropiperidine compounds as β-secretase inhibitors for treatment of Alzheimer's disease
-
Merck & Co., and Sunesis Pharm. PCT Int Appl; WO2006044497
-
Barrow JC, Coburn CA, Egbertson MS, McGaughey GB, McWheter MA, Neilson LA, Selnick HG, Stauffer SR, Yang Z-Q, Yang W, Lu W, Fahr B, Rittle KE. (Merck & Co., and Sunesis Pharm.) Preparation of spiropiperidine compounds as β-secretase inhibitors for treatment of Alzheimer's disease. PCT Int Appl 2006; WO2006044497.
-
(2006)
-
-
Barrow, J.C.1
Coburn, C.A.2
Egbertson, M.S.3
McGaughey, G.B.4
McWheter, M.A.5
Neilson, L.A.6
Selnick, H.G.7
Stauffer, S.R.8
Yang, Z.-Q.9
Yang, W.10
Lu, W.11
Fahr, B.12
Rittle, K.E.13
-
152
-
-
66249118850
-
Preparation of aminopyridines as β-secretase inhibitors for treatment of Alzheimer's disease
-
Merck & Co. PCT Int Appl; WO2006060109
-
Coburn CA, Holloway MK, Stachel SJ. (Merck & Co.) Preparation of aminopyridines as β-secretase inhibitors for treatment of Alzheimer's disease. PCT Int Appl 2006; WO2006060109.
-
(2006)
-
-
Coburn, C.A.1
Holloway, M.K.2
Stachel, S.J.3
-
153
-
-
66249122925
-
Amino-methyl β-secretase inhibitors for treatment of Alzheimer's disease
-
Merck & Co. PCT Int Appl; WO2006078576
-
Coburn CA, Nantermet PG, Rajapakse HA, Selniuck HG, Stauffer SR. (Merck & Co.) Amino-methyl β-secretase inhibitors for treatment of Alzheimer's disease. PCT Int Appl 2006; WO2006078576.
-
(2006)
-
-
Coburn, C.A.1
Nantermet, P.G.2
Rajapakse, H.A.3
Selniuck, H.G.4
Stauffer, S.R.5
-
154
-
-
66249144856
-
Spiropiperidine as β-secretase inhibitors for treatment of Alzheimer's disease
-
Merck & Co., and Sunesis Pharm. PCT Int Appl; WO2007011810
-
Coburn CA, Egberston MS, Graham SL, Mcgaughey GB, Stauffer SR, Yang W, Lu W, Fahr B. (Merck & Co., and Sunesis Pharm.) Spiropiperidine as β-secretase inhibitors for treatment of Alzheimer's disease. PCT Int Appl 2007; WO2007011810.
-
(2007)
-
-
Coburn, C.A.1
Egberston, M.S.2
Graham, S.L.3
Mcgaughey, G.B.4
Stauffer, S.R.5
Yang, W.6
Lu, W.7
Fahr, B.8
-
155
-
-
66249121211
-
Spiropiperidine as β-secretase inhibitors for treatment of Alzheimer's disease β-secretase inhibitors for treatment of Alzheimer's disease
-
Merck & Co. and Sunesis Pharm. PCT Int Appl; WO2007011833
-
Coburn CA, Egberston MS, Graham SL, Mcgaughey GB, Stauffer SR, Rajapakse HA, Nantermet PG, Stachel SR, Yang W, Lu W, Fahr B. (Merck & Co. and Sunesis Pharm.) Spiropiperidine as β-secretase inhibitors for treatment of Alzheimer's disease β-secretase inhibitors for treatment of Alzheimer's disease. PCT Int Appl 2007; WO2007011833.
-
(2007)
-
-
Coburn, C.A.1
Egberston, M.S.2
Graham, S.L.3
Mcgaughey, G.B.4
Stauffer, S.R.5
Rajapakse, H.A.6
Nantermet, P.G.7
Stachel, S.R.8
Yang, W.9
Lu, W.10
Fahr, B.11
-
156
-
-
66249132501
-
Preparation of 2-hydroxy-1,3-diaminoalkanes including spiro substituted chroman derivatives as β-secretase modulators and their use for treatment Alzheimer's disease and related condition
-
Amgen Inc. PCT Int Appl; WO2007061930
-
Xue Q, Albrecht BK, Andersen DL, Bartberger M, Brown J, Brown R, Chaffee SC, Cheng Y, Croghanm M, Graceffa R, Harried S, Hitchcock S, Hungate R, Judd T, Kaller M, Kreiman C, La D, Lopez P, Masse CE, Monenschein H, Nguyen T, Nixwy T, Patel VF, Pennington L, Weiss M, Yang B, Zhong W. (Amgen Inc.) Preparation of 2-hydroxy-1,3-diaminoalkanes including spiro substituted chroman derivatives as β-secretase modulators and their use for treatment Alzheimer's disease and related condition. PCT Int Appl 2007; WO2007061930.
-
(2007)
-
-
Xue, Q.1
Albrecht, B.K.2
Andersen, D.L.3
Bartberger, M.4
Brown, J.5
Brown, R.6
Chaffee, S.C.7
Cheng, Y.8
Croghanm, M.9
Graceffa, R.10
Harried, S.11
Hitchcock, S.12
Hungate, R.13
Judd, T.14
Kaller, M.15
Kreiman, C.16
La, D.17
Lopez, P.18
Masse, C.E.19
Monenschein, H.20
Nguyen, T.21
Nixwy, T.22
Patel, V.F.23
Pennington, L.24
Weiss, M.25
Yang, B.26
Zhong, W.27
more..
-
157
-
-
66249132501
-
Preparation of 2-hydroxy-1,3-diaminoalkanes including spiro substituted chroman derivatives as β-secretase modulators and their use for treatment Alzheimer's disease and related condition
-
Amgen Inc. PCT Int Appl; WO2007062007
-
Albrecht BK, Andersen DL, Bartberger M, Brown J, Brown R, Chaffee SC, Cheng Y, Croghan M, Graceffa R, Harried S, Hitchcock S, Hungate R, Judd T, Kaller M, Kreiman C, La D, Lopez P, Masse CE, Monenschein H, Nguyen T, Nixey T, Patel VF, Pennington L, Weiss M, Xue Q, Yang B, Zhong W. (Amgen Inc.) Preparation of 2-hydroxy-1,3-diaminoalkanes including spiro substituted chroman derivatives as β-secretase modulators and their use for treatment Alzheimer's disease and related condition. PCT Int Appl 2007; WO2007062007.
-
(2007)
-
-
Albrecht, B.K.1
Andersen, D.L.2
Bartberger, M.3
Brown, J.4
Brown, R.5
Chaffee, S.C.6
Cheng, Y.7
Croghan, M.8
Graceffa, R.9
Harried, S.10
Hitchcock, S.11
Hungate, R.12
Judd, T.13
Kaller, M.14
Kreiman, C.15
La, D.16
Lopez, P.17
Masse, C.E.18
Monenschein, H.19
Nguyen, T.20
Nixey, T.21
Patel, V.F.22
Pennington, L.23
Weiss, M.24
Xue, Q.25
Yang, B.26
Zhong, W.27
more..
-
158
-
-
66249094010
-
Preparation of 2-hydroxy-1,3-diaminoalkanes including spiro substituted chroman derivatives as β-secretase modulators and their use for treatment Alzheimer's disease and related condition
-
Amgen Inc. PCT Int Appl; WO2007061670
-
Zhong W, Hitchcock S, Albrecht BK, Bartberger M, Brown J, Brown R, Chaffee SC, Cheng Y, Croghan M, Graceffa R, Harried S, Hickman D, Horne D, Hungate R, Judd T, Kaller M, Kreiman C, La D, Lopez P, Masse CE, Monenschein H, Nguyen T, Nixey T, Patel VF, Pennington L, Weiss M, Xue Q,Yang B. (Amgen Inc.) Preparation of 2-hydroxy-1,3-diaminoalkanes including spiro substituted chroman derivatives as β-secretase modulators and their use for treatment Alzheimer's disease and related condition. PCT Int Appl 2007; WO2007061670.
-
(2007)
-
-
Zhong, W.1
Hitchcock, S.2
Albrecht, B.K.3
Bartberger, M.4
Brown, J.5
Brown, R.6
Chaffee, S.C.7
Cheng, Y.8
Croghan, M.9
Graceffa, R.10
Harried, S.11
Hickman, D.12
Horne, D.13
Hungate, R.14
Judd, T.15
Kaller, M.16
Kreiman, C.17
La, D.18
Lopez, P.19
Masse, C.E.20
Monenschein, H.21
Nguyen, T.22
Nixey, T.23
Patel, V.F.24
Pennington, L.25
Weiss, M.26
Xue, Q.27
Yang, B.28
more..
-
159
-
-
33750875336
-
Hydroxyethylene compounds with Asp-2 inhibitory activity
-
Smithkline Beecham P.L.C. PCT Int Appl; WO2003045903
-
Faller A, Milner PH, Waard JG. (Smithkline Beecham P.L.C.) Hydroxyethylene compounds with Asp-2 inhibitory activity. PCT Int Appl 2003; WO2003045903.
-
(2003)
-
-
Faller, A.1
Milner, P.H.2
Waard, J.G.3
-
160
-
-
66249111999
-
Preparation of benzamide derivatives as inhibitors of Asp-2
-
Smithkline Beecham P.L.C. PCT Int Appl; WO2003045913
-
Faller A, MacPherson DT, Milner PH, Stanway SJ, Trow LS. (Smithkline Beecham P.L.C.) Preparation of benzamide derivatives as inhibitors of Asp-2. PCT Int Appl 2003; WO2003045913.
-
(2003)
-
-
Faller, A.1
MacPherson, D.T.2
Milner, P.H.3
Stanway, S.J.4
Trow, L.S.5
-
161
-
-
21244432534
-
Preparation of hydroxyethylamine derivatives for the treatment of Alzheimer's disease
-
Glaxo Group Ltd. PCT Int Appl; WO2004050619
-
Demont EH, Faller A, MacPherson DT, Milner PH, Naylor AR, Redshaw S, Stanway SJ,Vesey DR, Walter DR. (Glaxo Group Ltd) Preparation of hydroxyethylamine derivatives for the treatment of Alzheimer's disease. PCT Int Appl 2004; WO2004050619.
-
(2004)
-
-
Demont, E.H.1
Faller, A.2
MacPherson, D.T.3
Milner, P.H.4
Naylor, A.R.5
Redshaw, S.6
Stanway, S.J.7
Vesey, D.R.8
Walter, D.R.9
-
162
-
-
66249104135
-
Preparation of tricyclic indole hydroxyethylamine derivatives and their use in the treatment of Alzheimer's disease
-
Glaxo Group Ltd. PCT Int Appl; WO2005058615
-
Redshaw S, Demont EH, Walter DS. (Glaxo Group Ltd) Preparation of tricyclic indole hydroxyethylamine derivatives and their use in the treatment of Alzheimer's disease. PCT Int Appl 2005; WO2005058615.
-
(2005)
-
-
Redshaw, S.1
Demont, E.H.2
Walter, D.S.3
-
163
-
-
66249095804
-
Preparation of 3-(1,1-dioxotetrahydro-1, 2-thiazin-2-yl) or 3-(1,1-dioxoisothiazolidin-2-yl) benzamido compounds for treatment of Alzheimer's disease
-
Glaxo Group Ltd. PCT Int Appl; WO2004111022
-
Demont EH, Redshaw S, Walter DS. (Glaxo Group Ltd) Preparation of 3-(1,1-dioxotetrahydro-1, 2-thiazin-2-yl) or 3-(1,1-dioxoisothiazolidin-2-yl) benzamido compounds for treatment of Alzheimer's disease. PCT Int Appl 2004; WO2004111022.
-
(2004)
-
-
Demont, E.H.1
Redshaw, S.2
Walter, D.S.3
-
164
-
-
21244432534
-
Preparation of hydroxyethylamine derivatives for the treatment of Alzheimer's disease
-
Glaxo Group Ltd. PCT Int Appl; WO2004080376
-
Demont EH, Redshaw S, Walter DS. (Glaxo Group Ltd) Preparation of hydroxyethylamine derivatives for the treatment of Alzheimer's disease. PCT Int Appl 2004; WO2004080376.
-
(2004)
-
-
Demont, E.H.1
Redshaw, S.2
Walter, D.S.3
-
165
-
-
33646130110
-
Preparation of hydroxydiaminopropyl tricyclic indolecarboxamides for treatment of β-amiloid related disease
-
Glaxo Group Ltd. PCT Int Appl; WO2004094430
-
Demont EH, Redshaw S, Walter DS. (Glaxo Group Ltd) Preparation of hydroxydiaminopropyl tricyclic indolecarboxamides for treatment of β-amiloid related disease. PCT Int Appl 2004; WO2004094430.
-
(2004)
-
-
Demont, E.H.1
Redshaw, S.2
Walter, D.S.3
-
166
-
-
66249089668
-
Preparation of N,N′-substituted-1,3-diamino-2-oxopropane derivatives as Asp2 inhibitors for use against diseases characterized by elevated β-amyloid deposits, particularly Alzheimer's disease
-
Glaxo Group Ltd. PCT Int Appl; WO2005113525
-
Demont EH, Redshaw S,Walter DS. (Glaxo Group Ltd) Preparation of N,N′-substituted-1,3-diamino-2-oxopropane derivatives as Asp2 inhibitors for use against diseases characterized by elevated β-amyloid deposits, particularly Alzheimer's disease. PCT Int Appl 2005; WO2005113525.
-
(2005)
-
-
Demont, E.H.1
Redshaw, S.2
Walter, D.S.3
-
167
-
-
66249091044
-
Tricyclic indole derivatives for use in the treatment of Alzheimer's disease
-
Glaxo Group Ltd. PCT Int Appl; WO2006040148
-
Demont EH, Redshaw S, Walter DS. (Glaxo Group Ltd) Tricyclic indole derivatives for use in the treatment of Alzheimer's disease. PCT Int Appl 2006; WO2006040148.
-
(2006)
-
-
Demont, E.H.1
Redshaw, S.2
Walter, D.S.3
-
168
-
-
66249147726
-
Heterocyclic ketone compounds for treating Alzheimer's disease
-
Glaxo Group Ltd. PCT Int Appl; WO2006040149
-
Demont EH, Redshaw S, Walter DS. (Glaxo Group Ltd) Heterocyclic ketone compounds for treating Alzheimer's disease. PCT Int Appl 2006; WO2006040149.
-
(2006)
-
-
Demont, E.H.1
Redshaw, S.2
Walter, D.S.3
-
169
-
-
66249134755
-
Novel hydroxyethylamine and ketone compounds having Asp2 inhibitory activity
-
Glaxo Group Ltd. PCT Int Appl; WO2006103088
-
Demont EH, Redshaw S, Walter DS. (Glaxo Group Ltd) Novel hydroxyethylamine and ketone compounds having Asp2 inhibitory activity. PCT Int Appl 2006; WO2006103088.
-
(2006)
-
-
Demont, E.H.1
Redshaw, S.2
Walter, D.S.3
-
170
-
-
66249101805
-
Preparation of novel α-amino-γ-lactams as β-secretase inhibitors
-
Bristol-Myers Squibb Co. PCT Int Appl; WO2004013098
-
Decicco CP, Tebben AJ, Thompson LA, Combs AP. (Bristol-Myers Squibb Co.) Preparation of novel α-amino-γ-lactams as β-secretase inhibitors. PCT Int Appl 2004; WO2004013098.
-
(2004)
-
-
Decicco, C.P.1
Tebben, A.J.2
Thompson, L.A.3
Combs, A.P.4
-
171
-
-
66249129185
-
Preparation of (succinylamino)azepinones as inhibitors of Aβ protein
-
Bristol-Myers Squibb Co. US Pat Appl; US6794381
-
Olson RE, Maduskuie TP, Thompson LA. (Bristol-Myers Squibb Co.) Preparation of (succinylamino)azepinones as inhibitors of Aβ protein. US Pat Appl 2004; US6794381.
-
(2004)
-
-
Olson, R.E.1
Maduskuie, T.P.2
Thompson, L.A.3
-
172
-
-
66249104137
-
Preparation of succinoylaminobenzodiazepines as inhibitors of Aβ protein production for treating neurological disorders
-
Bristol-Myers Squibb Co. US Pat Appl; US7053084
-
Olson RE. (Bristol-Myers Squibb Co.) Preparation of succinoylaminobenzodiazepines as inhibitors of Aβ protein production for treating neurological disorders. US Pat Appl 2006; US7053084.
-
(2006)
-
-
Olson, R.E.1
-
173
-
-
66249088859
-
Preparation of isophthalates as β-secretase inhibitors
-
Bristol-Myers Squibb Co. PCT Int Appl; WO2006099352
-
Thompson ILA, Boy KM,Shi JM, Macor JE. (Bristol-Myers Squibb Co.) Preparation of isophthalates as β-secretase inhibitors . PCT Int Appl 2006; WO2006099352.
-
(2006)
-
-
Thompson, I.L.A.1
Boy, K.M.2
Shi, J.M.3
Macor, J.E.4
-
174
-
-
66249121556
-
Preparation of indoleacetic acid acyl guanidines as β-secretase (BACE) inhibitors
-
Bristol-Myers Squibb Co. US Pat Appl; US2007049589
-
Thompson LA, Shi J, Zusi FC, Dee MF, Macor JE. (Bristol-Myers Squibb Co.) Preparation of indoleacetic acid acyl guanidines as β-secretase (BACE) inhibitors. US Pat Appl 2007; US2007049589.
-
(2007)
-
-
Thompson, L.A.1
Shi, J.2
Zusi, F.C.3
Dee, M.F.4
Macor, J.E.5
-
175
-
-
66249119843
-
Preparation of isoxazolylcarbonyl- and isothiazolyl-carbonylguanidines as β-secretase (BACE)
-
Bristol-Myers Squibb Co. PCT Int Appl; WO2007002214
-
Gerritz S, Zhai W, Shi S, Zhu S, Good AC, Thompson LA III. (Bristol-Myers Squibb Co.) Preparation of isoxazolylcarbonyl- and isothiazolyl- carbonylguanidines as β-secretase (BACE). PCT Int Appl 2007; WO2007002214.
-
(2007)
-
-
Gerritz, S.1
Zhai, W.2
Shi, S.3
Zhu, S.4
Good, A.C.5
Thompson III, L.A.6
-
176
-
-
84907933410
-
Diphenylimidazopyrimidine and imidazole amine as inhibitors of β-secretase
-
Wyeth, John & Br. US Pat Appl; US20050282826
-
Malamas MS, Erdei JJ, Gunawan IS, Barnes KD, Johnson MR, Hui Y. (Wyeth, John & Br.) Diphenylimidazopyrimidine and imidazole amine as inhibitors of β-secretase. US Pat Appl 2005; US20050282826.
-
(2005)
-
-
Malamas, M.S.1
Erdei, J.J.2
Gunawan, I.S.3
Barnes, K.D.4
Johnson, M.R.5
Hui, Y.6
-
177
-
-
66249127734
-
Amino-imidazolones for the inhibition of β-secretase
-
Wyeth, John & Br. PCT Int Appl; WO2006076284
-
Malamas MS, Erdei JJ, Nawan IS, Npwak P, Harrison BL. (Wyeth, John & Br.) Amino-imidazolones for the inhibition of β-secretase. PCT Int Appl 2006; WO2006076284.
-
(2006)
-
-
Malamas, M.S.1
Erdei, J.J.2
Nawan, I.S.3
Npwak, P.4
Harrison, B.L.5
-
178
-
-
77249122570
-
Amino 5,5-diphenylimidazolone derivatives for the inhibition of β-secretase
-
Wyeth, John & Br. PCT Int Appl; WO2006009653
-
Malamas MS, Erdei JJ, Gunawan IS, Zhou P, Yan Y, Quagliato DA. (Wyeth, John & Br.) Amino 5,5-diphenylimidazolone derivatives for the inhibition of β-secretase. PCT Int Appl 2006; WO2006009653.
-
(2006)
-
-
Malamas, M.S.1
Erdei, J.J.2
Gunawan, I.S.3
Zhou, P.4
Yan, Y.5
Quagliato, D.A.6
-
179
-
-
66249143922
-
Amino-pyridines as inhibitors of β-secretase
-
Wyeth, John & Br. PCT Int Appl; WO2006083760
-
Malamas MS, Fobare WF, Solvibile WR, Lovering FE, Condon JS, Robichaud AJ. (Wyeth, John & Br.) Amino-pyridines as inhibitors of β-secretase. PCT Int Appl 2006; WO2006083760.
-
(2006)
-
-
Malamas, M.S.1
Fobare, W.F.2
Solvibile, W.R.3
Lovering, F.E.4
Condon, J.S.5
Robichaud, A.J.6
-
180
-
-
33750132225
-
Acylguanidines as small-molecule β-secretase inhibitors
-
DOI 10.1021/jm0607451
-
Cole DC, Manas ES, Stock JR, Condon JS, Jennings LD, Aulabaugh A, Chopra R, Cowling R, Ellingboe JW, Fan KY, Harrison BL, Hu Y, Jacobsen S, Jin G, Lin L, Lovering FE, Malamas MS, Stahl ML, Strand J, Sukhdeo MN, Svenson K, Turner MJ, Wagner E, Wu J, Zhou P, Bard J. Acylguanidines as small-molecule β-Secretase inhibitors. J Med Chem 2006;49:6158-6161. (Pubitemid 44595192)
-
(2006)
Journal of Medicinal Chemistry
, vol.49
, Issue.21
, pp. 6158-6161
-
-
Cole, D.C.1
Manas, E.S.2
Stock, J.R.3
Condon, J.S.4
Jennings, L.D.5
Aulabaugh, A.6
Chopra, R.7
Cowling, R.8
Ellingboe, J.W.9
Fan, K.Y.10
Harrison, B.L.11
Hu, Y.12
Jacobsen, S.13
Jin, G.14
Lin, L.15
Lovering, F.E.16
Malamas, M.S.17
Stahl, M.L.18
Strand, J.19
Sukhdeo, M.N.20
Svenson, K.21
Turner, M.J.22
Wagner, E.23
Wu, J.24
Zhou, P.25
Bard, J.26
more..
-
181
-
-
66249113000
-
Preparation of azolylacylguanidines as β-secretase inhibitors
-
Wyeth, John & Br. PCT Int Appl; WO2006088711
-
Cole DC, Manas ES, Jennigs LD, Lovering FE, Stock JR, Moore WJ, Ellingboe JW, Condon JS, Sukhdeo MN, Zhou P, Wu J, Morris KM. (Wyeth, John & Br.) Preparation of azolylacylguanidines as β-secretase inhibitors. PCT Int Appl 2006; WO2006088711.
-
(2006)
-
-
Cole, D.C.1
Manas, E.S.2
Jennigs, L.D.3
Lovering, F.E.4
Stock, J.R.5
Moore, W.J.6
Ellingboe, J.W.7
Condon, J.S.8
Sukhdeo, M.N.9
Zhou, P.10
Wu, J.11
Morris, K.M.12
-
182
-
-
66249138303
-
Substituted thienyl and furyl acylguanidines as β-secretase modulators
-
Wyeth, John & Br. PCT Int Appl; WO2006088694
-
Fobare WF, Solvibile WR. (Wyeth, John & Br.) Substituted thienyl and furyl acylguanidines as β-secretase modulators. PCT Int Appl 2006; WO2006088694.
-
(2006)
-
-
Fobare, W.F.1
Solvibile, W.R.2
-
183
-
-
66249102809
-
Terphenyl acylguanidines as β-secretase modulators
-
Wyeth, John & Br. PCT Int Appl; WO2006088705
-
Baihua HU. (Wyeth, John & Br.) Terphenyl acylguanidines as β-secretase modulators. PCT Int Appl 2006; WO2006088705.
-
(2006)
-
-
Baihua, H.U.1
-
184
-
-
64349121143
-
Preparation of substituted 2-aminopyrimidin- 4-ones for treating or preventing Aβ-related pathologies
-
AstraZeneca AB and Astex Ther. PCT Int Appl; WO2006041404 and 2006; WO2006041405
-
Albert JS, Andrisk D, Arnold J, Brown D, Callaghan O, Campbell J, Carr RAE, Chessari G, Congreve MS, Edwards P, Empfield JR, Frederickson M, Koether GM, Krumrine J, Mauger R, Murray CW, Patel S, Sylvester M, Throner S. (AstraZeneca AB and Astex Ther.) Preparation of substituted 2-aminopyrimidin- 4-ones for treating or preventing Aβ-related pathologies. PCT Int Appl 2006; WO2006041404 and 2006; WO2006041405.
-
(2006)
-
-
Albert, J.S.1
Andrisk, D.2
Arnold, J.3
Brown, D.4
Callaghan, O.5
Campbell, J.6
Carr, R.A.E.7
Chessari, G.8
Congreve, M.S.9
Edwards, P.10
Empfield, J.R.11
Frederickson, M.12
Koether, G.M.13
Krumrine, J.14
Mauger, R.15
Murray, C.W.16
Patel, S.17
Sylvester, M.18
Throner, S.19
-
185
-
-
64349121143
-
Preparation of substituted 2-aminopyrimidin-4-ones for treating or preventing Aβ-related pathologies
-
AstraZeneca AB and Astex Ther. PCT Int Appl; WO2007058582
-
Albert J, Edwards P, Empfield J. (AstraZeneca AB and Astex Ther.) Preparation of substituted 2-aminopyrimidin-4-ones for treating or preventing Aβ-related pathologies. PCT Int Appl 2007; WO2007058582.
-
(2007)
-
-
Albert, J.1
Edwards, P.2
Empfield, J.3
-
186
-
-
64349121143
-
Preparation of substituted 2-aminopyrimidin-4-ones for treating or preventing Aβ-related pathologies
-
AstraZeneca AB and Astex Ther. PCT Int Appl; WO2007058580
-
Albert J, Andisik D, Edwards P, Sylvester M. (AstraZeneca AB and Astex Ther.) Preparation of substituted 2-aminopyrimidin-4-ones for treating or preventing Aβ-related pathologies. PCT Int Appl 2007; WO2007058580.
-
(2007)
-
-
Albert, J.1
Andisik, D.2
Edwards, P.3
Sylvester, M.4
-
187
-
-
64349121143
-
Preparation of substituted 2- aminopyrimidines for treating or preventing Aβ-related pathologies
-
AstraZeneca AB and Astex Ther. PCT Int Appl; WO2007058581
-
Albert J, Chessari G, Edwards P. (AstraZeneca AB and Astex Ther.) Preparation of substituted 2- aminopyrimidines for treating or preventing Aβ-related pathologies. PCT Int Appl 2007; WO2007058581.
-
(2007)
-
-
Albert, J.1
Chessari, G.2
Edwards, P.3
-
188
-
-
66249147730
-
Preparation of 2-aminoimidazole-4-ones for treatment of cognitive impairment, Alzheimer's disease, neurodegeneration and dementia
-
AstraZeneca AB and Astex Ther. PCT Int Appl; WO2007058601
-
Albert J, Arnold J, Chessari G, Congreve MS, Edwards P, Murrai C, Patel S. (AstraZeneca AB and Astex Ther.) Preparation of 2-aminoimidazole-4-ones for treatment of cognitive impairment, Alzheimer's disease, neurodegeneration and dementia. PCT Int Appl 2007; WO2007058601.
-
(2007)
-
-
Albert, J.1
Arnold, J.2
Chessari, G.3
Congreve, M.S.4
Edwards, P.5
Murrai, C.6
Patel, S.7
-
189
-
-
66249109766
-
New 2-amino-3,5-dihydro-4Himidazol- 4-one derivatives and their use as BACE inhibitors for treatment cognitive impairment, Alzheimer's disease, neurodegeneration and dementia
-
AstraZeneca AB. PCT Int Appl; WO2007058602
-
Berg S, Burrows J, Chessari G, Congreve MS, Hedstroem J, Hellberg S, Hoegdin K, Kihlstroem J, Kolmodin K, Lindstroem J, Murray C, Patel S. (AstraZeneca AB) New 2-amino-3,5-dihydro-4Himidazol- 4-one derivatives and their use as BACE inhibitors for treatment cognitive impairment, Alzheimer's disease, neurodegeneration and dementia. PCT Int Appl 2007; WO2007058602.
-
(2007)
-
-
Berg, S.1
Burrows, J.2
Chessari, G.3
Congreve, M.S.4
Hedstroem, J.5
Hellberg, S.6
Hoegdin, K.7
Kihlstroem, J.8
Kolmodin, K.9
Lindstroem, J.10
Murray, C.11
Patel, S.12
-
190
-
-
66249122924
-
Preparation of dihydroisoquinolin-1-amines for treating or preventing Aβ-related pathologies, such as cognitive impairment, Alzheimer's disease, neurodegeneration and dementia
-
AstraZeneca AB and Astex Ther. PCT Int Appl; WO2007058583
-
Albert J, Chessari G, Congreve MS, Edwards P, Murray C, Patel S, Sylvester M. (AstraZeneca AB and Astex Ther.) Preparation of dihydroisoquinolin-1-amines for treating or preventing Aβ-related pathologies, such as cognitive impairment, Alzheimer's disease, neurodegeneration and dementia. PCT Int Appl 2007; WO2007058583.
-
(2007)
-
-
Albert, J.1
Chessari, G.2
Congreve, M.S.3
Edwards, P.4
Murray, C.5
Patel, S.6
Sylvester, M.7
-
191
-
-
66249085368
-
Novel 2-aminoquinazoline derivatives, their preparation and use as inhibitors of β-secretase for treating Alzheimer's disease and related disorders
-
Janssen Pharm. PCT Int Appl; WO2006017844
-
Baxter E, Boyd R, Coats S, Jordan A, Reitz A, Reynolds CH, Scott M, Schulz M, DeWinter HLJ. (Janssen Pharm.) Novel 2-aminoquinazoline derivatives, their preparation and use as inhibitors of β-secretase for treating Alzheimer's disease and related disorders. PCT Int Appl 2006; WO2006017844.
-
(2006)
-
-
Baxter, E.1
Boyd, R.2
Coats, S.3
Jordan, A.4
Reitz, A.5
Reynolds, C.H.6
Scott, M.7
Schulz, M.8
DeWinter, H.L.J.9
-
192
-
-
66249085368
-
Novel 2 - Aminoquinazoline derivatives, their preparation and use as inhibitors of β-secretase for treating Alzheimer's disease and related disorders
-
Janssen Pharm. PCT Int Appl; WO2006017836
-
Baxter E, Bischoff FP, Braeken M, Coats S, Huang Y, Jordan A, Luo C, Mercken MH, Reynolds CH, Ross TM, Tounge BA, Schulz M, De Winte HLJ, Pieters SMA, Reitz AB. (Janssen Pharm.) Novel 2 - aminoquinazoline derivatives, their preparation and use as inhibitors of β-secretase for treating Alzheimer's disease and related disorders. PCT Int Appl 2006; WO2006017836.
-
(2006)
-
-
Baxter, E.1
Bischoff, F.P.2
Braeken, M.3
Coats, S.4
Huang, Y.5
Jordan, A.6
Luo, C.7
Mercken, M.H.8
Reynolds, C.H.9
Ross, T.M.10
Tounge, B.A.11
Schulz, M.12
De Winte, H.L.J.13
Pieters, S.M.A.14
Reitz, A.B.15
-
193
-
-
66249085368
-
Novel 2 -aminoquinazoline derivatives, their preparation and use as inhibitors of β-secretase for treating Alzheimer's disease and related disorders
-
Janssen Pharm. PCT Int Appl; WO2006024932
-
Bishoff FP, Bracken M, Pieters SMA, Mercken MH, De Winter HLJ, Berthelot DJ-C. (Janssen Pharm.) Novel 2 -aminoquinazoline derivatives, their preparation and use as inhibitors of β-secretase for treating Alzheimer's disease and related disorders. PCT Int Appl 2006; WO2006024932.
-
(2006)
-
-
Bishoff, F.P.1
Bracken, M.2
Pieters, S.M.A.3
Mercken, M.H.4
De Winter, H.L.J.5
Berthelot, D.J.-C.6
-
194
-
-
66249083643
-
Preparation of 2-amino-3,4-dihydropyrido[3,4-d]pyrimidines as inhibitors of β-secretase (BACE)
-
Janssen Pharm. PCT Int Appl; WO2007050612
-
Reitz AB, Luo C, Huang Y, Ross TM, Baxter EE, Tounge BA, Parker MH, Strobel ED, Reynolds CH. (Janssen Pharm.) Preparation of 2-amino-3,4- dihydropyrido[3,4-d]pyrimidines as inhibitors of β-secretase (BACE). PCT Int Appl 2007; WO2007050612.
-
(2007)
-
-
Reitz, A.B.1
Luo, C.2
Huang, Y.3
Ross, T.M.4
Baxter, E.E.5
Tounge, B.A.6
Parker, M.H.7
Strobel, E.D.8
Reynolds, C.H.9
-
195
-
-
34548510854
-
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
-
DOI 10.1021/jm0705408
-
Baxter EW, Conway KA, Kennis L, Bischoff F, Mercken MH, DeWinter HL, Reynolds CH, Tounge BA, Luo C, Scott MK, Huang Y, Braeken M, Pieters SMA, Berthelot DJC, Masure S, Bruinzeel WD, Jordan AD, Parker MH, Boyd RE, Qu J, Alexander RS, Brenneman DE, Reitz B. (Johnson & Johnson Pharm.) 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. J Med Chem 2007;50:4261-4264. (Pubitemid 47378825)
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, Issue.18
, pp. 4261-4264
-
-
Baxter, E.W.1
Conway, K.A.2
Kennis, L.3
Bischoff, F.4
Mercken, M.H.5
De Winter, H.L.6
Reynolds, C.H.7
Tounge, B.A.8
Luo, C.9
Scott, M.K.10
Huang, Y.11
Braeken, M.12
Pieters, S.M.A.13
Berthelot, D.J.C.14
Masure, S.15
Bruinzeel, W.D.16
Jordan, A.D.17
Parker, M.H.18
Boyd, R.E.19
Qu, J.20
Alexander, R.S.21
Brenneman, D.E.22
Reitz, A.B.23
more..
-
196
-
-
66249105172
-
Preparation of amides as BACE inhibitors for treating Alzheimer's
-
Eli Lilly & Co. PCT Int Appl; WO2005108391
-
Bueno Melendo AB, Chen S-H, Erickson JA, Gonzalez-Garcia MR, Guo D, Marcos Llorente A, McCarthy JR, Shepherd TA, Sheehan SM, Yip YYM. (Eli Lilly & Co.) Preparation of amides as BACE inhibitors for treating Alzheimer's. PCT Int Appl 2005; WO2005108391.
-
(2005)
-
-
Bueno Melendo, A.B.1
Chen, S.-H.2
Erickson, J.A.3
Gonzalez-Garcia, M.R.4
Guo, D.5
Marcos Llorente, A.6
McCarthy, J.R.7
Shepherd, T.A.8
Sheehan, S.M.9
Yip, Y.Y.M.10
-
197
-
-
66249107222
-
Preparation of acylated 2-amino-1-(pyrrolidin-2-yl)ethanols and derivatives as BACE inhibitors for treating Alzheimer's
-
Eli Lilly & Co. PCT Int Appl; WO2005108358
-
Dally RD, Shepherd TAB, David M, Rojo Garcia MI. (Eli Lilly & Co.) Preparation of acylated 2-amino-1-(pyrrolidin-2-yl)ethanols and derivatives as BACE inhibitors for treating Alzheimer's. PCT Int Appl 2005; WO2005108358.
-
(2005)
-
-
Dally, R.D.1
Shepherd, T.A.B.2
David, M.3
Rojo Garcia, M.I.4
-
198
-
-
33845495249
-
Preparation of acylated 2-amino-1-(morpholin-3-yl)ethanols and derivatives as BACE inhibitors for treating Alzheimer's
-
Eli Lilly & Co. PCT Int Appl; WO2006034093
-
Durham TB, Hahn PJ, Kohn TJ, McCarthy JR, Broughton HB, Dally RD, Gonzalez-Garcia MR, Henry KJ Jr, Shepherd TA, Erickson JA, Ana B. (Eli Lilly & Co.) Preparation of acylated 2-amino-1-(morpholin-3-yl)ethanols and derivatives as BACE inhibitors for treating Alzheimer's. PCT Int Appl 2006; WO2006034093.
-
(2006)
-
-
Durham, T.B.1
Hahn, P.J.2
Kohn, T.J.3
McCarthy, J.R.4
Broughton, H.B.5
Dally, R.D.6
Gonzalez-Garcia, M.R.7
Henry Jr., K.J.8
Shepherd, T.A.9
Erickson, J.A.10
Ana, B.11
-
199
-
-
33646140084
-
A preparation of dibenz[b,f]oxepincarboxamide derivatives, useful for the treatment of neurological and vascular disorders related to β-amyloid generation and aggregation
-
Novartis AG and Novartis Pharma PCT Int Appl; WO2005014517
-
Auberson Y, Betschart C, Flohr S, Glatthar R, Simic O, Tintelnot-Blomley M, Troxler TJ, Vangrevelinghe E, Veenstra SJ. (Novartis AG and Novartis Pharma) A preparation of dibenz[b,f]oxepincarboxamide derivatives, useful for the treatment of neurological and vascular disorders related to β-amyloid generation and aggregation. PCT Int Appl 2005; WO2005014517.
-
(2005)
-
-
Auberson, Y.1
Betschart, C.2
Flohr, S.3
Glatthar, R.4
Simic, O.5
Tintelnot-Blomley, M.6
Troxler, T.J.7
Vangrevelinghe, E.8
Veenstra, S.J.9
-
200
-
-
66249133770
-
Preparation of substituted spirocyclic lactams as inhibitors of proteinase BACE1
-
Novartis AG and Norvatis Pharma. PCT Int Appl; WO2005035535
-
Auberson Y, Glatthar R, Salter R, Simic O, Tintelnot-Blomley M. (Novartis AG and Norvatis Pharma) Preparation of substituted spirocyclic lactams as inhibitors of proteinase BACE1. PCT Int Appl 2005; WO2005035535.
-
(2005)
-
-
Auberson, Y.1
Glatthar, R.2
Salter, R.3
Simic, O.4
Tintelnot-Blomley, M.5
-
201
-
-
33646141113
-
Preparation of macrocyclic lactams for treatment of neurological or vascular disorders related to β-amyloid generation and/or aggregation
-
Novartis AG and Novartis Pharma. PCT Int Appl; WO2005049585
-
Auberson Y, Betschart C, Glatthar R, Laumen K, Machauer R, Tintelnot-Blomley M, Troxler TJ, Veenstra SJ. Novartis AG and Novartis Pharma) Preparation of macrocyclic lactams for treatment of neurological or vascular disorders related to β-amyloid generation and/or aggregation. PCT Int Appl 2005; WO2005049585.
-
(2005)
-
-
Auberson, Y.1
Betschart, C.2
Glatthar, R.3
Laumen, K.4
Machauer, R.5
Tintelnot-Blomley, M.6
Troxler, T.J.7
Veenstra, S.J.8
-
202
-
-
66249123425
-
Preparation of macrocyclic compounds as BACE inhibitors for treating vascular and neurological disorders related to β-amyloid generation
-
Novartis AG and Novartis Pharma. PCT Int Appl; WO2006074940
-
Lerchner A, Machauer R, Simic O, Tintelnot-Blomley M. (Novartis AG and Novartis Pharma) Preparation of macrocyclic compounds as BACE inhibitors for treating vascular and neurological disorders related to β-amyloid generation. PCT Int Appl 2006; WO2006074940.
-
(2006)
-
-
Lerchner, A.1
Machauer, R.2
Simic, O.3
Tintelnot-Blomley, M.4
-
203
-
-
66249116142
-
Macrocyclic compounds useful as BACE inhibitors
-
Novartis AG and Novartis Pharma. PCT Int Appl; WO2007077004
-
Betschart C, Koller M, Laumen K, Lerchner A, Machauer R, McCarthy C, Tintelnot-Blomley M, Veenstra SJ. (Novartis AG and Novartis Pharma) Macrocyclic compounds useful as BACE inhibitors. PCT Int Appl 2007; WO2007077004.
-
(2007)
-
-
Betschart, C.1
Koller, M.2
Laumen, K.3
Lerchner, A.4
Machauer, R.5
McCarthy, C.6
Tintelnot-Blomley, M.7
Veenstra, S.J.8
-
204
-
-
33947612966
-
Application of fragment screening by X-ray crystallography to β-secretase
-
DOI 10.1021/jm0611962
-
Murray CW, Callaghan O, Chessari C, Cleasby A, Congreve M, Frederickson M, Hartshorn MJ, McMenamin R, Patel S, Wallis N. Application of fragment screening by X-ray crystallography to β-secretase. J Med Chem 2007;50:1116-1123. (Pubitemid 46496312)
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, Issue.6
, pp. 1116-1123
-
-
Murray, C.W.1
Callaghan, O.2
Chessari, G.3
Cleasby, A.4
Congreve, M.5
Frederickson, M.6
Hartshorn, M.J.7
McMenamin, R.8
Patel, S.9
Wallis, N.10
-
205
-
-
33947636525
-
Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of β-secretase
-
DOI 10.1021/jm061197u
-
Congreve M, Aharony D, Albert A, Callaghan O, Campbell J, Carr RAE, Chessari G, Cowan S, Edwards PD, Frederickson M, McMenamin R, Murray CW, Patel S, Wallis N. Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of β-secretase. J Med Chem 2007;50:1124-1132. (Pubitemid 46496313)
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, Issue.6
, pp. 1124-1132
-
-
Congreve, M.1
Aharony, D.2
Albert, J.3
Callaghan, O.4
Campbell, J.5
Carr, R.A.E.6
Chessari, G.7
Cowan, S.8
Edwards, P.D.9
Frederickson, M.10
McMenamin, R.11
Murray, C.W.12
Patel, S.13
Wallis, N.14
-
206
-
-
32344436117
-
Aminoethylenes: A tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1
-
Sunesis Pharm. Inc.
-
Yang W, Lu W, Lu Y, Zhong M, Sun J, Thomas AE, Wilkinson JM, Fucini RV, Lam M, Randal M, Shi X-P, Jacobs JW, McDowell RS, Gordon EM, Ballinger MD. (Sunesis Pharm. Inc.) Aminoethylenes: A tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1. J Med Chem 2006;49:839-842.
-
(2006)
J Med Chem
, vol.49
, pp. 839-842
-
-
Yang, W.1
Lu, W.2
Lu, Y.3
Zhong, M.4
Sun, J.5
Thomas, A.E.6
Wilkinson, J.M.7
Fucini, R.V.8
Lam, M.9
Randal, M.10
Shi, X.-P.11
Jacobs, J.W.12
McDowell, R.S.13
Gordon, E.M.14
Ballinger, M.D.15
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