메뉴 건너뛰기




Volumn 29, Issue 2, 2009, Pages 295-338

Boom in the development of non-peptidic β-secretase (BACE1) inhibitors for the treatment of Alzheimer's disease

Author keywords

secretase; Alzheimer's disease; BACE1; Non peptidic inhibitors

Indexed keywords

3 (2,4 DIMETHOXYBENZYLIDENE)ANABASEINE; ACC 001; ALZHEIMER DISEASE VACCINE; AP 2238; BAPINEUZUMAB; BETA SECRETASE INHIBITOR; CHOLINESTERASE INHIBITOR; E 2012; GAMMA SECRETASE INHIBITOR; GT 1017; GUANIDINE DERIVATIVE; HETEROCYCLIC COMPOUND; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; ISONICOTINAMIDE; ISPRONICLINE; KMI 249; KMI 429; KMI 570; KMI 684; LACTAM DERIVATIVE; LADOSTIGIL; LY 2062430; MEM 3454; MEVINOLIN; MK 0752; MORPHOLINE DERIVATIVE; N2 [2 (3,5 DIFLUOROPHENYL) 2 HYDROXYACETYL] N1 (6,7 DIHYDRO 5 METHYL 6 OXO 5H DIBENZ[B,D]AZEPIN 7 YL)ALANINAMIDE; OM 00 3; OM 99 2; PF 4360365; SIMVASTATIN; SULFONIC ACID DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; PROTEINASE INHIBITOR; SECRETASE;

EID: 62249167406     PISSN: 01986325     EISSN: None     Source Type: Journal    
DOI: 10.1002/med.20132     Document Type: Review
Times cited : (115)

References (206)
  • 1
    • 34247876141 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 5
    • 0019972810 scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 10
    • 0027258525 scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 14
    • 33846633336 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 17
    • 33947314641 scopus 로고    scopus 로고
    • 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 scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 25
    • 34247581682 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 37
    • 33748774150 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고
    • 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
  • 41
    • 0026476297 scopus 로고
    • 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
  • 45
    • 5744225747 scopus 로고    scopus 로고
    • 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
  • 47
    • 0035005101 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 51
    • 24944439990 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 55
    • 0034613320 scopus 로고    scopus 로고
    • 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
  • 61
    • 34247647440 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 65
    • 33750877824 scopus 로고    scopus 로고
    • 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
  • 70
    • 33745052352 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 74
    • 0034881503 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 84
    • 0034965645 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 89
    • 66249115457 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 92
    • 33646140305 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 114
    • 66249125511 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 135
    • 66249089669 scopus 로고    scopus 로고
    • 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
  • 137
    • 21244479168 scopus 로고    scopus 로고
    • 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
  • 140
    • 33646152294 scopus 로고    scopus 로고
    • 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
  • 142
    • 33646153249 scopus 로고    scopus 로고
    • 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
  • 146
    • 66249101379 scopus 로고    scopus 로고
    • 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
  • 148
    • 66249106203 scopus 로고    scopus 로고
    • 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
  • 150
    • 66249118850 scopus 로고    scopus 로고
    • 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
  • 152
    • 66249118850 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 159
    • 33750875336 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 162
    • 66249104135 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 182
    • 66249138303 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 185
    • 64349121143 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 193
    • 66249085368 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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
  • 197
    • 66249107222 scopus 로고    scopus 로고
    • 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
  • 199
    • 33646140084 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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 scopus 로고    scopus 로고
    • 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


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.