메뉴 건너뛰기




Volumn 16, Issue 14, 2009, Pages 1806-1820

Progress in the development of nonpeptidomimetic BACE 1 inhibitors for Alzheimer's disease

Author keywords

Alzheimer's disease (AD); BACE 1 inhibitor; Nonpeptidomimetic inhibitors

Indexed keywords

2 AMINO ISOINDOLE DERIVATIVE; 2 AMINO PYRIDINONE DERIVATIVE; 2 AMINO QUINAZOLINE DERIVATIVE; 2 AMINO QUINOLINE DERIVATIVE; 2 AMINOTHIAZOLE DERIVATIVE; 6 AMINO IMIDAZOPYRIMIDINE DERIVATIVE; ACYLGUANIDINE DERIVATIVE; BETA SECRETASE; BETA SECRETASE INHIBITOR; HETEROARYL PHENYLPROPAN 2 AMINE DERIVATIVE; ISOPHTHALAMIDE DERIVATIVE; NONPEPTIDOMIMETIC BETA SECRETASE INHIBITOR; PIPERAZINE DERIVATIVE; UNCLASSIFIED DRUG; ASPARTIC PROTEINASE; BACE1 PROTEIN, HUMAN; PROTEINASE INHIBITOR; SECRETASE;

EID: 67651047153     PISSN: 09298673     EISSN: None     Source Type: Journal    
DOI: 10.2174/092986709788186174     Document Type: Review
Times cited : (58)

References (111)
  • 1
    • 29144508843 scopus 로고    scopus 로고
    • Global prevalence ofdementia: A delphi consensus study
    • Ferri, C.; Prince, M.; Brayne, C. Global prevalence ofdementia: A delphi consensus study. Lancet, 2005, 366, 2112-2117.
    • (2005) Lancet , vol.366 , pp. 2112-2117
    • Ferri, C.1    Prince, M.2    Brayne, C.3
  • 2
    • 5644239087 scopus 로고    scopus 로고
    • Alzheimer disease: Mechanistic understanding predicts novel therapies
    • Selkoe, D. Alzheimer disease: Mechanistic understanding predicts novel therapies. Ann. Intern. Med., 2004, 140, 627-638
    • (2004) Ann. Intern. Med , vol.140 , pp. 627-638
    • Selkoe, D.1
  • 3
    • 33645091918 scopus 로고    scopus 로고
    • Recent developments of structure based β-secretase inhibitors for Alzheimer's disease
    • Ghosha, A. K.; Kumaragurubaran, N.; Tang, J. Recent developments of structure based β-secretase inhibitors for Alzheimer's disease. Curr. Top Med. Chem., 2005, 5, 1609-1622.
    • (2005) Curr. Top Med. Chem , vol.5 , pp. 1609-1622
    • Ghosha, A.K.1    Kumaragurubaran, N.2    Tang, J.3
  • 4
    • 33745052352 scopus 로고    scopus 로고
    • Guo, T.; W. Hobbs, D. Development of BACE1 inhibitors for Alzheimer's disease. Curr. Med. Chem., 2006, 13, 1811-1829
    • Guo, T.; W. Hobbs, D. Development of BACE1 inhibitors for Alzheimer's disease. Curr. Med. Chem., 2006, 13, 1811-1829
  • 5
    • 33646133879 scopus 로고    scopus 로고
    • BACE inhibitor reduces APP-..-C-terminal fragment accumulation in axonal swellings of okadaic acid-induced neurodegeneration
    • Yoon, S. Y.; Choi, J. E.; Yoon, J. H.; Huh, J.-W.; Kim, D. H. BACE inhibitor reduces APP-..-C-terminal fragment accumulation in axonal swellings of okadaic acid-induced neurodegeneration. Neurobiol. Dis., 2006, 22, 435-444.
    • (2006) Neurobiol. Dis , vol.22 , pp. 435-444
    • Yoon, S.Y.1    Choi, J.E.2    Yoon, J.H.3    Huh, J.-W.4    Kim, D.H.5
  • 7
    • 0034633995 scopus 로고    scopus 로고
    • Proteolytic activation of recombinant pro-memapsin 2 (pro-β-secretase) studied with new fluorogenic substrates
    • Ermolieff, J.; Loy, J. A.; Koelsch, G.; Tang, J. Proteolytic activation of recombinant pro-memapsin 2 (pro-β-secretase) studied with new fluorogenic substrates. Biochemistry-US, 2000, 39, 12450-12456.
    • (2000) Biochemistry-US , vol.39 , pp. 12450-12456
    • Ermolieff, J.1    Loy, J.A.2    Koelsch, G.3    Tang, J.4
  • 8
    • 20844450922 scopus 로고    scopus 로고
    • Recent developments on the studies of human memapsin 2 (β-secretase)
    • Tang, J.; He, X.; Huang, X.; Hong, L. Recent developments on the studies of human memapsin 2 (β-secretase). Curr. Alzheimer Res., 2005, 2, 261-264.
    • (2005) Curr. Alzheimer Res , vol.2 , pp. 261-264
    • Tang, J.1    He, X.2    Huang, X.3    Hong, L.4
  • 9
    • 0345803941 scopus 로고    scopus 로고
    • Inhibition of receptor-mediated endocytosis demonstrates generation of amyloid β-protein at the cell surface
    • Chyung, J. H.; Selkoe, D. J. Inhibition of receptor-mediated endocytosis demonstrates generation of amyloid β-protein at the cell surface. J. Biol. Chem., 2003, 278, 51035-51043.
    • (2003) J. Biol. Chem , vol.278 , pp. 51035-51043
    • Chyung, J.H.1    Selkoe, D.J.2
  • 10
    • 68449100100 scopus 로고    scopus 로고
    • Transmembrane structure and catalytic mechanism of presenilin 1
    • Guang-Wei, X.; Ying-Jiu, Z. Transmembrane structure and catalytic mechanism of presenilin 1. J. Biochem. Mol. Biol., 2007, 23, 894-898.
    • (2007) J. Biochem. Mol. Biol , vol.23 , pp. 894-898
    • Guang-Wei, X.1    Ying-Jiu, Z.2
  • 14
    • 0033518264 scopus 로고    scopus 로고
    • Membrane-anchored aspartyl protease with Alzheimer's disease β-secretase activity
    • Yan, R.; Bienkowski, M.; Shuck, M.; Miao, H.; Tory, M.; Pauley, A. Membrane-anchored aspartyl protease with Alzheimer's disease β-secretase activity. Nature, 1999, 402, 533-537.
    • (1999) Nature , vol.402 , pp. 533-537
    • Yan, R.1    Bienkowski, M.2    Shuck, M.3    Miao, H.4    Tory, M.5    Pauley, A.6
  • 15
    • 0033595706 scopus 로고    scopus 로고
    • β-Secretase cleavage of Alzheimer's amyloid precursor-protein by the transmembrane aspartic protease BACE
    • Vassar, R.; Bennett, B.; Babu-Khan, S.; Kahn, S.; Mendiaz, E.; Denis, P. β-Secretase cleavage of Alzheimer's amyloid precursor-protein by the transmembrane aspartic protease BACE. Science, 1999, 286, 735-741.
    • (1999) Science , vol.286 , pp. 735-741
    • Vassar, R.1    Bennett, B.2    Babu-Khan, S.3    Kahn, S.4    Mendiaz, E.5    Denis, P.6
  • 17
  • 18
    • 24944550164 scopus 로고    scopus 로고
    • Thompson, L. A.; J.Bronson, J.; Zusi, F. C. Progress in the discovery of BACE inhibitors. Curr. Pharm. Design, 2005, 11, 3383-3404.
    • Thompson, L. A.; J.Bronson, J.; Zusi, F. C. Progress in the discovery of BACE inhibitors. Curr. Pharm. Design, 2005, 11, 3383-3404.
  • 19
    • 44349184966 scopus 로고    scopus 로고
    • Crystal structure of an active form of BACE1, an enzyme responsible for Amyloid-β protein production
    • Shimizu, H.; Tosaki, A.; Kaneko, K.; Hisano, T.; Sakurai, T.; Nukina, N. Crystal structure of an active form of BACE1, an enzyme responsible for Amyloid-β protein production. Mol. Cell Bio., 2008, 28, 3663-3671.
    • (2008) Mol. Cell Bio , vol.28 , pp. 3663-3671
    • Shimizu, H.1    Tosaki, A.2    Kaneko, K.3    Hisano, T.4    Sakurai, T.5    Nukina, N.6
  • 21
    • 33645544750 scopus 로고    scopus 로고
    • Small-sized BACE1 inhibitors
    • Ziora, Z.; Kimura, T.; Kiso, Y. Small-sized BACE1 inhibitors. Drug Future, 2006, 31, 53-63.
    • (2006) Drug Future , vol.31 , pp. 53-63
    • Ziora, Z.1    Kimura, T.2    Kiso, Y.3
  • 23
    • 33646189389 scopus 로고    scopus 로고
    • β-Secretase (BACE) and BACE inhibitors: Progress report
    • John, V. β-Secretase (BACE) and BACE inhibitors: Progress report. Curr. Top Med. Chem., 2006, 6, 569-578.
    • (2006) Curr. Top Med. Chem , vol.6 , pp. 569-578
    • John, V.1
  • 25
    • 33847711478 scopus 로고    scopus 로고
    • Disease-modifying therapies in Alzheimer's disease how far have we come?
    • Hull, M.; Berger, M.; Heneka, M. Disease-modifying therapies in Alzheimer's disease how far have we come? Drugs, 2006, 66, 2075-2093.
    • (2006) Drugs , vol.66 , pp. 2075-2093
    • Hull, M.1    Berger, M.2    Heneka, M.3
  • 26
    • 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, A. K.; Zhang, X. C.; 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
  • 28
    • 68449095692 scopus 로고    scopus 로고
    • Craig, A. C. Pyrrolidin-3-yl compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease. 2006, WO2006002004.
    • Craig, A. C. Pyrrolidin-3-yl compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease. 2006, WO2006002004.
  • 29
    • 68449088321 scopus 로고    scopus 로고
    • β-secretase inhibitors
    • Yoshiaki, K. β-secretase inhibitors. 2007, WO2007029587.
    • (2007) WO2007029587
    • Yoshiaki, K.1
  • 34
    • 9744221865 scopus 로고    scopus 로고
    • Coburn, C. A.; Stachel, S. J.; Li, Y.-M.; Rush, D. M.; Steele, T. G.; Chen-Dodson, E.; Holloway, M. K.; Xu, M.; Huang, Q.; Lai, M.-T.; DiMuzio, J.; Crouthamel, M.-C.; Shi, X.-P.; Sardana, V.; Chen, Z.; Munshi, S.; Kuo, L.; Makara, G. M.; Annis, D. A.; Tadikonda, P. K.; Nash, H. M.; Vacca, J. P.; 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.
    • Coburn, C. A.; Stachel, S. J.; Li, Y.-M.; Rush, D. M.; Steele, T. G.; Chen-Dodson, E.; Holloway, M. K.; Xu, M.; Huang, Q.; Lai, M.-T.; DiMuzio, J.; Crouthamel, M.-C.; Shi, X.-P.; Sardana, V.; Chen, Z.; Munshi, S.; Kuo, L.; Makara, G. M.; Annis, D. A.; Tadikonda, P. K.; Nash, H. M.; Vacca, J. P.; 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.
  • 36
    • 68449096918 scopus 로고    scopus 로고
    • Novel phenylcarboxyamides as beta-secretase inhibiors.
    • US20070032470
    • Wu, Y.-J.; Zhang, Y. Novel phenylcarboxyamides as beta-secretase inhibiors. 2007, US20070032470.
    • (2007)
    • Wu, Y.-J.1    Zhang, Y.2
  • 38
    • 68449092675 scopus 로고    scopus 로고
    • Cyclic ketal beta-secretase inhibitors for the treatment of Alzheimer's disease
    • Philippe, G. N.; Joseph, P. V. Cyclic ketal beta-secretase inhibitors for the treatment of Alzheimer's disease. 2007, WO2007019111.
    • (2007) WO2007019111
    • Philippe, G.N.1    Joseph, P.V.2
  • 39
    • 29544449814 scopus 로고    scopus 로고
    • Stachel, S. J.; Coburn, C. A.; Steele, T. G.; Min-Chirouthamel; Pietrak, B. L.; Lai, M.-T.; Holloway, M. K.; Munshi, S. K.; Grahama, S. L.; Vacca, J. P. Conformationally biased P3 amide replacements of β-secretase inhibitors. Bioorg. Med. Chem. Lett., 2006, 16, 641-644.
    • Stachel, S. J.; Coburn, C. A.; Steele, T. G.; Min-Chirouthamel; Pietrak, B. L.; Lai, M.-T.; Holloway, M. K.; Munshi, S. K.; Grahama, S. L.; Vacca, J. P. Conformationally biased P3 amide replacements of β-secretase inhibitors. Bioorg. Med. Chem. Lett., 2006, 16, 641-644.
  • 44
    • 33847029846 scopus 로고    scopus 로고
    • Stauffer, S. R.; Stanton, M. G.; Gregro, A. R.; Steinbeiser, M. A.; Shaffer, J. R.; Nantermet, P. G.; Barrow, J. C.; Rittle, K. E.; Collusi, D.; Espeseth, A. S.; Lai, M.-T.; Pietrak, B. L.; Holloway, M. K.; McGaughey, G. B.; Munshi, S. K.; Hochman, J. H.; Simon, A. J.; Selnick, H. G.; Grahama, S. L.; Vaccaa, J. P. 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.
    • Stauffer, S. R.; Stanton, M. G.; Gregro, A. R.; Steinbeiser, M. A.; Shaffer, J. R.; Nantermet, P. G.; Barrow, J. C.; Rittle, K. E.; Collusi, D.; Espeseth, A. S.; Lai, M.-T.; Pietrak, B. L.; Holloway, M. K.; McGaughey, G. B.; Munshi, S. K.; Hochman, J. H.; Simon, A. J.; Selnick, H. G.; Grahama, S. L.; Vaccaa, J. P. 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.
  • 47
    • 68449085818 scopus 로고    scopus 로고
    • N-methyl hydroxythylamine useful in treating CNS conditions
    • Fox, K. E.; Charles, M. J. N-methyl hydroxythylamine useful in treating CNS conditions. 2006, WO2006032999.
    • (2006) WO2006032999
    • Fox, K.E.1    Charles, M.J.2
  • 48
    • 32344436117 scopus 로고    scopus 로고
    • Yang, W.; Lu, W.; Lu, Y.; Zhong, M.; Sun, J.; Thomas, A. E.; Wilkinson, J. M.; Fucini, R. V.; Lam, M.; Randal, M.; Shi, X.-P.; Jacobs, J. W.; McDowell, R. S.; Gordon, E. M.; Ballinger, M. D. Aminoethylenes: A tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1. J. Med. Chem., 2006, 49, 839-842.
    • Yang, W.; Lu, W.; Lu, Y.; Zhong, M.; Sun, J.; Thomas, A. E.; Wilkinson, J. M.; Fucini, R. V.; Lam, M.; Randal, M.; Shi, X.-P.; Jacobs, J. W.; McDowell, R. S.; Gordon, E. M.; Ballinger, M. D. Aminoethylenes: A tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1. J. Med. Chem., 2006, 49, 839-842.
  • 53
    • 68449095690 scopus 로고    scopus 로고
    • 2-aminopyridine compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
    • Craig, A. C.; Katharine, H. M.; Shawn, J. S. 2-aminopyridine compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease. 2006, WO2006060109.
    • (2006) WO2006060109
    • Craig, A.C.1    Katharine, H.M.2    Shawn, J.S.3
  • 61
    • 34548510854 scopus 로고    scopus 로고
    • Baxter, E. W.; Conway, K. A.; Kennis, L.; Bischoff, F.; Mercken, M. H.; Winter, H. L. D.; Reynolds, C. H.; Tounge, B. A.; Luo, C.; Scott, M. K.; Huang, Y.; Braeken, M.; Pieters, S. M. A.; Berthelot, D. J. C.; Masure, S.; Bruinzeel, W. D.; Jordan, A. D.; Parker, M. H.; Boyd, R. E.; Qu, J.; Alexander, R. S.; Brenneman, D. E.; Reitz, A. B. 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.
    • Baxter, E. W.; Conway, K. A.; Kennis, L.; Bischoff, F.; Mercken, M. H.; Winter, H. L. D.; Reynolds, C. H.; Tounge, B. A.; Luo, C.; Scott, M. K.; Huang, Y.; Braeken, M.; Pieters, S. M. A.; Berthelot, D. J. C.; Masure, S.; Bruinzeel, W. D.; Jordan, A. D.; Parker, M. H.; Boyd, R. E.; Qu, J.; Alexander, R. S.; Brenneman, D. E.; Reitz, A. B. 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.
  • 63
    • 68449101247 scopus 로고    scopus 로고
    • 2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of β-secretase (BACE)
    • Ellen, B.; Allen, B. R.; John, C. C. 2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of β-secretase (BACE). 2007;. 2007, WO2007092846.
    • (2007) WO2007092846
    • Ellen, B.1    Allen, B.R.2    John, C.C.3
  • 66
    • 68449098852 scopus 로고    scopus 로고
    • Novel 2-aminopyrimidinone or 2-aminopyridinone derivatives and their use
    • Jeffrey, A.; Phil, E.; James, E. Novel 2-aminopyrimidinone or 2-aminopyridinone derivatives and their use. 2007, WO2007058582.
    • (2007) WO2007058582
    • Jeffrey, A.1    Phil, E.2    James, E.3
  • 67
    • 68449088319 scopus 로고    scopus 로고
    • 2-aminopyrimidin-4-ones and their use for treating or preventing Aβ-related pathologies
    • Stefan, B.; Johan, H.; Sven, H.; Johan, M. 2-aminopyrimidin-4-ones and their use for treating or preventing Aβ-related pathologies. 2007, WO2007114771.
    • (2007) WO2007114771
    • Stefan, B.1    Johan, H.2    Sven, H.3    Johan, M.4
  • 68
    • 68449096316 scopus 로고    scopus 로고
    • Wu, Y.; Iserloh, U.; N.Cumming, J.; Liu, X.; Mazzola, R. D.; Sun, Z.-Y.; Huang, Y.; Stamford, A.; McKittrick, B.; Zhu, Z. Aspartyl protease inhibitors. 2007, US20070287692.
    • Wu, Y.; Iserloh, U.; N.Cumming, J.; Liu, X.; Mazzola, R. D.; Sun, Z.-Y.; Huang, Y.; Stamford, A.; McKittrick, B.; Zhu, Z. Aspartyl protease inhibitors. 2007, US20070287692.
  • 69
    • 37849043411 scopus 로고    scopus 로고
    • Edwards, P. D.; Albert, J. S.; Sylvester, M.; Aharony, D.; Andisik, D.; Callaghan, O.; Campbell, J. B.; Carr, R. A.; Chessari, G.; Congreve, M.; Frederickson, M.; Folmer, R. H. A.; Geschwindner, S.; Koether, G.; Kolmodin, K.; Krumrine, J.; Mauger, R. C.; Murray, C. W.; Olsson, L.-L.; Patel, S.; Spear, N.; Tian, G. Application of fragment-based lead generation to the discovery of novel, cyclic amidine β-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency. J. Med. Chem., 2007, 50, 5912-5925.
    • Edwards, P. D.; Albert, J. S.; Sylvester, M.; Aharony, D.; Andisik, D.; Callaghan, O.; Campbell, J. B.; Carr, R. A.; Chessari, G.; Congreve, M.; Frederickson, M.; Folmer, R. H. A.; Geschwindner, S.; Koether, G.; Kolmodin, K.; Krumrine, J.; Mauger, R. C.; Murray, C. W.; Olsson, L.-L.; Patel, S.; Spear, N.; Tian, G. Application of fragment-based lead generation to the discovery of novel, cyclic amidine β-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency. J. Med. Chem., 2007, 50, 5912-5925.
  • 71
    • 68449093263 scopus 로고    scopus 로고
    • Quagliato, D. A, Andrae, P. M, Fan, Y. Dihydrospiro+8 dibenzo+ 8 A,D+9+8 7+9 annulene-5,4′-imidazol +9+0 compounds for the inhibition of beta-secretase. 2007, US2007203116
    • Quagliato, D. A.; Andrae, P. M.; Fan, Y. Dihydrospiro+8 dibenzo+ 8 A,D+9+8 7+9 annulene-5,4′-imidazol +9+0 compounds for the inhibition of beta-secretase. 2007, US2007203116.
  • 73
    • 68449091431 scopus 로고    scopus 로고
    • 2-Amino-imidazole-4-one compounds and their use in the manufacture of a medicament to be used in the treatment of cogntive impairment, Alzheimer's diease neurodegeneration and dementia
    • Jeffrey, A.; James, A.; Gianni, C.; Stuart, G. M.; Phil, E.; Christopher, M.; Sahil, P. 2-Amino-imidazole-4-one compounds and their use in the manufacture of a medicament to be used in the treatment of cogntive impairment, Alzheimer's diease neurodegeneration and dementia. 2007, WO2007058601.
    • (2007) WO2007058601
    • Jeffrey, A.1    James, A.2    Gianni, C.3    Stuart, G.M.4    Phil, E.5    Christopher, M.6    Sahil, P.7
  • 75
    • 68449094513 scopus 로고    scopus 로고
    • Novel 2-aminopyrimidine derivatives and their use
    • Jeffrey, A.; Gianni, C.; Phil, E. Novel 2-aminopyrimidine derivatives and their use. 2007, WO2007058581.
    • (2007) WO2007058581
    • Jeffrey, A.1    Gianni, C.2    Phil, E.3
  • 77
    • 68449084604 scopus 로고    scopus 로고
    • Substituted theienyl and furyl acylguanudines and methouds of their use as beta-secretase modulators.
    • US20060183792
    • Fobare, W. F.; Solvible, J. W. R. Substituted theienyl and furyl acylguanudines and methouds of their use as beta-secretase modulators. 2006, US20060183792.
    • (2006)
    • Fobare, W.F.1    Solvible, J.W.R.2
  • 78
    • 68449087674 scopus 로고    scopus 로고
    • A.; McKittrick, B. Aspartyl protease inhibitors.
    • US2007009987
    • Zhu, Z.; W.Stamford, A.; McKittrick, B. Aspartyl protease inhibitors. 2007, US2007009987.
    • (2007)
    • Zhu, Z.1    Stamford, W.2
  • 79
    • 68449083992 scopus 로고    scopus 로고
    • Thompson, L. A.; Shi, J.; E.Macor, J.; Zusi, F. C.; F.Dee, M.; Macor, J. E. Indole acetic acid acylguandines as beta-secretase inhibitors. 2007, US20070049589.
    • Thompson, L. A.; Shi, J.; E.Macor, J.; Zusi, F. C.; F.Dee, M.; Macor, J. E. Indole acetic acid acylguandines as beta-secretase inhibitors. 2007, US20070049589.
  • 80
    • 64349113476 scopus 로고    scopus 로고
    • N-aryl pyrrolidine derivatives as beta-secretase inhibitors.
    • US2007232679
    • Boy, K. M.; Zhu, S.; Macor, J. E.; Shi, S.; Gerritz, S. N-aryl pyrrolidine derivatives as beta-secretase inhibitors. 2007, US2007232679.
    • (2007)
    • Boy, K.M.1    Zhu, S.2    Macor, J.E.3    Shi, S.4    Gerritz, S.5
  • 81
    • 68449093909 scopus 로고    scopus 로고
    • Thiazol-guanidine derivatives useful as A(beta)-related pathologies
    • Stefan, B.; Karin, K. Thiazol-guanidine derivatives useful as A(beta)-related pathologies. 2007, WO2007120096.
    • (2007) WO2007120096
    • Stefan, B.1    Karin, K.2
  • 82
    • 85017409795 scopus 로고    scopus 로고
    • Oxime-containing acylguanidines as beta-secretase inhibitors.
    • US2007232581
    • Wu, Y.-J.; Gerritz, S.; Shi, S.; Zhu, S. Oxime-containing acylguanidines as beta-secretase inhibitors. 2007, US2007232581.
    • (2007)
    • Wu, Y.-J.1    Gerritz, S.2    Shi, S.3    Zhu, S.4
  • 84
    • 33745814403 scopus 로고    scopus 로고
    • Naphthyl and coumarinyl biarylpiperazine derivatives as highly potent human β-secretase inhibitors. Design, synthesis, and enzymatic BACE-1 and cell assays
    • Garino, C.; Tomita, T.; Pietrancosta, N.; Laras, Y.; Rosas, R.; Herbette, G.; Maigret, B.; Quéléver, G.; Iwatsubo, T.; Kraus, J.-L. Naphthyl and coumarinyl biarylpiperazine derivatives as highly potent human β-secretase inhibitors. Design, synthesis, and enzymatic BACE-1 and cell assays. J. Med. Chem., 2006, 49, 4275-4285.
    • (2006) J. Med. Chem , vol.49 , pp. 4275-4285
    • Garino, C.1    Tomita, T.2    Pietrancosta, N.3    Laras, Y.4    Rosas, R.5    Herbette, G.6    Maigret, B.7    Quéléver, G.8    Iwatsubo, T.9    Kraus, J.-L.10
  • 85
    • 33144455805 scopus 로고
    • BACE-1 inhibitory activities of new substituted phenyl-piperazine coupled to various heterocycles: Chromene, coumarin and quinoline
    • Garino, C.; Pietrancosta, N.; Laras, Y.; Moret, V.; Rolland, A.; Quéléver, G.; Kraus, J.-L. BACE-1 inhibitory activities of new substituted phenyl-piperazine coupled to various heterocycles: chromene, coumarin and quinoline. Bioorg. Med. Chem. Lett., 2006, 16, 1995-1999.
    • (1995) Bioorg. Med. Chem. Lett , vol.2006 , pp. 16
    • Garino, C.1    Pietrancosta, N.2    Laras, Y.3    Moret, V.4    Rolland, A.5    Quéléver, G.6    Kraus, J.-L.7
  • 86
    • 56349084787 scopus 로고    scopus 로고
    • Identification of pharmacophore model, synthesis and biological evaluation of Nphenyl-1-arylamide and N-phenylbenzenesulfonamide derivatives as BACE 1 inhibitors
    • Huang, W.; Yu, H.; Sheng, R.; Li, J.; Hu, Y. Identification of pharmacophore model, synthesis and biological evaluation of Nphenyl-1-arylamide and N-phenylbenzenesulfonamide derivatives as BACE 1 inhibitors. Bioorg. Med. Chem., 2008, 16, 10190-10197.
    • (2008) Bioorg. Med. Chem , vol.16 , pp. 10190-10197
    • Huang, W.1    Yu, H.2    Sheng, R.3    Li, J.4    Hu, Y.5
  • 87
    • 68449098226 scopus 로고    scopus 로고
    • Peter, H.; Robert, M.; Stefan, S.; Vincenzo, T.; Christiane, M.; Christoph, S. Organische verbindungen. 2006, EP1707202.
    • Peter, H.; Robert, M.; Stefan, S.; Vincenzo, T.; Christiane, M.; Christoph, S. Organische verbindungen. 2006, EP1707202.
  • 88
    • 68449087029 scopus 로고    scopus 로고
    • Piperazinderivate zur inhibition von beta-sekretase, cathepsin D, plasmepsin II und HIV-protease und zur behandlung von malaria, Alzheimer und
    • Peter, H.; Robert, M.; Stefan, S.; Vincenzo, T.; Christiane, M.; Christoph, S. Piperazinderivate zur inhibition von beta-sekretase, cathepsin D, plasmepsin II und HIV-protease und zur behandlung von malaria, Alzheimer und AIDS. 2006, EP1707206.
    • (2006) AIDS , vol.EP1707206
    • Peter, H.1    Robert, M.2    Stefan, S.3    Vincenzo, T.4    Christiane, M.5    Christoph, S.6
  • 89
    • 68449083991 scopus 로고    scopus 로고
    • Compositions and treatment using pyridazine compounds and secretases
    • Martin, W.; Linda, V. E.; Wnhui, H. Compositions and treatment using pyridazine compounds and secretases. 2007, WO2007 130383.
    • (2007) WO2007 130383
    • Martin, W.1    Linda, V.E.2    Wnhui, H.3
  • 91
    • 68449099476 scopus 로고    scopus 로고
    • Herold, P, Mah, R, Stutz, S, Tschinke, V, Schumacher, C, Stojanovic, A, Jotterand, N, Behnke, D. 3,4,5-substituted piperidines as therapeutic compounds. 2007, US2007167433
    • Herold, P.; Mah, R.; Stutz, S.; Tschinke, V.; Schumacher, C.; Stojanovic, A.; Jotterand, N.; Behnke, D. 3,4,5-substituted piperidines as therapeutic compounds. 2007, US2007167433.
  • 93
    • 68449088320 scopus 로고    scopus 로고
    • Tertiary carbinamines having substituted heterocycles, which are active as inhibitors of beta-secretase, for the treatment of Alzheimer's disease
    • Georgia, B. M.; Philippe, G. N.; Hemaka, A. R.; Shaun, R. S. Tertiary carbinamines having substituted heterocycles, which are active as inhibitors of beta-secretase, for the treatment of Alzheimer's disease. 2006, WO2006078577.
    • (2006) WO2006078577
    • Georgia, B.M.1    Philippe, G.N.2    Hemaka, A.R.3    Shaun, R.S.4
  • 94
    • 68449086421 scopus 로고    scopus 로고
    • Tricyclic beta-secretase inhibitors for the treatment of Alzheimer's disease
    • Philippe, G. N. Tricyclic beta-secretase inhibitors for the treatment of Alzheimer's disease. 2007, WO2007019078.
    • (2007) WO2007019078
    • Philippe, G.N.1
  • 95
    • 68449086421 scopus 로고    scopus 로고
    • Tricyclic beta-secretase inhibitors for the treatment of Alzheimer's disease
    • Philippe, G. N.; Hemaka, A. R. Tricyclic beta-secretase inhibitors for the treatment of Alzheimer's disease. 2007, WO2007019080.
    • (2007) WO2007019080
    • Philippe, G.N.1    Hemaka, A.R.2
  • 97
    • 4544280990 scopus 로고    scopus 로고
    • Structure-based design of a macrocyclic inhibitor for peptide deformylase
    • Hu, X.; Nguyen, K. T.; Jiang, V. C.; Lofland, D.; Moser, H. E.; Pei, D. Structure-based design of a macrocyclic inhibitor for peptide deformylase. J. Med. Chem., 2004, 47, 4941-4949.
    • (2004) J. Med. Chem , vol.47 , pp. 4941-4949
    • Hu, X.1    Nguyen, K.T.2    Jiang, V.C.3    Lofland, D.4    Moser, H.E.5    Pei, D.6
  • 99
    • 68449091430 scopus 로고    scopus 로고
    • Macrocyclic diaminopropanes as beta-secretase inhibitors.
    • US20070037868
    • Marcin, L. R.; Good, A. C. Macrocyclic diaminopropanes as beta-secretase inhibitors. 2007, US20070037868.
    • (2007)
    • Marcin, L.R.1    Good, A.C.2
  • 100
    • 68449087676 scopus 로고    scopus 로고
    • Macrocyclic compounds and composions useful as beta-secretase inhibitors
    • Andreas, L.; Rainer, M.; Oliver, S.; Marina, T.-B. Macrocyclic compounds and composions useful as beta-secretase inhibitors. 2006, WO2006074940.
    • (2006) WO2006074940
    • Andreas, L.1    Rainer, M.2    Oliver, S.3    Marina, T.-B.4
  • 103
    • 33746330728 scopus 로고    scopus 로고
    • Synthesis of tetramic and tetronic acids as β-secretase inhibitors
    • Larbig, G.; Schmidt, B. Synthesis of tetramic and tetronic acids as β-secretase inhibitors. J. Comb. Chem., 2006, 8, 480-490.
    • (2006) J. Comb. Chem , vol.8 , pp. 480-490
    • Larbig, G.1    Schmidt, B.2
  • 104
    • 68449090785 scopus 로고    scopus 로고
    • Benzazole derivatives, compositions, and methods of use as beta-secretase inhibitors.
    • US20060223849
    • Mjalli, A. M. M.; Jones, D.; Gohimukkula, D. R.; Huang, G.; Zhu, J.; Rao, M.; Andrews, R. C.; Ren, T. Benzazole derivatives, compositions, and methods of use as beta-secretase inhibitors. 2006, US20060223849.
    • (2006)
    • Mjalli, A.M.M.1    Jones, D.2    Gohimukkula, D.R.3    Huang, G.4    Zhu, J.5    Rao, M.6    Andrews, R.C.7    Ren, T.8
  • 105
    • 68449083370 scopus 로고    scopus 로고
    • Organic compounds useful for the treatment of Alzheimer's disease and method of prepartion
    • Michela, R.; Vincenza, A.; Manuela, B.; Cario, M. Organic compounds useful for the treatment of Alzheimer's disease and method of prepartion. 2006, WO2006080043.
    • (2006) WO2006080043
    • Michela, R.1    Vincenza, A.2    Manuela, B.3    Cario, M.4
  • 111
    • 68449097525 scopus 로고    scopus 로고
    • Substituted 1,3,4-triazine derivatives
    • Willems, H. Substituted 1,3,4-triazine derivatives. 2004, GB2397301.
    • (2004) GB2397301
    • Willems, H.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.