Drug development and PET-diagnostics for Alzheimer's disease

Current Medicinal Chemistry

Volumn 12, Issue 14, 2005, Pages 1677-1695

  Schmidt, Boris ^a   Braun, Hannes A ^a   Narlawar, Rajeshwar ^a  

^a DARMSTADT UNIVERSITY OF TECHNOLOGY   (Germany)

Author keywords

Alzheimer's disease; Aspartic protease; Cholesterol; Copper; Imaging; Secretase; Statine

Indexed keywords

ALZHEIMER DISEASE VACCINE; BENZENESULFONAMIDE DERIVATIVE; BETA SECRETASE INHIBITOR; CHOLINESTERASE INHIBITOR; DONEPEZIL; FLUPIRTINE; FLURBIPROFEN; GALANTAMINE; HYPOCHOLESTEROLEMIC AGENT; IBUPROFEN; INDOMETACIN; KENPAULLONE; MEMANTINE; METAL CHELATE; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT; NONSTEROID ANTIINFLAMMATORY AGENT; PEPTIDE DERIVATIVE; PLACEBO; PYRIMIDINE DERIVATIVE; RIVASTIGMINE; SEROTONIN AGONIST; SULFONAMIDE; SULINDAC; TACRINE;

ALZHEIMER DISEASE; CLINICAL TRIAL; COHORT ANALYSIS; DRUG DOSE REGIMEN; DRUG POTENCY; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION; GENE MUTATION; HALLUCINATION; HUMAN; IN VITRO STUDY; IN VIVO STUDY; LIVER TOXICITY; NONHUMAN; PATENT; POSITRON EMISSION TOMOGRAPHY; REVIEW; TOXICITY TESTING;

ALZHEIMER DISEASE; AMYLOID BETA-PROTEIN; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ENDOPEPTIDASES; ENDOPEPTIDASES; ENZYME INHIBITORS; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NEUROPROTECTIVE AGENTS; OLIGOPEPTIDES; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS;

EID: 21244437567     PISSN: 09298673     EISSN: None     Source Type: Journal    
DOI: 10.2174/0929867054367130     Document Type: Review

References (252)

1. WHO, The World Health Report 2001 Mental Health: New Understanding, New Hope.
2. Polvikoski, T.; Sulkava, R.; Myllykangas, L.; Notkola, I. L.; Niinisto, L.; Verkkoniemi, A.; Kainulainen, K.; Kontula, K.; Perez-Tur, J.; Hardy, J.; Haltia, M. Neurology 2001, 56, 1690.
3. Gil Gregorio, P.; Ramirez Diaz, S. P.; Ribera Casado, J. M. J. Nutr. Health Aging 2003, 7, 304.
4. Thorsett, E. D.; Latimer, L. H. Curr. Opin. Chem. Biol. 2000, 4, 377-382.
5. Grant, W. B. J. Alzheimer's Dis. 1999, 1, 197.
6. Cummings, J. L. N. Engl. J. Med. 2004, 351, 56.
7. Chou, K.-C. J. Proteome Res. 2004, 3, 1969.
8. Mattson, M. P. Nature 2004, 430, 631.
9. Czech, C.; Adessi, C. Curr. Neuropharmacol. 2004, 2, 295.
10. Mandelkow, E.-M.; Mandelkow, E. Trends Cell Biol. 1998, 8, 425.
11. Augustinack, J. C.; Schneider, A.; Mandelkow, E.-M.; Hyman, B. T. Acta Neuropathologica 2002, 103, 26.
12. Ritchie, C. W.; Bush, A. I.; Mackinnon, A.; Macfarlane, S.; Mastwyk, M.; MacGregor, L.; Kiers, L.; Cherny, R.; Li, Q. X.; Tammer, A.; Carrington, D.; Mavros, C.; Volitakis, I.; Xilinas, M.; Ames, D.; Davis, S.; Beyreuther, K.; Tanzi, R. E.; Masters, C. L. Arch. Neurol. 2003, 60, 1685.
13. Bush, A. I.; Masters, C. L.; Tanzi, R. E. PNAS 2003, 11193.
14. Altmann, P. Alum. Alzheimer's Dis. 2001, 1.
15. Fischer, F.; Matthisson, M.; Herrling, P. Neurodegenerative Diseases 2004, 1, 50.
16. Kwon, M.-O.; Fischer, F.; Matthisson, M.; Herrling, P. Neurodegenerative Diseases 2004, 1, 113.
17. Luond, R. M.; Banziger, M.; Frey, P. Preparation of piperidine and piperazine derivatives as inhibitors of the Aβ fibril formation. WO 0047571, 2000.
18. Goldsbury, C. S.; Wirtz, S.; Muller, S. A.; Sunderji, S.; Wicki, P.; Aebi, U.; Frey, P. J. Struct. Biol. 2000, 130, 217.
19. Howlett, D. R.; Perry, A. E.; Godfrey, F.; Swatton, J. E.; Jennings, K. H.; Spitzfaden, C.; Wadsworth, H.; Wood, S. J.; Markwell, R. E. Biochem. J. 1999, 340, 283.
20. Courtney, C.; Farrell, D.; Gray, R.; Hills, R.; Lynch, L.; Sellwood, E.; Edwards, S.; Hardyman, W.; Raftery, J.; Crome, P.; Lendon, C.; Shaw, H.; Bentham, P. Lancet 2004, 363, 2105.
21. Jacobsen, J. S. Curr. Top. Med. Chem. 2002, 2, 343.
22. Ikeda, S.; Yamada, Y.; Ikegami, N. Dementia Geriatr. Cognit. Disord. 2002, 13, 33.
23. Carlson, M. C.; Brandt, J.; Steele, C.; Baker, A.; Stern, Y.; Lyketsos, C. G. J. Gerontol. A Biol. Sci. Med. Sci. 2001, 56, M567.
24. Schneider, L. S. The Lancet 2004, 363, 2100.
25. AD2000Collaborative Group. The Lancet 2004, 363, 2105.
26. Witt, A.; Macdonald, N.; Kirkpatrick, P. Nat. Rev. Drug Discov. 2004, 3, 109.
27. Serradji, N.; Bensaid, O.; Martin, M.; Kan, E.; Dereuddre-Bosquet, N.; Redeuilh, C.; Huet, J.; Heymans, F.; Lamouri, A.; Clayette, P.; Chang Zhi Dong; Dormont, D.; Godfroid, J.-J. J. Med. Chem. 2004, 47, 6410.
28. Weggen, S.; Eriksen, J. L.; Das, P.; Sagi, S. A.; Wang, R.; Pietrizik, C. U.; Findlay, K. A.; Smith, T. E.; Murphy, M. P.; Bulter, T.; Kang, D. E.; Marquez-Sterling, N.; Golde, T. E.; Koo, E. H. Nature 2001, 414, 212.
29. Weggen, S.; Eriksen, J. L.; Sagi, S. A.; Pietrzik, C. U.; Golde, T. E.; Koo, E. H. J. Biol. Chem. 2003, 278, 30748.
30. in't Veld, B. A.; Ruitenberg, A.; Hofman, A.; Launer, L. J.; van Duijn, C. M.; Stijnen, T.; Breteler, M. M. B.; Stricker, B. H. C. N. Engl. J. Med. 2001, 345, 1515.
31. Zhou, Y.; Su, Y.; Li, B.; Liu, F.; Ryder, J. W.; Wu, X.; Gonzalez-DeWhitt, P. A.; Gelfanova, V.; Hale, J. E.; May, P. C.; Paul, S. M.; Ni, B. Science 2003, 302, 1215.
32. Lanz, T. A.; Fici, G. J.; Merchant, K. M. J. Pharm. Exp. Therapeutics 2004, 309, 49.
33. Eriksen, J. L.; Sagi, S. A.; Smith, T. E.; Weggen, S.; Das, P.; McLendon, D. C.; Ozols, V. V.; Jessing, K. W.; Zavitz, K. H.; Koo, E. H.; Golde, T. E. J. Clin. Investigation 2003, 112, 440.
34. Beher, D.; Clarke, E. E.; Wrigley, J. D. J.; Martin, A. C. L.; Nadin, A.; Churcher, I.; Shearman, M. S. J. Biol. Chem. 2004, 279, 43419.
35. Bachmann, M. F.; Tissot, A.; Ortmann, R.; Lueoend, R.; Staufenbiel, M.; Frey, P. Vaccine compositions containing amyloid β1-6 antigen epitopes conjugated with virus-like particles. WO 2004016282, 2004.
36. Schenk, D.; Games, D.; Seubert, P. Neurosci. News 2000, 3, 46.
37. Nicoll, J. A.; Wilkinson, D.; Holmes, C.; Steart, P.; Markham, H.; Weller, R. O. Nat. Med. 2003, 9, 448.
38. Greenberg, S. M.; Bacskai, B. J.; Hyman, B. T. Nat. Med. 2003, 9, 389.
39. Abbott, A. Nature 2004, 430, 715.
40. Oddo, S.; Billings, L.; Kesslak, J. P.; Cribbs, D. H.; LaFerla, F. M. Neuron 2004, 43, 321.
41. Saunders, A. M. Pharmacogenomics 2001, 2, 239.
42. Holmes, C. Br. J. Psychiatry 2002, 180, 131.
43. Tanzi, R. E.; Bertram, L. Neuron 2001, 32, 181.
44. Hardy, J. PNAS 1997, 94, 2095.
45. Hardy, J.; Myers, A.; Wavrant-De Vrieze, F. Neurodegenerative Diseases 2004, 1, 213.
46. Bertram, L.; Tanzi, R. E. J. Mol. Neurosci. 2001, 17, 127.
47. Fraser, P. E.; Yang, D.-S.; Yu, G.; Lévesque, L.; Nishimura, M.; Arawak, S.; Serpell, L. C.; Rogaev, E.; George-Hyslop, P. S. Biochim. Biophys. Acta (BBA) - Molecular Basis of Disease 2000, 1502, 1.
48. Janus, C.; Westaway, D. Physiol. Behav. 2001, 73, 873.
49. Schmitz, C.; Rutten Bart, P. F.; Pielen, A.; Schafer, S.; Wirths, O.; Tremp, G.; Czech, C.; Blanchard, V.; Multhaup, G.; Rezaie, P.; Korr, H.; Steinbusch Harry, W. M.; Pradier, L.; Bayer Thomas, A. Am. J. Pathology 2004, 164, 1495.
50. Eckert, G. P.; Kirsch, C.; Leutz, S.; Wood, W. G.; Muller, W. E. Pharmacopsychiatry 2003, 36 Suppl 2, S136.
51. Moss, M. L.; White, J. M.; Lambert, M. H.; Andrews, R. C. Drug Discov. Today 2001, 6, 417.
52. Kinoshita, A.; Whelan, C. M.; Smith, C. J.; Berezovska, O.; Hyman, B. T. J. Neurochemistry 2002, 82, 839.
53. Kinoshita, A.; Whelan, C. M.; Berezovska, O.; Hyman, B. T. J. Biol. Chem. 2002, 277, 28530.
54. Soto, C. Mol. Med. Today 1999, 5, 343.
55. Kayed, R.; Glabe, C. G. Immunogens and corresponding antibodies specific for high molecular weight aggregation intermediates common to amyloids formed from proteins of differing sequence. WO 2004024090, 2004.
56. Kayed, R.; Head, E.; Thompson, J. L.; McIntire, T. M.; Milton, S. C.; Cotman, C. W.; Glabe, C. G. Science 2003, 300, 486.
57. Capell, A.; Steiner, H.; Willem, M.; Kaiser, H.; Meyer, C.; Walter, J.; Lammich, S.; Multhaup, G.; Haass, C. J. Biol. Chem. 2000, 275, 30849.
58. Marcinkeviciene, J.; Luo, Y.; Graciani, N. R.; Combs, A. P.; Copeland, R. A. J. Biol. Chem. 2001, 276, 23790.
59. Leung, D.; Abbenante, G.; Fairlie, D. P. J. Med. Chem. 2000, 43, 305.
60. Farzan, M.; Schnitzler, C. E.; Vasilieva, N.; Leung, D.; Choe, H. PNAS 2000, 97, 9712.
61. Yan, R.; Munzner, J. B.; Shuck, M. E.; Bienkowski, M. J. J. Biol. Chem. 2001, 276, 34019.
62. Westmeyer, G. G.; Willem, M.; Lichtenthaler, S. F.; Lurman, G.; Multhaup, G.; Assfalg-Machleidt, I.; Reiss, K.; Saftig, P.; Haass, C. J. Biol. Chem. 2004, 279, 53205.
63. Fischer, F.; Molinari, M.; Bodendorf, U.; Paganetti, P. J. Neurochem. 2002, 80, 1079.
64. Luo, Y.; Bolon, B.; Kahn, S.; Bennett, B. D.; Babu-Khan, S.; Denis, P.; Fan, W.; Kha, H.; Zhang, J.; Gong, Y.; Martin, L.; Louis, J.-C.; Yan, Q.; Richards, W. G.; Citron, M.; Vassar, R. Nat. Neurosci. 2001, 4, 231.
65. Vassar, R. J. Mol. Neurosci. 2001, 17, 157.
66. Gruninger-Leitch, F.; Schlatter, D.; Kung, E.; Nelbock, P.; Dobeli, H. J. Biol. Chem. 2002, 277, 4687.
67. Roggo, S. Curr. Top. Med. Chem. 2002, 2, 359.
68. Dominguez, D. I.; Hartmann, D.; De Strooper, B. 2004, 1, 168.
69. Wolfe, M. S.; Haass, C. J. Biol. Chem. 2001, 276, 5413.
70. Ishiura, S. Dementia Jpn. 2000, 14, 236.
71. Citron, M. Trends Pharmacol. Sci. 2004, 25, 92.
72. Varghese, J.; Beck, J. P.; Bienkowski, M. J.; Sinha, S.; Heinrikson, R. L. J. Med. Chem. 2003, 46, 4625.
73. Schmidt, B. ChemBioChem 2003, 4, 366.
74. Hong, L.; Koelsch, G.; Lin, X.; Wu, S.; Terzyan, S.; Ghosh, A. K.; Zhang, X. C.; Tang, J. Science 2000, 290, 150.
75. Hong, L.; Turner, R. T. III.; Koelsch, G.; Shin, D.; Ghosh, A. K.; Tang, J. Biochemistry 2002, 41, 10963.
76. Hong, L.; Tang, J. Biochemistry 2004, 43, 4689.
77. Hong, L.; Turner, I. R. T.; Koelsch, G.; Ghosh, A. K.; Tang, J. Biochem. Soc. Trans. 2002, 30, 530.
78. Tung, J. S.; Davis, D. L.; Anderson, J. P.; Walker, D. E.; Mamo, S.; Jewett, N.; Hom, R. K.; Sinha, S.; Thorsett, E. D.; John, V. J. Med. Chem. 2002, 45, 259.
79. Shuto, D.; Kasai, S.; Kimura, T.; Liu, P.; Hidaka, K.; Hamada, T.; Shibakawa, S.; Hayashi, Y.; Hattori, C.; Szabo, B.; Ishiura, S.; Kiso, Y. Bioorg. Med. Chem. Lett. 2003, 13, 4273.
80. Tamamura, H.; Kato, T.; Otaka, A.; Fujii, N. Org. Biomol. Chem. 2003, 1, 2468.
81. Brady, S. F.; Singh, S.; Crouthamel, M.-C.; Holloway, M. K.; Coburn, C. A.; Garsky, V. M.; Bogusky, M.; Pennington, M. W.; Vacca, J. P.; Hazuda, D.; Lai, M.-T. Bioorg. Med. Chem. Lett. 2004, 14, 601.
82. Ghosh, A. K.; Bilcer, G.; Harwood, C.; Kawahama, R.; Shin, D.; Hussain, K. A.; Hong, L.; Loy, J. A.; Nguyen, C.; Koelsch, G.; Ermolieff, J.; Tang, J. J. Med. Chem. 2001, 44, 2865.
83. Kimura, T.; Shuto, D.; Kasai, S.; Liu, P.; Hidaka, K.; Hamada, T.; Hayashi, Y.; Hattori, C.; Asai, M.; Kitazume, S.; Saido, T. C.; Ishiura, S.; Kiso, Y. Bioorg. Med. Chem. Lett. 2004, 14, 1527.
84. Chen, S.-H.; Lamar, J.; Guo, D.; Kohn, T.; Yang, H.-C.; McGee, J.; Timm, D.; Erickson, J.; Yip, Y.; May, P.; McCarthy, J. Bioorg. Med. Chem. Lett. 2004, 14, 245.
85. Lamar, J.; Hu, J.; Bueno, A. B.; Yang, H.-C.; Guo, D.; Copp, J. D.; McGee, J.; Gitter, B.; Timm, D.; May, P.; McCarthy, J.; Chen, S.-H. Bioorg. Med. Chem. Lett. 2004, 14, 239.
86. Hu, B.; Fan, K. Y.; Bridges, K.; Chopra, R.; Lovering, F.; Cole, D.; Zhou, P.; Ellingboe, J.; Jin, G.; Cowling, R.; Bard, J. Bioorg. Med. Chem. Lett. 2004, 14, 3457.
87. Hom, R. K.; Fang, L. Y.; Mamo, S.; Tung, J. S.; Guinn, A. C.; Walker, D. E.; Davis, D. L.; Gailunas, A. F.; Thorsett, E. D.; Sinha, S.; Knops, J. E.; Jewett, N. E.; Anderson, J. P.; John, V. J. Med. Chem. 2003, 46, 1799.
88. Hom, R. K.; Gailunas, A. F.; Mamo, S.; Fang, L. Y.; Tung, J. S.; Walker, D. E.; Davis, D.; Thorsett, E. D.; Jewett, N. E.; Moon, J. B.; John, V. J. Med. Chem. 2004, 47, 158.
89. Maillaird, M.; Hom, C.; Gailunas, A.; Jagodzinska, B.; Fang, L. Y.; John, V.; Freskos, J. N.; Pulley, S. R.; Beck, J. P.; Tenbrink, R. E. Preparation of substituted amines to treat Alzheimer's disease. WO 200202512, 2002.
90. Beck, J. P.; Gailunas, A.; Hom, R.; Jagodzinska, B.; John, V.; Maillaird, M. Compounds to treat alzheimer's disease. WO 0202520, 2002.
91. Patel, S.; Vuillard, L.; Cleasby, A.; Murray, C. W.; Yon, J. J. Mol. Biol. 2004, 343, 407.
92. Uchikawa, O.; Aso, K.; Koike, T.; Tarui, N.; Hirai, K. Preparation of benzamide derivatives as β-secretase inhibitors. WO 2004014843, 2004.
93. Demont, E. H.; Faller, A.; MacPherson, D. T.; Milner, P. H.; Naylor, A.; Redshaw, S.; Stanway, S. J.; Vesey, D. R.; Walter, D. S. Preparation of hydroxyethylamine derivatives for the treatment of Alzheimer's disease. WO 2004050619, 2004.
94. Pulley, S. R.; Beck, J. P.; Tenbrink, R. E.; Jacobs, J. S. Preparation of macrocycles useful in the treatment of Alzheimer's disease. WO 2002100399, 2002.
95. Reeder, M. R. Processes for the synthesis of amino acid-related benzyl epoxides used in the production of pharmaceutical agents. WO 2002085877, 2002.
96. Tenbrink, R.; Maillard, M.; Warpehoski, M. Preparation of substituted hydroxyethyl-amines as β-secretase inhibitors. WO 0350073, 2003.
97. Fang, L. Y.; Hom, R.; John, V.; Maillaird, M. Preparation of substituted amines for treating Alzheimer's disease. WO 0202505, 2002.
98. Fang, L. Y.; John, V. Compounds to treat Alzheimer's disease. WO 0202506, 2002.
99. Fobian, Y. M.; Freskos, J. N.; Jagodzinska, B. A preparation of 1,3-diamino-2-hydroxypropane derivatives as β-secretase enzyme inhibitors. WO 2004022523, 2004.
100. Vuillard, L. M. M.; Patel, S. J.; Yon, J. R.; Cleasby, A.; Hamilton, B. J.; Shah, A. Crystal structure of human β-secretase mutants and drug discovery applications. WO 2004011641, 2004.
101. Yang, W. Preparation of amino carboxamide derivatives as aspartyl protease inhibitors. WO 2004147454, 2004.
102. Brockhaus, M.; Doebeli, H.; Grueninger, F.; Huguenin, P.; Kitas, E. A.; Nelboeck-Hochstetter, P. Fluorescence and competitive radioligand binding assays for identifying β-secretase inhibitors and for screening agents for treatment of Alzheimer's disease and cerebrovascular amyloidosis. US 2003125257, 2003.
103. Brockhaus, M.; Doebeli, H.; Grueninger, F.; Huguenin, P.; Kitas, E. A.; Nelboeck-Hochstetter, P. Assay for identifying beta secretase inhibitors. US 20030125257, 2003.
104. Miyamoto, M.; Matsui, J.; Fukumoto,H.;Tarui, N. Preparation of 2-[2-amino- or 2-(N-heterocyclyl)ethyl]-6-(4-biphenylylmethoxy)-tetralin derivatives as β secretase inhibitors. WO 0187293, 2001.
105. Qiao, L.; Etcheberrigaray, R. Preparation of phosphinylmethyl and phosphorylmethyl succinic and glutaric acid analogs as β-secretase inhibitors useful in the treatment of Alzheimer's disease. WO 2002096897, 2002.
106. Ramakrishna, N. V. S.; Kumar, E. K. S. V.; Kulkarni, A. S.; Jain, A. K.; Bhat, R. G.; Parikh, S.; Quadros, A.; Deuskar, N.; Kalakoti, B. S. Indian J. Chem., Sect. B: Org. Chem. Incl. Med. Chem. 2001, 40B, 539.
107. Bhisetti, G. R.; Saunders, J. O.; Murcko, M. A.; Lepre, C. A.; Britt, S. D.; Come, J. H.; Deninger, D. D.; Wang, T. Preparation of β-carbolines and other inhibitors of BACE-1 aspartic proteinase useful against Alzheimer's and other BACE-mediated diseases. WO 2002088101, 2002.
108. Park, H.; Lee, S. J. Am. Chem. Soc. 2003, 125, 16416.
109. Boss, C.; Bur, D.; Fischli, W.; Jenck, F.; Weller, T. Preparation of piperidines for the treatment of central nervous system disorders. WO 2004009549, 2004.
110. Boss, C.; Bur, D.; Fischli, W.; Jenck, F.; Weller, T. Preparation of substituted 3- and 4-(aminomethyl)piperidines for use as β-secretase inhibitors in the treatment of Alzheimer's disease. WO 2004002483, 2004.
111. Coburn, C. A.; Stachel, S. J.; Vacca, J. P. Preparation of phenylcarboxamide derivatives as β-secretase inhibitors for the treatment of Alzheimer's disease. WO 2004043916, 2004.
112. Coburn, C. A.; Stachel, S. J.; Vacca, J. P. Preparation of macrocyclic β-secretase inhibitors for treatment of Alzheimer's disease. WO 2004062625, 2004.
113. Holloway, M. K.; Culberson, J. C.; Shpungin, J.; Munshi, S.; Coburn, C. A.; Stachel, S. J.; Jones, K. G.; Loutzenhiser, E.; Gregro, A. R.; Lai, M.-T.; Crouthamel, M.-C.; Pietrak, B. L. Abstracts of Papers, 228th ACS National Meeting, Philadelphia, PA, United States, August 22-26, 2004 2004.
114. Rajamani, R.; Reynolds, C. H. Bioorg. Med. Chem. Lett. 2004, 14, 4843.
115. Rajamani, R.; Reynolds, C. H. J. Med. Chem. 2004, 47, 5159.
116. Tounge, B. A.; Reynolds, C. H. J. Med. Chem. 2003, 46, 2074.
117. 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. J. Med. Chem. 2004, 47, 6117.
118. Stachel, S. J.; Coburn, C. A.; Steele, T. G.; Jones, K. G.; Loutzenhiser, E. F.; Gregro, A. R.; Rajapakse, H. A.; Lai, M.-T.; Crouthamel, M.-C.; Xu, M.; Tugusheva, K.; Lineberger, J. E.; Pietrak, B. L.; Espeseth, A. S.; Shi, X.-P.; Chen-Dodson, E.; Holloway, M. K.; Munshi, S.; Simon, A. J.; Kuo, L.; Vacca, J. P. J. Med. Chem. 2004, 47, 6447.
119. Willems, H. Preparation of piperazines as β-amyloid converting enzyme (BACE) inhibitors for the treatment of Alzheimer's disease. WO 2004020422, 2004.
120. Willems, H.; Gordon, R. Protected amino acid derivatives for the treatment of Alzheimer's disease. GB 2392443, 2004.
121. Willems, H.; Harris, W.; John, D. E. A preparation of triazinoindole derivatives as inhibitors of β-secretase (BACE), useful in the treatment of Alzheimer's disease. WO 2004063196, 2004.
122. Willems, H.; Harris, W. H. Preparation of N-sulfonyl amino acid derivatives for the treatment of Alzheimer's disease. WO 2004020402, 2004.
123. De Strooper, B.; Annaert, W. J. Cell Biol. 2001, 152, F17.
124. Herreman, A.; Serneels, L.; Annaert, W.; Collen, D.; Schoonjans, L.; Strooper, B. D. Nat. Cell Biol. 2000, 2, 461.
125. Figueroa, D. J.; Morris, J. A.; Ma, L.; Kandpal, G.; Chen, E.; Li, Y. M.; Austin, C. P. Neurobiol. Dis. 2002, 9, 49.
126. Kopan, R.; Ilagan, M. X. G. Nat. Rev. Mol. Cell Biol. 2004, 5, 499.
127. Shirotani, K.; Edbauer, D.; Prokop, S.; Haass, C.; Steiner, H. J. Biol. Chem. 2004, 279, 41340.
128. Cousin, E.; Hannequin, D.; Mace, S.; Dubois, B.; Ricard, S.; Genin, E.; Brun, C.; Chansac, C.; Pradier, L.; Frebourg, T.; Brice, A.; Campion, D.; Deleuze, J.-F. Neurosci. Lett. 2003, 353, 153.
129. Edbauer, D.; Winkler, E.; Regula, J. T.; Pesold, B.; Steiner, H.; Haass, C. Nat. Cell Biol. 2003, 5, 486.
130. Turner, R. T.; Loy, J. A.; Nguyen, C.; Devasamudram, T.; Ghosh, A. K.; Koelsch, G.; Tang, J. Biochemistry 2002, 41, 8742.
131. Farmery, M. R.; Tjernberg, L. O.; Pursglove, S. E.; Bergman, A.; Winblad, B.; Naslund, J. J. Biol. Chem. 2003, 278, 24277.
132. Weihofen, A.; Binns, K.; Lemberg, M. K.; Ashman, K.; Martoglio, B. Science 2002, 296, 2215.
133. Lichtenthaler, S. F.; Wang, R.; Grimm, H.; Uljon, S. U.; Masters, C. L.; Beyreuther, K. PNAS 1999, 96, 3053.
134. Kaether, C.; Capell, A.; Edbauer, D.; Winkler, E.; Novak, B.; Steiner, H.; Haass, C. EMBO J. 2004, 23, 4738.
135. Wolfe, M. S.; Xia, W.; Ostaszewski, B. L.; Diehl, T. S.; Kimberly, W. T.; Selkoe, D. J. Nature 1999, 398, 513.
136. Kimberly, W. T.; Xia, W.; Rahmati, T.; Wolfe, M. S.; Selkoe, D. J. J. Biol. Chem. 2000, 275, 3173.
137. Paris, D.; Mullan, M. J. Anti-angiogenic and anti-tumoral properties of beta and gamma secretase inhibitors. WO 2004073630, 2004.
138. Kan, T.; Tominari, Y.; Rikimaru, K.; Morohashi, Y.; Natsugari, H.; Tomita, T.; Iwatsubo, T.; Fukuyama, T. Bioorg. Med. Chem. Lett. 2004, 14, 1983.
139. Shearman, M. S.; Beher, D.; Clarke, E. E.; Lewis, H. D.; Harrison, T.; Hunt, P.; Nadin, A.; Smith, A. L.; Stevenson, G.; Castro, J. L. Biochemistry 2000, 39, 8698.
140. Nadin, A. J.; Stevenson, G. I. Preparation of peptides as γ-secretase inhibitors. WO 0177144, 2001.
141. Nadin, A.; Owens, A. P.; Castro, J. L.; Harrison, T.; Shearman, M. S. Bioorg. Med. Chem. Lett. 2003, 13, 37.
142. Nadin, A.; López, J. M. S.; Neduvelil, J. G.; Thomas, S. R. Tetrahedron 2001, 57, 1861.
143. Moore, C. L.; Leatherwood, D. D.; Diehl, T. S.; Selkoe, D. J.; Wolfe, M. S. J. Med. Chem. 2000, 43, 3434.
144. Wolfe, M. S. J. Mol. Neurosci. 2001, 17, 199.
145. Campbell, W. A.; Iskandar, M. K.; Reed, M. L.; Xia, W. Biochemistry 2002, 41, 3372.
146. Petit, A.; Bihel, F.; Alves da Costa, C.; Pourquie, O.; Checler, F.; Kraus, J.-L. Nat. Cell Biol. 2001, 3, 507.
147. Zhang, L.; Song, L.; Terracina, G.; Liu, Y.; Pramanik, B.; Parker, E. Biochemistry 2001, 40, 5049.
148. Berezovska, O.; Jack, C.; McLean, P.; Aster, J. C.; Hicks, C.; Xia, W.; Wolfe, M. S.; Kimberly, W. T.; Weinmaster, G.; Selkoe, D. J.; Hyman, B. T. J. Neurochem. 2000, 75, 583.
149. Wolfe, M. S.; Xia, W.; Moore, C. L.; Leatherwood, D. D.; Ostaszewski, B.; Rahmati, T.; Donkor, I. O.; Selkoe, D. J. Biochemistry 1999, 38, 4720.
150. Wolfe, M. S.; Citron, M.; Diehl, T. S.; Xia, W.; Donkor, I. O.; Selkoe, D. J. J. Med. Chem. 1998, 41, 6.
151. Doerfler, P.; Shearman, M. S.; Perlmutter, R. M. PNAS 2001, 98, 9312.
152. Roncarati, R.; Sestan, N.; Scheinfeld, M. H.; Berechid, B. E.; Lopez, P. A.; Meucci, O.; McGlade, J. C.; Rakic, P.; D'Adamio, L. PNAS 2002, 99, 7102.
153. Das, C.; Wolfe, M. S.; Tsai, J.-Y.; Diehl, T. S. Abstracts of Papers, 223rd ACS National Meeting, Orlando, FL, United States, April 7-11, 2002 2002, MEDI.
154. Wolfe, M. S. Helical peptidomimetics as inhibitors of β-amyloid production, and therapeutic use thereof. WO 2003068168, 2003.
155. Bihel, F.; Das, C.; Bowman, M. J.; Wolfe, M. S. J. Med. Chem. 2004, 47, 3931.
156. Bakshi, P.; Wolfe, M. S. J. Med. Chem. 2004, 47, 6485.
157. McLendon, C.; Xin, T.; Ziani-Cherif, C.; Murphy, M. P.; Findlay, K. A.; Lewis, P. A.; Pinnix, I.; Sambamurti, K.; Wang, R.; Fauq, A.; Golde, T. E. FASEB 2000, 14, 2383.
158. Castro Pineiro, J. L.; Smith, A. L.; Stevenson, G. I. γ-Secretase inhibitors for treatment or prevention of Alzheimer's disease. WO 0166564, 2001.
159. Esler, W. P.; Kimberly, W. T.; Ostaszewski, B. L.; Ye, W.; Diehl, T. S.; Selkoe, D. J.; Wolfe, M. S. PNAS 2002, 99, 2720.
160. Dovey, H. F.; John, V.; Anderson, J. P.; Chen, L. Z.; De Saint Andrieu, P.; Fang, L. Y.; Freedman, S. B.; Folmer, B.; Goldbach, E.; Holsztynska, E. J.; Hu, K. L.; Johnson-Wood, K. L.; Kennedy, S. L.; Kholodenko, D.; Knops, J. E.; Latimer, L. H.; Lee, M.; Liao, Z.; Lieberburg, I. M.; Motter, R. N.; Mutter, L. C.; Nietz, J.; Quinn, K. P.; Sacchi, K. L.; Seubert, P. A.; Shopp, G. M.; Thorsett, E. D.; Tung, J. S.; Wu, J.; Yang, S.; Yin, C. T.; Schenk, D. B.; May, P. C.; Altstiel, L. D.; Bender, M. H.; Boggs, L. N.; Britton, T. C.; Clemens, J. C.; Czilli, D. L.; Dieckman-McGinty, D. K.; Droste, J. J.; Fuson, K. S.; Gitter, B. D.; Hyslop, P. A.; Johnstone, E. M.; Li, W. Y.; Little, S. P.; Mabry, T. E.; Miller, F. D.; Ni, B.; Nissen, J. S.; Porter, W. J.; Potts, B. D.; Reel, J. K.; Stephenson, D.; Su, Y.; Shipley, L. A.; Whitesitt, C. A.; Yin, T.; Audia, J. E. J. Neurochem. 2001, 76, 173.
161. Audia, J. E.; Britton, T. C.; Droste, J. J.; Folmer, B. K.; Huffman, G. W.; John, V.; Latimer, L. H.; Mabry, T. E.; Nissen, J. S.; Porter, W. J.; Reel, J. K.; Thorsett, E. D.; Tung, J. S.; Eid, C. N.; Scott, W. L. Preparation of N-(phenylacetyl)di- and tripeptide derivatives for inhibiting β-amyloid peptide release. WO 9822494, 1998.
162. Audia, J. E.; Britton, T. C.; Droste, J. J.; Folmer, B. K.; Huffman, G. W.; Varghese, J.; Latimer, L. H.; Mabry, T. E.; Nissen, J. S.; Porter, W. J.; Reel, J. K.; Thorsett, E. D.; Tung, J. S.; Wu, J.; Eid, C. N.; Scott, W. L. Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis. US 6191166, 2001.
163. Larbig, G.; Zall, A.; Schmidt, B. Helvetica Chimica Acta 2004, 87, 2334.
164. Garofalo, A. W.; Wone, D. W. G.; Phuc, A.; Audia, J. E.; Bales, C. A.; Dovey, H. F.; Dressen, D. B.; Folmer, B.; Goldbach, E. G.; Guinn, A. C.; Latimer, L. H.; Mabry, T. E.; Nissen, J. S.; Pleiss, M. A.; Sohn, S.; Thorsett, E. D.; Tung, J. S.; Wu, J. Bioorg. Med. Chem. Lett. 2002, 12, 3051-3053.
165. Hutton, M.; Lewis, J.; Dickson, D.; Yen, S. H.; McGowan, E. Trends Mol. Med. 2001, 7, 467.
166. Hadland, B. K.; Manley, N. R.; Su, D.-M.; Longmore, G. D.; Moore, C. L.; Wolfe, M. S.; Schroeter, E. H.; Kopan, R. PNAS 2001, 98, 7487.
167. Wong, G. T.; Manfra, D.; Poulet, F. M.; Zhang, Q.; Josien, H.; Bara, T.; Engstrom, L.; Pinzon-Ortiz, M.; Fine, J. S.; Lee, H.-J. J.; Zhang, L.; Higgins, G. A.; Parker, E. M. J. Biol. Chem. 2004, 279, 12876.
168. Iwata, N.; Tsubuki, S.; Takaki, Y.; Shirotani, K.; Lu, B.; Gerard, N. P.; Gerard, C.; Hama, E.; Lee, H.-J.; Saido, T. C. Science 2001, 292, 1550.
169. Iwata, N.; Tsubuki, S.; Takaki, Y.; Watanabe, K.; Sekiguchi, M.; Hosoki, E.; Kawashima-Morishima, M.; Lee, H.-J.; Hama, E.; Sekine-Aizawa, Y.; Saido, T. C. Nat. Med. 2000, 6, 143.
170. Iwata, N.; Saido, T. C. Dementia Jpn. 2000, 14, 80.
171. Abraham, C. R.; McGraw, W. T.; Slot, F.; Yamin, R. Ann. N. Y. Acad. Sci. 2000, 920, 245.
172. Smith, D. W.; Munoz, B.; Srinivasan, K.; Bergstrom, C. P.; Chaturvedula, P. V.; Deshpande, M. S.; Keavy, D. J.; Lau, W. Y.; Parker, M. F.; Sloan, C. P.; Wallace, O. B.; Wang, H. H. Preparation of sulfonamide derivs. as amyloidβ production inhibitors useful in treating or preventing diseases related to Aβ. WO 0050391, 2000.
173. Rishton, G. M.; Retz, D. M.; Tempest, P. A.; Novotny, J.; Kahn, S.; Treanor, J. J. S.; Lile, J. D.; Citron, M. J. Med. Chem. 2000, 43, 2297.
174. Belanger, P. C.; Collins, I. J.; Hannam, J. C.; Harrison, T.; Lewis, S. J.; Madin, A.; McIver, E. G.; Nadin, A. J.; Neduvelil, J. G.; Shearman, M. S.; Smith, A. L.; Sparey, T. J.; Stevenson, G. I.; Teall, M. R. Synthesis of sulfonamido-substituted bridged bicycloalkyl derivatives as γ-secretase inhibitors. WO 0170677, 2001.
175. Olson, R. E.; Maduskuie, T. P.; Thomas, L. A. Preparation of succinoylamino-azepinones and related compounds as inhibitors of Aβ-peptide production. WO 0007995, 2000.
176. Seiffert, D.; Bradley, J. D.; Rominger, C. M.; Rominger, D. H.; Yang, F.; Meredith, J. E. Jr.; Wang, Q.; Roach, A. H.; Thompson, L. A.; Spitz, S. M.; Higaki, J. N.; Prakash, S. R.; Combs, A. P.; Copeland, R. A.; Arneric, S. P.; Hartig, P. R.; Robertson, D. W.; Cordell, B.; Stern, A. M.; Olson, R. E.; Zaczek, R. J. Biol. Chem. 2000, 275, 34086.
177. Thompson, L. A.; Han, A. Q. Preparation of amino lactam sulfonamides as inhibitors of Aβ-protein production. WO 0127108, 2001.
178. Thompson, L. A. Amino lactam sulfonamides as inhibitors of Aβ protein production. WO 0127091, 2001.
179. Teall, M. R. γ-secretase inhibitors. Us 20020013315, 2002.
180. Fuchs, K.; Romig, M.; Mendla, K.; Briem, H.; Fechteler, K. Preparation of novel imidazopyridines as β-amyloid formation inhibitors. WO 2002014313, 2002.
181. Himmelsbach, F.; Fuchs, K.; Briem, H.; Fechteler, K.; Kostka, M.; Dorner-Ciossek, C.; Bornemann, K.; Klinder, K. Preparation of diaminopyrimidines as inhibitors of β-amyloid formation or its release. WO 2003032994, 2003.
182. Otto, M.; Cepek, L.; Ratzka, P.; Doehlinger, S.; Boekhoff, I.; Wiltfang, J.; Irle, E.; Pergande, G.; Ellers-Lenz, B.; Windl, O.; Kretzschmar, H. A.; Poser, S.; Prange, H. Neurology 2004, 62, 714.
183. Churcher, I.; Williams, S.; Kerrad, S.; Harrison, T.; Castro, J. L.; Shearman, M. S.; Lewis, H. D.; Clarke, E. E.; Wrigley, J. D.; Beher, D.; Tang, Y. S.; Liu, W. J. Med. Chem. 2003, 46, 2275.
184. Churcher, I.; Ashton, K.; Butcher, J. W.; Clarke, E. E.; Harrison, T.; Lewis, H. D.; Owens, A. P.; Teall, M. R.; Williams, S.; Wrigley, J. D. Bioorg. Med. Chem. Lett. 2003, 13, 179.
185. Lewis, H. D.; Perez Revuelta, B. I.; Nadin, A.; Neduvelil, J. G.; Harrison, T.; Pollack, S. J.; Shearman, M. S. Biochemistry 2003, 42, 7580.
186. Sun, X.; Sato, S.; Murayama, O.; Murayama, M.; Park, J. M.; Yamaguchi, H.; Takashima, A. Neurosci. Lett. 2002, 321, 61.
187. Phiel, C. J.; Wilson, C. A.; Lee, V. M.; Klein, P. S. Nature 2003, 423, 435.
188. Cohen, P.; Goedert, M. Nat. Rev. Drug Discov. 2004, 3, 479.
189. Ryder, J.; Su, Y.; Liu, F.; Li, B.; Zhou, Y.; Ni, B. Biochem. Biophys. Res. Commun. 2003, 312, 922.
190. Eckert, G. P.; Wood, W. G.; Müller, W. E. J. Neural. Transm. 2004, in press.
191. Cucchiara, B.; Kasner, S. E. J. Neurol. Sci. 2001, 187, 81.
192. Fassbender, K.; Simons, M.; Bergmann, C.; Stroick, M.; Lutjohann, D.; Keller, P.; Runz, H.; Kuhl, S.; Bertsch, T.; Von Bergmann, K.; Hennerici, M.; Beyreuther, K.; Hartmann, T. PNAS 2001, 98, 5856.
193. Simons, M.; Keller, P.; Dichgans, J.; Schulz, J. B. Neurology 2001, 57, 1089.
194. Riddell, D. R.; Christie, G.; Hussain, I.; Dingwall, C. Curr. Biol. 2001, 11, 1298.
195. Kojro, E.; Gimpl, G.; Lammich, S.; Marz, W.; Fahrenholz, F. PNAS 2001, 98, 5815.
196. George, A. J.; Holsinger, R. M. D.; McLean, C. A.; Laughton, K. M.; Beyreuther, K.; Evin, G.; Masters, C. L.; Li, Q.-X. Neurobiol. Dis. 2004, 16, 124.
197. Refolo, L. M.; Pappolla, M. A.; LaFrancois, J.; Malester, B.; Schmidt, S. D.; Thomas-Bryant, T.; Tint, G. S.; Wang, R.; Mercken, M.; Petanceska, S. S.; Duff, K. E. Neurobiol. Dis. 2001, 8, 890.
198. Bayer, T. A.; Schaefer, S.; Simons, A.; Kemmling, A.; Kamer, T.; Tepest, R.; Eckert, A.; Schuessel, K.; Eikenberg, O.; Sturchler-Pierrat, C.; Abramowski, D.; Staufenbiel, M.; Multhaup, G. PNAS 2003, 100, 14187.
199. Regland, B.; Lehmann, W.; Abedini, I.; Blennow, K.; Jonsson, M.; Karlsson, I.; Sjoegren, M.; Wallin, A.; Xilinas, M.; Gottfries, C.-G. Dement. Geriatr. Cog. Disord. 2001, 12, 408.
200. Melov, S. Trends. Neurosci. 2002, 25, 121.
201. Treiber, C.; Simons, A.; Strauss, M.; Hafner, M.; Cappai, R.; Bayer, T. A.; Multhaup, G. J. Biol. Chem. 2004, 279, 51958.
202. Barnham, K. J.; Gautier, E. C. L.; Kok, G. B.; Krippner, G. Preparation of 8-hydroxy-quinolines for treatment of neurological conditions. WO 2004007461, 2004.
203. Khachaturian, Z. S. Neurobiol. Aging. 2002, 23, 509.
204. Papassotiropoulos, A.; Hock, C. Neurobiol. Aging 2002, 23, 513.
205. Papassotiropoulos, A.; Lutjohann, D.; Bagli, M.; Locatelli, S.; Jessen, F.; Buschfort, R.; Ptok, U.; Bjorkhem, I.; von Bergmann, K.; Heun, R. J. Psychiatr. Res. 2002, 36, 27.
206. Boss, M. A. Biochim. Biophysica Acta 2000, 1502, 188.
207. Teunissen, C. E.; de Vente, J.; Steinbusch, H. W.; De Bruijn, C. Neurobiol. Aging 2002, 23, 485.
208. Klunk, W. E. Neurobiol. Aging 2002, 23, 517.
209. Kawarabayashi, T.; Younkin, L. H.; Saido, T. C.; Shoji, M.; Ashe, K. H.; Younkin, S. G. J. Neurosci. 2001, 21, 372.
210. Couderc, R. Ann. Biol. Clin. 2000, 58, 581.
211. Montine, T. J.; Kaye, J. A.; Montine, K. S.; McFarland, L.; Morrow, J. D.; Quinn, J. F. Arch. Pathol. Lab. Med. 2001, 125, 510.
212. Pratico, D.; Clark, C. M.; Lee, V. M. Y.; Trojanowski, J. Q.; Rokach, J.; FitzGerald, G. A. Ann. Neurol. 2000, 48, 809.
213. Pratico, D.; Clark, C. M.; Liun, F.; Lee, V. Y.; Trojanowski, J. Q. Arch. Neurol. 2002, 59, 972.
214. Ripova, D.; Strunecka, A. Physiol. Res. (Prague, Czech Repub.) 2001, 50, 119.
215. Lee, D. H. S.; Reitz, A. B.; Plata-Salaman, C. R.; Wang, H.-Y. Method of diagnosing neurodegenerative disease. WO 0140261, 2001.
216. Gupta-Bansal, R.; Brunden, K. R. J. Neurochem. 1998, 70, 292.
217. Ashburn, T.; Hogyu, T. H.; McGuinness, B. F.; Lansbury, Jr. P. T. Chem. Biol. 1996, 3, 351.
218. Probst, A.; Heitz, P. U.; Ulrich, J. Virchows Archiv. A, Pathol. Anat. Histol. 1980, 388, 327.
219. Klunk, W. E.; Debnath, M. L.; Pettegrew, J. W. Neurobiol. Aging 1994, 15, 691.
220. Klunk, W. E.; Debnath, M. L.; Koros, A. M. C.; Pettegrew, J. W. Life Sci. 1998, 63, 1807.
221. Klunk, W. E.; Pettegrew, J. W.; Mathis, C. A. Jr. Azo compounds for the antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition. WO 9634853, 1996.
222. Klunk, W. E.; Pettegrew, J. W.; Mathis, C. A. Jr. Alkyl, alkenyl and alkynyl Chrysamine G derivatives for the antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition. WO 9847969, 1998.
223. Klunk, W. E.; Pettegrew, J. W.; Mathis, C. A. Jr. Compounds for the antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition. WO 9924394, 1999.
224. Klunk, W. E.; Wang, Y.; Huang, G.-F.; Debnath, M. L.; Holt, D. P.; Mathis, C. A. Life Sci. 2001, 69, 1471.
225. Han, H.; Cho, C.-G.; Lansbury, P. T. Jr. J. Am. Chem. Soc. 1996, 118, 4506.
226. Link, C. D.; Johnson, C. J.; Fonte, V.; Paupard, M. C.; Hall, D. H.; Styren, S.; Mathis, C. A.; Klunk, W. E. Neurobiol. Aging 2001, 22, 217.
227. Caltech; Magnetic resonance imaging agents for in vivo labeling and detection of amyloid deposits. WO 028441, 2002.
228. Skovronsky, D. M.; Zhang, B.; Kung, M.-P.; Kung, H. F.; Trojanowski, J. Q.; Lee, V. M.-Y. PNAS 2000, 97, 7609-7614.
229. Zhuang, Z. P.; Kung, M. P.; Hou, C.; Skovronsky, D. M.; Gur, T. L.; Ploessl, K.; Trojanowski, J. Q.; Lee, V. M. Y.; Kung, H. F. J. Med. Chem. 2001, 44, 1905.
230. Okamura, N.; Suemoto, T.; Shimadzu, H.; Suzuki, M.; Shiomitsu, T.; Akatsu, H.; Yamamoto, T.; Staufenbiel, M.; Yanai, K.; Arai, H.; Sasaki, H.; Kudo, Y.; Sawada, T. J. Neurosci. 2004, 24, 2535.
231. Kung, M.-P.; Hou, C.; Zhuang, Z.-P.; Skovronsky, D.; Kung, H. F. Brain Res. 2004, 1025, 98.
232. Mathis, C. A.; Wang, Y.; Holt, D. P.; Huang, G. F.; Debnath, M. L.; Klunk, W. E. J. Med. Chem. 2003, 46, 2740.
233. Wilson, A. A.; Garcia, A.; Chestakova, A.; Kung, H.; Houle, S. J. Labelled Comp. Radiopharm. 2004, 47, 679.
234. Wang, Y.; Klunk, W. E.; Debnath, M. L.; Huang, G.-F.; Holt, D. P.; Li, S.; Mathis, C. A. J. Mol. Neurosci. 2004, 24, 55.
235. Agdeppa, E. D.; Kepe, V.; Liu, J.; Flores-Torres, S.; Satyamurthy, N.; Petric, A.; Cole, G. M.; Small, G. W.; Huang, S.-C.; Barrio, J., J. Neurosci. 2001, 21, RC189/1.
236. Cai, L.; Chin, F. T.; Pike, V. W.; Toyama, H.; Liow, J.-S.; Zoghbi, S. S.; Modell, K.; Briard, E.; Shetty, H. U.; Sinclair, K.; Donohue, S.; Tipre, D.; Kung, M.-P.; Dagostin, C.; Widdowson, D. A.; Green, M.; Gao, W.; Herman, M. M.; Ichise, M.; Innis, R. B. J. Med. Chem. 2004, 47, 2208.
237. Klunk, W. E.; Engler, H.; Nordberg, A.; Wang, Y.; Blomqvist, G.; Holt, D. P.; Bergstrom, M.; Savitcheva, I.; Huang, G.-f.; Estrada, S.; Ausen, B.; Debnath, M. L.; Barletta, J.; Price, J. C.; Sandell, J.; Lopresti, B. J.; Wall, A.; Koivisto, P.; Antoni, G.; Mathis, C. A.; Langstrom, B. Ann. Neurol. 2004, 55, 306.
238. Shoghi-Jadid, K.; Small, G. W.; Agdeppa, E. D.; Kepe, V.; Ercoli, L. M.; Siddarth, P.; Read, S.; Satyamurthy, N.; Petric, A.; Huang, S. C.; Barrio, J. R. Am. J. Geriatr. Psychiatry 2002, 10, 24.
239. Enguehard, C.; Allouchi, H.; Gueiffier, A.; Buchwald, S. L. J. Org. Chem. 2003, 68, 4367.
240. Enguehard, C.; Allouchi, H.; Gueiffier, A.; Buchwald, S. L. J. Org. Chem. 2003, 68, 5614.
241. Manas, E. S.; Unwalla, R. J.; Xu, Z. B.; Malamas, M. S.; Miller, C. P.; Harris, H. A.; Hsiao, C.; Akopian, T.; Hum, W.-T.; Malakian, K.; Wolfrom, S.; Bapat, A.; Bhat, R. A.; Stahl, M. L.; Somers, W. S.; Alvarez, J. C. J. Am. Chem. Soc. 2004, 126, 15106.
242. Barlaam, B.; Bernstein, P.; Dantzman, C.; Warwick, P. Preparation of benzoxazoles and benzothiazoles as selective ligands for human β-estrogen receptor. WO 2002051821, 2002.
243. Lockhart, A.; Ye, L.; Judd, D. B.; Merritt, A. T.; Lowe, P.; Morgenstern, J. L.; Hong, G.; Gee, A. D.; Brown, J. J. Biol. Chem. 2004, 10.1074/jbc.M41205620.
244. Auberson, Y. Coumarines useful as biomarkers. WO 03074519, 2003.
245. Klunk, W. E.; Wang, Y.; Huang, G. F.; Debnath, M. L.; Holt, D. P.; Shao, L.; Hamilton, R. L.; Ikonomovic, M. D.; DeKosky, S. T.; Mathis, C. A. J. Neurosci. 2003, 23, 2086.
246. Zhao, G.; Mao, G.; Tan, J.; Dong, Y.; Cui, M.-Z.; Seong-Hun, K.; Xu, X. J. Biol. Chem. 2004, 279, 50647.
247. McLean, C. A.; Cherny, R. A.; Fraser, F. W.; Fuller, S. J.; Smith, M. J.; Beyreuther, K.; Bush, A. I.; Masters, C. L. Ann. Neurol. 1999, 46, 860.
248. apo: The protein component of an enzyme that is separable from the prosthetic group but that requires the prosthetic group to form the functioning holoenzyme.
249. Confaloni, A.; Terreni, L.; Piscopo, P.; Crestini, A.; Campeggi, L. M.; Frigerio, C. S.; Blotta, I.; Perri, M.; Di Natale, M.; Maletta, R.; Marcon, G.; Franceschi, M.; Bruni, A. C.; Forloni, G.; Cantafora, A. Neurosci. Lett. 2003, 353, 61.
250. Hunger, K. In Industrial Dyes, Wiley-VCH 2004, Weinheim. pp. 141
251. Puglielli, L.; Konopka, G.; Pack-Chung, E.M.; Ingano, L. A. M.; Berezovska, O.; Hyman, B. T.; Chang Ta, Y.; Tanzi, R.E.; Kovacs, D.
252. Puglielli, L.; Ellis, B. C.; Ingano, L. A. M.; Kovacs, D. M. J. Mol. Neurosci. 2004, 24, 93.