-
1
-
-
70349923038
-
Alzheimer's Disease: From Pathology to Therapeutic Approaches
-
Jakob-Roetne, R.; Jacobsen, H. Alzheimer's Disease: From Pathology to Therapeutic Approaches Angew. Chem., Int. Ed. 2009, 48, 3030-3059
-
(2009)
Angew. Chem., Int. Ed.
, vol.48
, pp. 3030-3059
-
-
Jakob-Roetne, R.1
Jacobsen, H.2
-
2
-
-
0026597063
-
Alzheimer's disease: The amyloid cascade hypothesis
-
Hardy, J. A.; Higgins, G. A. Alzheimer's disease: the amyloid cascade hypothesis Science 1992, 256, 184-185
-
(1992)
Science
, vol.256
, pp. 184-185
-
-
Hardy, J.A.1
Higgins, G.A.2
-
3
-
-
0028170818
-
Cell biology of the amyloid β-protein precursor and the mechanism of Alzheimer's disease
-
Selkoe, D. J. Cell biology of the amyloid β-protein precursor and the mechanism of Alzheimer's disease Annu. Rev. Cell Biol. 1994, 10, 373-403
-
(1994)
Annu. Rev. Cell Biol.
, vol.10
, pp. 373-403
-
-
Selkoe, D.J.1
-
4
-
-
0025753852
-
The molecular pathology of Alzheimer's disease
-
Selkoe, D. J. The molecular pathology of Alzheimer's disease Neuron 1991, 6, 487-498
-
(1991)
Neuron
, vol.6
, pp. 487-498
-
-
Selkoe, D.J.1
-
5
-
-
0034516988
-
Toward a comprehensive theory for Alzheimer's disease. Hypothesis: Alzheimer's disease is caused by the cerebral accumulation and cytotoxicity of amyloid β-protein
-
Selkoe, D. J. Toward a comprehensive theory for Alzheimer's disease. Hypothesis: Alzheimer's disease is caused by the cerebral accumulation and cytotoxicity of amyloid β-protein Ann. N. Y. Acad. Sci. 2000, 924, 17-25
-
(2000)
Ann. N. Y. Acad. Sci.
, vol.924
, pp. 17-25
-
-
Selkoe, D.J.1
-
6
-
-
77951776829
-
Alzheimer's disease: Strategies for disease modification
-
Citron, M. Alzheimer's disease: strategies for disease modification Nature Rev. Drug Discovery 2010, 9, 387-398
-
(2010)
Nature Rev. Drug Discovery
, vol.9
, pp. 387-398
-
-
Citron, M.1
-
7
-
-
0035159756
-
The β-secretase, BACE. A prime drug target for Alzheimer's disease
-
Vassar, R. The β-secretase, BACE. A prime drug target for Alzheimer's disease J. Mol. Neurosci. 2001, 17, 157-170
-
(2001)
J. Mol. Neurosci.
, vol.17
, pp. 157-170
-
-
Vassar, R.1
-
8
-
-
42149130900
-
BACE1 structure and function in health and Alzheimer's disease
-
Cole, S. L.; Vassar, R. BACE1 structure and function in health and Alzheimer's disease Curr. Alzheimer Res. 2008, 5, 100-120
-
(2008)
Curr. Alzheimer Res.
, vol.5
, pp. 100-120
-
-
Cole, S.L.1
Vassar, R.2
-
9
-
-
0035112647
-
BACE1 is the major beta-secretase for generation of Abeta peptides by neurons
-
Cai, H.; Wang, Y.; McCarthy, D.; Wen, H.; Borchelt, D. R.; Price, D. L.; Wong, P. C. BACE1 is the major beta-secretase for generation of Abeta peptides by neurons Nature Neurosci. 2001, 4, 233-234
-
(2001)
Nature Neurosci.
, vol.4
, 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
-
10
-
-
0035116273
-
Mice deficient in BACE1, the Alzheimer's β-secretase, have normal phenotype and abolished β-amyloid generation
-
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. Mice deficient in BACE1, the Alzheimer's β-secretase, have normal phenotype and abolished β-amyloid generation Nature Neurosci. 2001, 4, 231-232
-
(2001)
Nature Neurosci.
, vol.4
, pp. 231-232
-
-
Luo, Y.1
Bolon, B.2
Kahn, S.3
Bennett, B.D.4
Babu-Khan, S.5
Denis, P.6
Fan, W.7
Kha, H.8
Zhang, J.9
Gong, Y.10
Martin, L.11
Louis, J.-C.12
Yan, Q.13
Richards, W.G.14
Citron, M.15
Vassar, R.16
-
11
-
-
34548847452
-
Partial reduction of BACE1 has dramatic effects on Alzheimer plaque and synaptic pathology in APP transgenic mice
-
McConlogue, L.; Buttini, M.; Anderson, J. P.; Brigham, E. F.; Chen, K. S.; Freedman, S. B.; Games, D.; Johnson-Wood, K.; Lee, M.; Zeller, M.; Liu, W.; Motter, R.; Sinha, S. Partial reduction of BACE1 has dramatic effects on Alzheimer plaque and synaptic pathology in APP transgenic mice J. Biol. Chem. 2007, 282, 26326-26334
-
(2007)
J. Biol. Chem.
, vol.282
, pp. 26326-26334
-
-
McConlogue, L.1
Buttini, M.2
Anderson, J.P.3
Brigham, E.F.4
Chen, K.S.5
Freedman, S.B.6
Games, D.7
Johnson-Wood, K.8
Lee, M.9
Zeller, M.10
Liu, W.11
Motter, R.12
Sinha, S.13
-
12
-
-
80052656815
-
The Swedish APP mutation alters the effect of genetically reduced BACE1 expression on the APP processing
-
Rabe, S.; Reichwald, J.; Ammaturo, D.; de, S. B.; Saftig, P.; Neumann, U.; Staufenbiel, M. The Swedish APP mutation alters the effect of genetically reduced BACE1 expression on the APP processing J. Neurochem. 2011, 119, 231-239
-
(2011)
J. Neurochem.
, vol.119
, pp. 231-239
-
-
Rabe, S.1
Reichwald, J.2
Ammaturo, D.3
De, S.B.4
Saftig, P.5
Neumann, U.6
Staufenbiel, M.7
-
13
-
-
33845236399
-
Bace1 modulates myelination in the central and peripheral nervous system
-
Hu, X.; Hicks, C. W.; He, W.; Wong, P.; Macklin, W. B.; Trapp, B. D.; Yan, R. Bace1 modulates myelination in the central and peripheral nervous system Nature Neurosci. 2006, 9, 1520-1525
-
(2006)
Nature Neurosci.
, vol.9
, pp. 1520-1525
-
-
Hu, X.1
Hicks, C.W.2
He, W.3
Wong, P.4
MacKlin, W.B.5
Trapp, B.D.6
Yan, R.7
-
14
-
-
33750455150
-
Control of Peripheral Nerve Myelination by the β-Secretase BACE1
-
Willem, M.; Garratt, A. N.; Novak, B.; Citron, M.; Kaufmann, S.; Rittger, A.; DeStrooper, B.; Saftig, P.; Birchmeier, C.; Haass, C. Control of Peripheral Nerve Myelination by the β-Secretase BACE1 Science 2006, 314, 664-666
-
(2006)
Science
, vol.314
, pp. 664-666
-
-
Willem, M.1
Garratt, A.N.2
Novak, B.3
Citron, M.4
Kaufmann, S.5
Rittger, A.6
Destrooper, B.7
Saftig, P.8
Birchmeier, C.9
Haass, C.10
-
15
-
-
80052723784
-
Bace2 Is a β Cell-Enriched Protease that Regulates Pancreatic β Cell Function and Mass
-
Esterhazy, D.; Stuetzer, I.; Wang, H.; Rechsteiner, M. P.; Beauchamp, J.; Doebeli, H.; Hilpert, H.; Matile, H.; Prummer, M.; Schmidt, A.; Lieske, N.; Boehm, B.; Marselli, L.; Bosco, D.; Kerr-Conte, J.; Aebersold, R.; Spinas, G. A.; Moch, H.; Migliorini, C.; Stoffel, M. Bace2 Is a β Cell-Enriched Protease that Regulates Pancreatic β Cell Function and Mass Cell Metab. 2011, 14, 365-377
-
(2011)
Cell Metab.
, vol.14
, pp. 365-377
-
-
Esterhazy, D.1
Stuetzer, I.2
Wang, H.3
Rechsteiner, M.P.4
Beauchamp, J.5
Doebeli, H.6
Hilpert, H.7
Matile, H.8
Prummer, M.9
Schmidt, A.10
Lieske, N.11
Boehm, B.12
Marselli, L.13
Bosco, D.14
Kerr-Conte, J.15
Aebersold, R.16
Spinas, G.A.17
Moch, H.18
Migliorini, C.19
Stoffel, M.20
more..
-
16
-
-
0033518251
-
Purification and cloning of amyloid precursor protein β-secretase from human brain
-
Sinha, S.; Anderson, J. P.; Barbour, R.; Basi, G. S.; Caccavello, R.; Davis, D.; Doan, M.; Dovey, H. F.; Frigon, N.; Hong, J.; Jacobson-Croak, K.; Jewett, N.; Keim, P.; Knops, J.; Lieberburg, I.; Power, M.; Tan, H.; Tatsuno, G.; Tung, J.; Schenk, D.; Seubert, P.; Suomensaari, S. M.; Wang, S.; Walker, D.; Zhao, J.; McConlogue, L.; John, V. Purification and cloning of amyloid precursor protein β-secretase from human brain Nature 1999, 402, 537-540
-
(1999)
Nature
, vol.402
, pp. 537-540
-
-
Sinha, S.1
Anderson, J.P.2
Barbour, R.3
Basi, G.S.4
Caccavello, R.5
Davis, D.6
Doan, M.7
Dovey, H.F.8
Frigon, N.9
Hong, J.10
Jacobson-Croak, K.11
Jewett, N.12
Keim, P.13
Knops, J.14
Lieberburg, I.15
Power, M.16
Tan, H.17
Tatsuno, G.18
Tung, J.19
Schenk, D.20
Seubert, P.21
Suomensaari, S.M.22
Wang, S.23
Walker, D.24
Zhao, J.25
McConlogue, L.26
John, V.27
more..
-
17
-
-
0033595706
-
β-Secretase cleavage of Alzheimer's amyloid precursor protein by the transmembrane aspartic protease BACE
-
Vassar, R.; Bennett, B. D.; Babu-Khan, S.; Kahn, S.; Mendiaz, E. A.; Denis, P.; Teplow, D. B.; Ross, S.; Amarante, P.; Loeloff, R.; Luo, Y.; Fisher, S.; Fuller, J.; Edenson, S.; Lile, J.; Jarosinski, M. A.; Biere, A. L.; Curran, E.; Burgess, T.; Louis, J.-C.; Collins, F.; Treanor, J.; Rogers, G.; Citron, M. 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.D.2
Babu-Khan, S.3
Kahn, S.4
Mendiaz, E.A.5
Denis, P.6
Teplow, D.B.7
Ross, S.8
Amarante, P.9
Loeloff, R.10
Luo, Y.11
Fisher, S.12
Fuller, J.13
Edenson, S.14
Lile, J.15
Jarosinski, M.A.16
Biere, A.L.17
Curran, E.18
Burgess, T.19
Louis, J.-C.20
Collins, F.21
Treanor, J.22
Rogers, G.23
Citron, M.24
more..
-
18
-
-
0033518264
-
Membrane-anchored aspartyl protease with Alzheimer's disease β-secretase activity
-
Yan, R.; Bienkowski, M. J.; Shuck, M. E.; Miao, H.; Tory, M. C.; Pauley, A. M.; Brashler, J. R.; Stratman, N. C.; Mathews, W. R.; Buhl, A. E.; Carter, D. B.; Tomasselli, A. G.; Parodi, L. A.; Heinrikson, R. L.; Gurney, M. E. 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.J.2
Shuck, M.E.3
Miao, H.4
Tory, M.C.5
Pauley, A.M.6
Brashler, J.R.7
Stratman, N.C.8
Mathews, W.R.9
Buhl, A.E.10
Carter, D.B.11
Tomasselli, A.G.12
Parodi, L.A.13
Heinrikson, R.L.14
Gurney, M.E.15
-
19
-
-
0034652309
-
Human aspartic protease memapsin 2 cleaves the β-secretase site of β-amyloid precursor protein
-
Lin, X.; Koelsch, G.; Wu, S.; Downs, D.; Dashti, A.; Tang, J. Human aspartic protease memapsin 2 cleaves the β-secretase site of β-amyloid precursor protein Proc. Natl. Acad. Sci. U. S. A. 2000, 97, 1456-1460
-
(2000)
Proc. Natl. Acad. Sci. U. S. A.
, vol.97
, pp. 1456-1460
-
-
Lin, X.1
Koelsch, G.2
Wu, S.3
Downs, D.4
Dashti, A.5
Tang, J.6
-
20
-
-
0033382226
-
Identification of a Novel Aspartic Protease (Asp 2) as β-Secretase
-
Hussain, I.; Powell, D.; Howlett, D. R.; Tew, D. G.; Meek, T. D.; Chapman, C.; Gloger, I. S.; Murphy, K. E.; Southan, C. D.; Ryan, D. M.; Smith, T. S.; Simmons, D. L.; Walsh, F. S.; Dingwall, C.; Christie, G. Identification of a Novel Aspartic Protease (Asp 2) as β-Secretase Mol. Cell. Neurosci. 1999, 14, 419-427
-
(1999)
Mol. Cell. Neurosci.
, vol.14
, pp. 419-427
-
-
Hussain, I.1
Powell, D.2
Howlett, D.R.3
Tew, D.G.4
Meek, T.D.5
Chapman, C.6
Gloger, I.S.7
Murphy, K.E.8
Southan, C.D.9
Ryan, D.M.10
Smith, T.S.11
Simmons, D.L.12
Walsh, F.S.13
Dingwall, C.14
Christie, G.15
-
21
-
-
84861512510
-
Small-molecule BACE1 inhibitors: A patent literature review (2006-2011)
-
Probst, G.; Xu, Y.-z. Small-molecule BACE1 inhibitors: a patent literature review (2006-2011) Expert Opin. Ther. Pat. 2012, 22, 511-540
-
(2012)
Expert Opin. Ther. Pat.
, vol.22
, pp. 511-540
-
-
Probst, G.1
Xu, Y.-Z.2
-
22
-
-
0017379735
-
Synthesis of 2-amino-5,6-dihydro-4 H -1,3-thiazines and related compounds by acid catalyzed cyclization of allylic isothiuronium salts
-
Cohen, N.; Banner, B. L. Synthesis of 2-amino-5,6-dihydro-4 H -1,3-thiazines and related compounds by acid catalyzed cyclization of allylic isothiuronium salts J. Heterocycl. Chem. 1977, 14, 717-723
-
(1977)
J. Heterocycl. Chem.
, vol.14
, pp. 717-723
-
-
Cohen, N.1
Banner, B.L.2
-
23
-
-
84878037706
-
-
WO2007049532A1.
-
Kobayashi, N.; Ueda, K.; Itoh, N.; Suzuki, S.; Sakaguchi, G.; Kato, A.; Yukimasa, A.; Hori, A.; Koriyama, Y.; Haraguchi, H.; Yasui, K.; Kanda, Y. Preparation of 2-aminodihydrothiazine derivatives as β-secretase inhibitors. WO2007049532A1, 2007.
-
(2007)
Preparation of 2-aminodihydrothiazine Derivatives As β-secretase Inhibitors
-
-
Kobayashi, N.1
Ueda, K.2
Itoh, N.3
Suzuki, S.4
Sakaguchi, G.5
Kato, A.6
Yukimasa, A.7
Hori, A.8
Koriyama, Y.9
Haraguchi, H.10
Yasui, K.11
Kanda, Y.12
-
24
-
-
84878034663
-
-
WO2009091016A1.
-
Suzuki, Y.; Motoki, T.; Kaneko, T.; Takaishi, M.; Ishida, T.; Takeda, K.; Kita, Y.; Yamamoto, N.; Khan, A.; Dimopoulos, P. Preparation of condensed aminodihydrothiazine derivatives as inhibitors of β-site APP-cleaving enzyme 1 (BACE1). WO2009091016A1, 2009.
-
(2009)
Preparation of Condensed Aminodihydrothiazine Derivatives As Inhibitors of β-site APP-cleaving Enzyme 1 (BACE1)
-
-
Suzuki, Y.1
Motoki, T.2
Kaneko, T.3
Takaishi, M.4
Ishida, T.5
Takeda, K.6
Kita, Y.7
Yamamoto, N.8
Khan, A.9
Dimopoulos, P.10
-
26
-
-
84878042374
-
-
WO2011115928A1.
-
Chen, J. J.; Zhong, W.; Yang, B.; Qian, W.; Lopez, P.; White, R.; Weiss, M.; Judd, T.; Powers, T.; Cheng, Y.; Dineen, T.; Epstein, O.; Low, J.; Marx, I.; Minatti, A. E.; Paras, N. A.; Potashman, M. Aminodihydrooxazine and aminodihydrothiazine spiro compounds as beta-secretase modulators and their their preparation and medical use. WO2011115928A1, 2011.
-
(2011)
Aminodihydrooxazine and Aminodihydrothiazine Spiro Compounds As Beta-secretase Modulators and Their Their Preparation and Medical Use
-
-
Chen, J.J.1
Zhong, W.2
Yang, B.3
Qian, W.4
Lopez, P.5
White, R.6
Weiss, M.7
Judd, T.8
Powers, T.9
Cheng, Y.10
Dineen, T.11
Epstein, O.12
Low, J.13
Marx, I.14
Minatti, A.E.15
Paras, N.A.16
Potashman, M.17
-
27
-
-
84878067329
-
-
WO2011123674A1.
-
Clark, C. T.; Cook, A.; Gunawardana, I. W.; Hunt, K. W.; Kallan, N. C.; Siu, M.; Thomas, A. A.; Volgraf, M. Spirotetrahydronaphthalene derivatives as β-secretase inhibitors and their preparation and use for the treatment of neurodegenerative diseases. WO2011123674A1, 2011.
-
(2011)
Spirotetrahydronaphthalene Derivatives As β-secretase Inhibitors and Their Preparation and Use for the Treatment of Neurodegenerative Diseases
-
-
Clark, C.T.1
Cook, A.2
Gunawardana, I.W.3
Hunt, K.W.4
Kallan, N.C.5
Siu, M.6
Thomas, A.A.7
Volgraf, M.8
-
28
-
-
81255143061
-
Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor
-
May, P. C.; Dean, R. A.; Lowe, S. L.; Martenyi, F.; Sheehan, S. M.; Boggs, L. N.; Monk, S. A.; Mathes, B. M.; Mergott, D. J.; Watson, B. M.; Stout, S. L.; Timm, D. E.; LaBell, E. S.; Gonzales, C. R.; Nakano, M.; Jhee, S. S.; Yen, M.; Ereshefsky, L.; Lindstrom, T. D.; Calligaro, D. O.; Cocke, P. J.; Hall, D. G.; Friedrich, S.; Citron, M.; Audia, J. E. Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor J. Neurosci. 2011, 31, 16507-16516
-
(2011)
J. Neurosci.
, vol.31
, pp. 16507-16516
-
-
May, P.C.1
Dean, R.A.2
Lowe, S.L.3
Martenyi, F.4
Sheehan, S.M.5
Boggs, L.N.6
Monk, S.A.7
Mathes, B.M.8
Mergott, D.J.9
Watson, B.M.10
Stout, S.L.11
Timm, D.E.12
Labell, E.S.13
Gonzales, C.R.14
Nakano, M.15
Jhee, S.S.16
Yen, M.17
Ereshefsky, L.18
Lindstrom, T.D.19
Calligaro, D.O.20
Cocke, P.J.21
Hall, D.G.22
Friedrich, S.23
Citron, M.24
Audia, J.E.25
more..
-
29
-
-
84878048906
-
BACE1 Inhibitors: A Head Group Scan on a Series of Amides. Submitted to
-
Woltering, T. J.; Wostl, W.; Hilpert, H.; Rogers-Evans, M.; Pinard, E.; Mayweg, A.; Banner, D. W.; Benz, J.; Narquizian, R.; Travagli, M.; Power, E.; Pollastrini, M.; Marconi, G.; Gabellieri, E.; Guba, W.; Mauser, H.; Andreini, M.; Jacobsen, H. BACE1 Inhibitors: A Head Group Scan on a Series of Amides. Submitted to Bioorg. Med. Chem. Lett.
-
Bioorg. Med. Chem. Lett.
-
-
Woltering, T.J.1
Wostl, W.2
Hilpert, H.3
Rogers-Evans, M.4
Pinard, E.5
Mayweg, A.6
Banner, D.W.7
Benz, J.8
Narquizian, R.9
Travagli, M.10
Power, E.11
Pollastrini, M.12
Marconi, G.13
Gabellieri, E.14
Guba, W.15
Mauser, H.16
Andreini, M.17
Jacobsen, H.18
-
30
-
-
0033534429
-
The tert -Butanesulfinyl Group: An Ideal Chiral Directing Group and Boc-Surrogate for the Asymmetric Synthesis and Applications of β-Amino Acids
-
Tang, T. P.; Ellman, J. A. The tert -Butanesulfinyl Group: An Ideal Chiral Directing Group and Boc-Surrogate for the Asymmetric Synthesis and Applications of β-Amino Acids J. Org. Chem. 1999, 64, 12-13
-
(1999)
J. Org. Chem.
, vol.64
, pp. 12-13
-
-
Tang, T.P.1
Ellman, J.A.2
-
31
-
-
0141454899
-
Convenient Asymmetric Synthesis of β-Substituted α,α-Difluoro-β-amino Acids via Reformatskii Reaction between Davis' N -Sulfinylimines and Ethyl Bromodifluoroacetate
-
Sorochinsky, A.; Voloshin, N.; Markovsky, A.; Belik, M.; Yasuda, N.; Uekusa, H.; Ono, T.; Berbasov, D. O.; Soloshonok, V. A. Convenient Asymmetric Synthesis of β-Substituted α,α-Difluoro-β-amino Acids via Reformatskii Reaction between Davis' N -Sulfinylimines and Ethyl Bromodifluoroacetate J. Org. Chem. 2003, 68, 7448-7454
-
(2003)
J. Org. Chem.
, vol.68
, pp. 7448-7454
-
-
Sorochinsky, A.1
Voloshin, N.2
Markovsky, A.3
Belik, M.4
Yasuda, N.5
Uekusa, H.6
Ono, T.7
Berbasov, D.O.8
Soloshonok, V.A.9
-
32
-
-
84878059669
-
-
WO2008133274A1.
-
Tamura, Y.; Suzuki, S.; Tada, Y.; Yonezawa, S.; Fujikoshi, C.; Matsumoto, S.; Kooriyama, Y.; Ueno, T. Preparation of aminodihydrothiazine derivatives as BACE1 inhibitors. WO2008133274A1, 2008.
-
(2008)
Preparation of Aminodihydrothiazine Derivatives As BACE1 Inhibitors
-
-
Tamura, Y.1
Suzuki, S.2
Tada, Y.3
Yonezawa, S.4
Fujikoshi, C.5
Matsumoto, S.6
Kooriyama, Y.7
Ueno, T.8
-
34
-
-
0032793232
-
Esterification of carboxylic acids with alcohols by 4-(4,6-dimethoxy-1,3, 5-triazin-2-yl)-4-methylmorpholinium chloride (DMTMM)
-
Kunishima, M.; Morita, J.; Kawachi, C.; Iwasaki, F.; Terao, K.; Tani, S. Esterification of carboxylic acids with alcohols by 4-(4,6-dimethoxy-1,3,5- triazin-2-yl)-4-methylmorpholinium chloride (DMTMM) Synlett 1999, 1255-1256
-
(1999)
Synlett
, pp. 1255-1256
-
-
Kunishima, M.1
Morita, J.2
Kawachi, C.3
Iwasaki, F.4
Terao, K.5
Tani, S.6
-
35
-
-
0002343032
-
Syntheses via isoxazolines. Part 18. Old concepts and recent results on stereoselection at isoxazoline ring and adjacent centers
-
Jaeger, V.; Muller, I.; Schohe, R.; Frey, M.; Ehrler, R.; Hafele, B.; Schroter, D. Syntheses via isoxazolines. Part 18. Old concepts and recent results on stereoselection at isoxazoline ring and adjacent centers Lect. Heterocycl. Chem. 1985, 8, 79-98
-
(1985)
Lect. Heterocycl. Chem.
, vol.8
, pp. 79-98
-
-
Jaeger, V.1
Muller, I.2
Schohe, R.3
Frey, M.4
Ehrler, R.5
Hafele, B.6
Schroter, D.7
-
36
-
-
84878085195
-
-
WO2011070029A1.
-
Banner, D.; Hilpert, H.; Mauser, H.; Mayweg, A. V.; Rogers-Evans, M. Preparation of oxazine derivatives as BACE2 inhibitors for treatment of diabetes. WO2011070029A1, 2011.
-
(2011)
Preparation of Oxazine Derivatives As BACE2 Inhibitors for Treatment of Diabetes
-
-
Banner, D.1
Hilpert, H.2
Mauser, H.3
Mayweg, A.V.4
Rogers-Evans, M.5
-
39
-
-
68149160053
-
Physicochemical drug properties associated with in vivo toxicological outcomes: A review
-
Price, D. A.; Blagg, J.; Jones, L.; Greene, N.; Wager, T. Physicochemical drug properties associated with in vivo toxicological outcomes: a review Expert Opin. Drug Metab. Toxicol. 2009, 5, 921-931
-
(2009)
Expert Opin. Drug Metab. Toxicol.
, vol.5
, pp. 921-931
-
-
Price, D.A.1
Blagg, J.2
Jones, L.3
Greene, N.4
Wager, T.5
-
40
-
-
65549132575
-
Pharmacological Promiscuity: Dependence on Compound Properties and Target Specificity in a Set of Recent Roche Compounds
-
Peters, J.-U.; Schnider, P.; Mattei, P.; Kansy, M. Pharmacological Promiscuity: Dependence on Compound Properties and Target Specificity in a Set of Recent Roche Compounds ChemMedChem 2009, 4, 680-686
-
(2009)
ChemMedChem
, vol.4
, pp. 680-686
-
-
Peters, J.-U.1
Schnider, P.2
Mattei, P.3
Kansy, M.4
-
41
-
-
84859269944
-
Can we discover pharmacological promiscuity early in the drug discovery process?
-
Peters, J.-U.; Hert, J.; Bissantz, C.; Hillebrecht, A.; Gerebtzoff, G.; Bendels, S.; Tillier, F.; Migeon, J.; Fischer, H.; Guba, W.; Kansy, M. Can we discover pharmacological promiscuity early in the drug discovery process? Drug Discovery Today 2012, 17, 325-335
-
(2012)
Drug Discovery Today
, vol.17
, pp. 325-335
-
-
Peters, J.-U.1
Hert, J.2
Bissantz, C.3
Hillebrecht, A.4
Gerebtzoff, G.5
Bendels, S.6
Tillier, F.7
Migeon, J.8
Fischer, H.9
Guba, W.10
Kansy, M.11
-
42
-
-
34848848499
-
Fluorine in Pharmaceuticals: Looking beyond Intuition
-
Mueller, K.; Faeh, C.; Diederich, F. Fluorine in Pharmaceuticals: Looking Beyond Intuition Science 2007, 317, 1881-1886
-
(2007)
Science
, vol.317
, pp. 1881-1886
-
-
Mueller, K.1
Faeh, C.2
Diederich, F.3
-
43
-
-
84878037081
-
-
WO2011069934A1.
-
Banner, D.; Guba, W.; Hilpert, H.; Mauser, H.; Mayweg, A. V.; Narquizian, R.; Pinard, E.; Power, E.; Rogers-Evans, M.; Woltering, T.; Wostl, W. Preparation of 2-amino-5,5-difluoro-5,6-dihydro-4 H -oxazine derivatives as BACE1 and/or BACE2 inhibitors. WO2011069934A1, 2011.
-
(2011)
Preparation of 2-amino-5,5-difluoro-5,6-dihydro-4 H -oxazine Derivatives As BACE1 And/or BACE2 Inhibitors
-
-
Banner, D.1
Guba, W.2
Hilpert, H.3
Mauser, H.4
Mayweg, A.V.5
Narquizian, R.6
Pinard, E.7
Power, E.8
Rogers-Evans, M.9
Woltering, T.10
Wostl, W.11
-
44
-
-
4644364822
-
Apo and Inhibitor Complex Structures of BACE (β-secretase)
-
Patel, S.; Vuillard, L.; Cleasby, A.; Murray, C. W.; Yon, J. Apo and Inhibitor Complex Structures of BACE (β-secretase) J. Mol. Biol. 2004, 343, 407-416
-
(2004)
J. Mol. Biol.
, vol.343
, pp. 407-416
-
-
Patel, S.1
Vuillard, L.2
Cleasby, A.3
Murray, C.W.4
Yon, J.5
-
45
-
-
33847029846
-
Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind β-secretase in a N-terminal 10s-loop down conformation
-
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.; Graham, S. L.; Vacca, 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
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 1788-1792
-
-
Stauffer, S.R.1
Stanton, M.G.2
Gregro, A.R.3
Steinbeiser, M.A.4
Shaffer, J.R.5
Nantermet, P.G.6
Barrow, J.C.7
Rittle, K.E.8
Collusi, D.9
Espeseth, A.S.10
Lai, M.-T.11
Pietrak, B.L.12
Holloway, M.K.13
McGaughey, G.B.14
Munshi, S.K.15
Hochman, J.H.16
Simon, A.J.17
Selnick, H.G.18
Graham, S.L.19
Vacca, J.P.20
more..
-
46
-
-
28844509722
-
Crystal Structure of Human BACE2 in Complex with a Hydroxyethylamine Transition-State Inhibitor
-
Ostermann, N.; Eder, J.; Eidhoff, U.; Zink, F.; Hassiepen, U.; Worpenberg, S.; Maibaum, J.; Simic, O.; Hommel, U.; Gerhartz, B. Crystal Structure of Human BACE2 in Complex with a Hydroxyethylamine Transition-State Inhibitor J. Mol. Biol. 2006, 355, 249-261
-
(2006)
J. Mol. Biol.
, vol.355
, pp. 249-261
-
-
Ostermann, N.1
Eder, J.2
Eidhoff, U.3
Zink, F.4
Hassiepen, U.5
Worpenberg, S.6
Maibaum, J.7
Simic, O.8
Hommel, U.9
Gerhartz, B.10
-
47
-
-
84863275812
-
Flexibility of the flap in the active site of BACE1 as revealed by crystal structures and molecular dynamics simulations
-
Xu, Y.; Li, M.-j.; Greenblatt, H.; Chen, W.; Paz, A.; Dym, O.; Peleg, Y.; Chen, T.; Shen, X.; He, J.; Jiang, H.; Silman, I.; Sussman, J. L. Flexibility of the flap in the active site of BACE1 as revealed by crystal structures and molecular dynamics simulations Acta Crystallogr., Sect. D: Biol. Crystallogr. 2012, D68, 13-25
-
(2012)
Acta Crystallogr., Sect. D: Biol. Crystallogr.
, vol.68
, pp. 13-25
-
-
Xu, Y.1
Li, M.-J.2
Greenblatt, H.3
Chen, W.4
Paz, A.5
Dym, O.6
Peleg, Y.7
Chen, T.8
Shen, X.9
He, J.10
Jiang, H.11
Silman, I.12
Sussman, J.L.13
-
48
-
-
84878078602
-
Mapping the conformational space accessible to BACE2 using surface mutants and co-crystals with Fab-fragments, Fynomers, and Xaperones
-
in press.
-
Banner, D. W.; Gsell, B.; Benz, J.; Bertschinger, J.; Burger, D.; Brack, S.; Cuppuleri, S.; Debulpaep, M.; Gast, A.; Grabulovski, D.; Hennig, M.; Hilpert, H.; Huber, W.; Kuglstatter, A.; Kusznir, E.; Laeremans, T.; Matile, H.; Miscenic, C.; a, Rufer, A.; Schlatter, D.; Staeyert, J.; Stihle, M.; Thoma, R.; Weber, M.; Ruf, A. Mapping the conformational space accessible to BACE2 using surface mutants and co-crystals with Fab-fragments, Fynomers, and Xaperones. Acta Crystallogr., Sect. D: Biol. Crystallogr., in press.
-
Acta Crystallogr., Sect. D: Biol. Crystallogr.
-
-
Banner, D.W.1
Gsell, B.2
Benz, J.3
Bertschinger, J.4
Burger, D.5
Brack, S.6
Cuppuleri, S.7
Debulpaep, M.8
Gast, A.9
Grabulovski, D.10
Hennig, M.11
Hilpert, H.12
Huber, W.13
Kuglstatter, A.14
Kusznir, E.15
Laeremans, T.16
Matile, H.17
Miscenic, C.18
Rufer A, A.19
Schlatter, D.20
Staeyert, J.21
Stihle, M.22
Thoma, R.23
Weber, M.24
Ruf, A.25
more..
-
49
-
-
0036500382
-
Stereoelectronic substituent effects in polyhydroxylated piperidines and hexahydropyridazines
-
Jensen, H. H.; Lyngbye, L.; Jensen, A.; Bols, M. Stereoelectronic substituent effects in polyhydroxylated piperidines and hexahydropyridazines Chem.-Eur. J. 2002, 8, 1218-1226
-
(2002)
Chem. - Eur. J.
, vol.8
, pp. 1218-1226
-
-
Jensen, H.H.1
Lyngbye, L.2
Jensen, A.3
Bols, M.4
-
50
-
-
34848921683
-
Predicting and tuning physicochemical properties in lead optimization: Amine basicities
-
Morgenthaler, M.; Schweizer, E.; Hoffmann-Roder, A.; Benini, F.; Martin, R. E.; Jaeschke, G.; Wagner, B.; Fischer, H.; Bendels, S.; Zimmerli, D.; Schneider, J.; Diederich, F.; Kansy, M.; Muller, K. Predicting and tuning physicochemical properties in lead optimization: amine basicities ChemMedChem 2007, 2, 1100-1115
-
(2007)
ChemMedChem
, vol.2
, pp. 1100-1115
-
-
Morgenthaler, M.1
Schweizer, E.2
Hoffmann-Roder, A.3
Benini, F.4
Martin, R.E.5
Jaeschke, G.6
Wagner, B.7
Fischer, H.8
Bendels, S.9
Zimmerli, D.10
Schneider, J.11
Diederich, F.12
Kansy, M.13
Muller, K.14
-
52
-
-
84878038596
-
-
version 9.0; Accelrys Inc. San Diego, CA.
-
VAMP, version 9.0; Accelrys Inc.: San Diego, CA; http://www.accelrys.com.
-
VAMP
-
-
-
53
-
-
84859788625
-
Discovery of Cyclic Sulfone Hydroxyethylamines as Potent and Selective β-Site APP-Cleaving Enzyme 1 (BACE1) Inhibitors: Structure-Based Design and in Vivo Reduction of Amyloid β-Peptides
-
Rueeger, H.; Lueoend, R.; Rogel, O.; Rondeau, J.-M.; Mobitz, H.; Machauer, R.; Jacobson, L.; Staufenbiel, M.; Desrayaud, S.; Neumann, U. Discovery of Cyclic Sulfone Hydroxyethylamines as Potent and Selective β-Site APP-Cleaving Enzyme 1 (BACE1) Inhibitors: Structure-Based Design and in Vivo Reduction of Amyloid β-Peptides J. Med. Chem. 2012, 55, 3364-3386
-
(2012)
J. Med. Chem.
, vol.55
, pp. 3364-3386
-
-
Rueeger, H.1
Lueoend, R.2
Rogel, O.3
Rondeau, J.-M.4
Mobitz, H.5
MacHauer, R.6
Jacobson, L.7
Staufenbiel, M.8
Desrayaud, S.9
Neumann, U.10
-
54
-
-
84868540195
-
Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction
-
Stamford, A. W.; Scott, J. D.; Li, S. W.; Babu, S.; Tadesse, D.; Hunter, R.; Wu, Y.; Misiaszek, J.; Cumming, J. N.; Gilbert, E. J.; Huang, C.; McKittrick, B. A.; Hong, L.; Guo, T.; Zhu, Z.; Strickland, C.; Orth, P.; Voigt, J. H.; Kennedy, M. E.; Chen, X.; Kuvelkar, R.; Hodgson, R.; Hyde, L. A.; Cox, K.; Favreau, L.; Parker, E. M.; Greenlee, W. J. Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction ACS Med. Chem. Lett. 2012, 3, 897-902
-
(2012)
ACS Med. Chem. Lett.
, vol.3
, pp. 897-902
-
-
Stamford, A.W.1
Scott, J.D.2
Li, S.W.3
Babu, S.4
Tadesse, D.5
Hunter, R.6
Wu, Y.7
Misiaszek, J.8
Cumming, J.N.9
Gilbert, E.J.10
Huang, C.11
McKittrick, B.A.12
Hong, L.13
Guo, T.14
Zhu, Z.15
Strickland, C.16
Orth, P.17
Voigt, J.H.18
Kennedy, M.E.19
Chen, X.20
Kuvelkar, R.21
Hodgson, R.22
Hyde, L.A.23
Cox, K.24
Favreau, L.25
Parker, E.M.26
Greenlee, W.J.27
more..
-
55
-
-
77957882573
-
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model
-
Truong, A. P.; Toth, G.; Probst, G. D.; Sealy, J. M.; Bowers, S.; Wone, D. W. G.; Dressen, D.; Hom, R. K.; Konradi, A. W.; Sham, H. L.; Wu, J.; Peterson, B. T.; Ruslim, L.; Bova, M. P.; Kholodenko, D.; Motter, R. N.; Bard, F.; Santiago, P.; Ni, H.; Chian, D.; Soriano, F.; Cole, T.; Brigham, E. F.; Wong, K.; Zmolek, W.; Goldbach, E.; Samant, B.; Chen, L.; Zhang, H.; Nakamura, D. F.; Quinn, K. P.; Yednock, T. A.; Sauer, J.-M. Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model Bioorg. Med. Chem. Lett. 2010, 20, 6231-6236
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 6231-6236
-
-
Truong, A.P.1
Toth, G.2
Probst, G.D.3
Sealy, J.M.4
Bowers, S.5
Wone, D.W.G.6
Dressen, D.7
Hom, R.K.8
Konradi, A.W.9
Sham, H.L.10
Wu, J.11
Peterson, B.T.12
Ruslim, L.13
Bova, M.P.14
Kholodenko, D.15
Motter, R.N.16
Bard, F.17
Santiago, P.18
Ni, H.19
Chian, D.20
Soriano, F.21
Cole, T.22
Brigham, E.F.23
Wong, K.24
Zmolek, W.25
Goldbach, E.26
Samant, B.27
Chen, L.28
Zhang, H.29
Nakamura, D.F.30
Quinn, K.P.31
Yednock, T.A.32
Sauer, J.-M.33
more..
-
56
-
-
37849005419
-
Ligand structural aspects of hERG channel blockade
-
Aronov, A. M. Ligand structural aspects of hERG channel blockade Curr. Top. Med. Chem. 2008, 8, 1113-1127
-
(2008)
Curr. Top. Med. Chem.
, vol.8
, pp. 1113-1127
-
-
Aronov, A.M.1
-
57
-
-
23944456331
-
Method for the determination of the levels of β-amyloid peptide in the CSF sampled from freely moving rats
-
El, M. M.; Haseldonckx, M.; Mackie, C.; Meert, T.; Mercken, M. Method for the determination of the levels of β-amyloid peptide in the CSF sampled from freely moving rats J. Pharmacol. Toxicol. Methods 2005, 52, 229-233
-
(2005)
J. Pharmacol. Toxicol. Methods
, vol.52
, pp. 229-233
-
-
El, M.M.1
Haseldonckx, M.2
MacKie, C.3
Meert, T.4
Mercken, M.5
-
58
-
-
0037085353
-
Substrate and inhibitor profile of BACE (β-secretase) and comparison with other mammalian aspartic proteases
-
Gruninger-Leitch, F.; Schlatter, D.; Kung, E.; Nelbock, P.; Dobeli, H. Substrate and inhibitor profile of BACE (β-secretase) and comparison with other mammalian aspartic proteases J. Biol. Chem. 2002, 277, 4687-4693
-
(2002)
J. Biol. Chem.
, vol.277
, pp. 4687-4693
-
-
Gruninger-Leitch, F.1
Schlatter, D.2
Kung, E.3
Nelbock, P.4
Dobeli, H.5
-
59
-
-
71749086143
-
Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists
-
Martin, R. E.; Mohr, P.; Maerki, H. P.; Guba, W.; Kuratli, C.; Gavelle, O.; Binggeli, A.; Bendels, S.; Alvarez-Sanchez, R.; Alker, A.; Polonchuk, L.; Christ, A. D. Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists Bioorg. Med. Chem. Lett. 2009, 19, 6106-6113
-
(2009)
Bioorg. Med. Chem. Lett.
, vol.19
, pp. 6106-6113
-
-
Martin, R.E.1
Mohr, P.2
Maerki, H.P.3
Guba, W.4
Kuratli, C.5
Gavelle, O.6
Binggeli, A.7
Bendels, S.8
Alvarez-Sanchez, R.9
Alker, A.10
Polonchuk, L.11
Christ, A.D.12
-
60
-
-
39049094722
-
Tyramine fragment binding to BACE-1
-
Kuglstatter, A.; Stahl, M.; Peters, J.-U.; Huber, W.; Stihle, M.; Schlatter, D.; Benz, J.; Ruf, A.; Roth, D.; Enderle, T.; Hennig, M. Tyramine fragment binding to BACE-1 Bioorg. Med. Chem. Lett. 2008, 18, 1304-1307
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 1304-1307
-
-
Kuglstatter, A.1
Stahl, M.2
Peters, J.-U.3
Huber, W.4
Stihle, M.5
Schlatter, D.6
Benz, J.7
Ruf, A.8
Roth, D.9
Enderle, T.10
Hennig, M.11
-
61
-
-
33748191750
-
Demonstration of a common artifact in immunosorbent assays of brain extracts: Development of a solid-phase extraction protocol to enable measurement of amyloid-β from wild-type rodent brain
-
Lanz, T. A.; Schachter, J. B. Demonstration of a common artifact in immunosorbent assays of brain extracts: development of a solid-phase extraction protocol to enable measurement of amyloid-β from wild-type rodent brain J. Neurosci. Methods 2006, 157, 71-81
-
(2006)
J. Neurosci. Methods
, vol.157
, pp. 71-81
-
-
Lanz, T.A.1
Schachter, J.B.2
-
62
-
-
0032507667
-
Caspase-mediated cleavage is not required for the activity of presenilins in amyloidogenesis and NOTCH signaling
-
Brockhaus, M.; Grunberg, J.; Rohrig, S.; Loetscher, H.; Wittenburg, N.; Baumeister, R.; Jacobsen, H.; Haass, C. Caspase-mediated cleavage is not required for the activity of presenilins in amyloidogenesis and NOTCH signaling NeuroReport 1998, 9, 1481-1486
-
(1998)
NeuroReport
, vol.9
, pp. 1481-1486
-
-
Brockhaus, M.1
Grunberg, J.2
Rohrig, S.3
Loetscher, H.4
Wittenburg, N.5
Baumeister, R.6
Jacobsen, H.7
Haass, C.8
|