-
1
-
-
76449085569
-
Gamma-Secretases: From cell biology to therapeutic strategies
-
Bergmans BA, De Strooper B. gamma-Secretases: From cell biology to therapeutic strategies. Lancet Neurol 2010;9:215-26
-
(2010)
Lancet Neurol
, Issue.9
, pp. 215-226
-
-
Bergmans, B.A.1
De Strooper, B.2
-
2
-
-
35348860241
-
Presenilin: Running with Scissors in the Membrane
-
DOI 10.1016/j.cell.2007.10.012, PII S0092867407012822
-
Selkoe DJ, Wolfe MS. Presenilin: Running with scissors in the membrane. Cell 2007;131:215-21 (Pubitemid 47576152)
-
(2007)
Cell
, vol.131
, Issue.2
, pp. 215-221
-
-
Selkoe, D.J.1
Wolfe, M.S.2
-
3
-
-
33745614108
-
The γ-secretase complex: Membrane-embedded proteolytic ensemble
-
DOI 10.1021/bi060799c
-
Wolfe MS. The gamma-secretase complex: Membrane-embedded proteolytic ensemble. Biochemistry 2006;45:7931-9 (Pubitemid 43993216)
-
(2006)
Biochemistry
, vol.45
, Issue.26
, pp. 7931-7939
-
-
Wolfe, M.S.1
-
4
-
-
78650718960
-
Activation and intrinsic gamma-secretase activity of presenilin 1
-
doi: 10.1073/pnas.1013246107
-
Ahn K, Shelton CC, Tian Y, et al Activation and intrinsic gamma-secretase activity of presenilin 1. Proc Natl Acad Sci USA 2010 doi: 10.1073/pnas. 1013246107
-
(2010)
Proc Natl Acad Sci USA
-
-
Ahn, K.1
Shelton, C.C.2
Tian, Y.3
-
5
-
-
0034621824
-
Photoactivated γ-secretase inhibitors directed to the active site covalently label presenilin 1
-
DOI 10.1038/35015085
-
Li YM, Xu M, Lai MT, et al Photoactivated gamma-secretase inhibitors directed to the active site covalently label presenilin 1. Nature 2000;405:689-94 (Pubitemid 30428655)
-
(2000)
Nature
, vol.405
, Issue.6787
, pp. 689-694
-
-
Li, Y.-M.1
Xu, M.2
Lai, M.-T.3
Huang, Q.4
Castro, J.L.5
DiMuzlo-Mower, J.6
Harrison, T.7
Lellis, C.8
Nadin, A.9
Neduvelli, J.G.10
Register, R.B.11
Sardana, M.K.12
Shearman, M.S.13
Smith, A.L.14
Shi, X.-P.15
Yin, K.-C.16
Shafer, J.A.17
Gardell, S.J.18
-
6
-
-
0033780472
-
Transition-state analogue inhibitors of gamma-secretase bind directly to presenilin-1
-
Esler WP, Kimberly WT, Ostaszewski BL, et al Transition-state analogue inhibitors of gamma-secretase bind directly to presenilin-1. Nat Cell Biol 2000;2:428-34
-
(2000)
Nat Cell Biol
, vol.2
, pp. 428-34
-
-
Esler, W.P.1
Kimberly, W.T.2
Ostaszewski, B.L.3
-
7
-
-
43049163813
-
Substrate specificity of gamma-secretase and other intramembrane proteases
-
Beel AJ, Sanders CR. Substrate specificity of gamma-secretase and other intramembrane proteases. Cell Mol Life Sci 2008;65:1311-34
-
(2008)
Cell Mol Life Sci
, vol.65
, pp. 1311-1334
-
-
Beel, A.J.1
Sanders, C.R.2
-
8
-
-
0037135111
-
The amyloid hypothesis of Alzheimer's disease: Progress and problems on the road to therapeutics
-
DOI 10.1126/science.1072994
-
Hardy J, Selkoe DJ. The amyloid hypothesis of Alzheimer's disease: Progress and problems on the road to therapeutics. Science 2002;297:353-6 (Pubitemid 34790756)
-
(2002)
Science
, vol.297
, Issue.5580
, pp. 353-356
-
-
Hardy, J.1
Selkoe, D.J.2
-
9
-
-
13944276825
-
Twenty years of the Alzheimer's disease amyloid hypothesis: A genetic perspective
-
DOI 10.1016/j.cell.2005.02.008
-
Tanzi RE, Bertram L. Twenty years of the Alzheimer's disease amyloid hypothesis: A genetic perspective. Cell 2005;120:545-55 (Pubitemid 40269768)
-
(2005)
Cell
, vol.120
, Issue.4
, pp. 545-555
-
-
Tanzi, R.E.1
Bertram, L.2
-
10
-
-
77957927865
-
The genetics of Alzheimer disease: Back to the future
-
Bertram L, Lill CM, Tanzi RE. The genetics of Alzheimer disease: Back to the future. Neuron 2010;68:270-81
-
(2010)
Neuron
, Issue.68
, pp. 270-281
-
-
Bertram, L.1
Lill, C.M.2
Tanzi, R.E.3
-
11
-
-
49449101906
-
Phase 2 safety trial targeting amyloid beta production with a gamma-secretase inhibitor in Alzheimer disease
-
Fleisher AS, Raman R, Siemers ER, et al Phase 2 safety trial targeting amyloid beta production with a gamma-secretase inhibitor in Alzheimer disease. Arch Neurol 2008;65:1031-8
-
(2008)
Arch Neurol
, vol.65
, pp. 1031-1038
-
-
Fleisher, A.S.1
Raman, R.2
Siemers, E.R.3
-
12
-
-
66749084437
-
A gamma-secretase inhibitor decreases amyloid-beta production in the central nervous system
-
Bateman RJ, Siemers ER, Mawuenyega KG, et al A gamma-secretase inhibitor decreases amyloid-beta production in the central nervous system. Ann Neurol 2009;66:48-54
-
(2009)
Ann Neurol
, vol.66
, pp. 48-54
-
-
Bateman, R.J.1
Siemers, E.R.2
Mawuenyega, K.G.3
-
13
-
-
77957361080
-
Alzheimer's failure raises questions about disease-modifying strategies
-
Extance A. Alzheimer's failure raises questions about disease-modifying strategies. Nat Rev Drug Discov 2010;9:749-51
-
(2010)
Nat Rev Drug Discov
, Issue.9
, pp. 749-751
-
-
Extance, A.1
-
14
-
-
0033535504
-
A presenilin-1-dependent gamma-secretase-like protease mediates release of Notch intracellular domain
-
De Strooper B, Annaert W, Cupers P, et al A presenilin-1-dependent gamma-secretase-like protease mediates release of Notch intracellular domain. Nature 1999;398:518-22
-
(1999)
Nature
, vol.398
, pp. 518-522
-
-
De Strooper, B.1
Annaert, W.2
Cupers, P.3
-
15
-
-
11144355129
-
Chronic treatment with the gamma-secretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation
-
Wong GT, Manfra D, Poulet FM, et al Chronic treatment with the gamma-secretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation. J Biol Chem 2004;279:12876-82
-
(2004)
J Biol Chem
, vol.279
, pp. 12876-1282
-
-
Wong, G.T.1
Manfra, D.2
Poulet, F.M.3
-
16
-
-
20544460148
-
Notch/γ-secretase inhibition turns proliferative cells in intestinal crypts and adenomas into goblet cells
-
DOI 10.1038/nature03659
-
van Es JH, van Gijn ME, Riccio O, et al Notch/gamma-secretase inhibition turns proliferative cells in intestinal crypts and adenomas into goblet cells. Nature 2005;435:959-63 (Pubitemid 40896322)
-
(2005)
Nature
, vol.435
, Issue.7044
, pp. 959-963
-
-
Van Es, J.H.1
Van Gijn, M.E.2
Riccio, O.3
Van Den Born, M.4
Vooijs, M.5
Begthel, H.6
Cozijnsen, M.7
Robine, S.8
Winton, D.J.9
Radtke, F.10
Clevers, H.11
-
17
-
-
22144471581
-
Notch to remember
-
DOI 10.1016/j.tins.2005.05.003, PII S0166223605001281
-
Costa RM, Drew C, Silva AJ. Notch to remember. Trends Neurosci 2005;28:429-35 (Pubitemid 40982556)
-
(2005)
Trends in Neurosciences
, vol.28
, Issue.8
, pp. 429-435
-
-
Costa, R.M.1
Drew, C.2
Silva, A.J.3
-
18
-
-
31444447881
-
Notch signalling in vertebrate neural development
-
DOI 10.1038/nrn1847, PII NRN1847
-
Louvi A, Artavanis-Tsakonas S. Notch signalling in vertebrate neural development. Nat Rev Neurosci 2006;7:93-102 (Pubitemid 43151596)
-
(2006)
Nature Reviews Neuroscience
, vol.7
, Issue.2
, pp. 93-102
-
-
Louvi, A.1
Artavanis-Tsakonas, S.2
-
19
-
-
77954122667
-
Discovery and evaluation of BMS-708163, a potent, selective and orally bioavailable gamma-secretase inhibitor
-
Gillman KW, Starrett JE, Parker MF, et al Discovery and evaluation of BMS-708163, a potent, selective and orally bioavailable gamma-secretase inhibitor. ACS Med Chem Lett 2010;1:120-4
-
(2010)
ACS Med Chem Lett
, Issue.1
, pp. 120-124
-
-
Gillman, K.W.1
Starrett, J.E.2
Parker, M.F.3
-
20
-
-
70350059834
-
Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease
-
Kreft AF, Martone R, Porte A. Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease. J Med Chem 2009;52:6169-88
-
(2009)
J Med Chem
, vol.52
, pp. 6169-6188
-
-
Kreft, A.F.1
Martone, R.2
Porte, A.3
-
21
-
-
0035829592
-
A subset of NSAIDs lower amyloidogenic Aβ42 independently of cyclooxygenase activity
-
DOI 10.1038/35102591
-
Weggen S, Eriksen JL, Das P, et al A subset of NSAIDs lower amyloidogenic Abeta42 independently of cyclooxygenase activity. Nature 2001;414:212-16 (Pubitemid 33051236)
-
(2001)
Nature
, vol.414
, Issue.6860
, pp. 212-216
-
-
Weggen, S.1
Eriksen, J.L.2
Das, P.3
Sagi, S.A.4
Wang, R.5
Pietrzik, C.U.6
Findlay, K.A.7
Smith, T.E.8
Murphy, M.P.9
Bulter, T.10
Kang, D.E.11
Marquez-Sterling, N.12
Golde, T.E.13
Koo, E.H.14
-
22
-
-
85047691727
-
NSAIDs and enantiomers of flurbiprofen target γ-secretase and lower Aβ42 in vivo
-
DOI 10.1172/JCI200318162
-
Eriksen JL, Sagi SA, Smith TE, et al NSAIDs and enantiomers of flurbiprofen target gamma-secretase and lower Abeta 42 in vivo. J Clin Invest 2003;112:440-9 (Pubitemid 38063773)
-
(2003)
Journal of Clinical Investigation
, vol.112
, Issue.3
, pp. 440-449
-
-
Eriksen, J.L.1
Sagi, S.A.2
Smith, T.E.3
Weggen, S.4
Das, P.5
McLendon, D.C.6
Ozols, V.V.7
Jessing, K.W.8
Zavitz, K.H.9
Koo, E.H.10
Golde, T.E.11
-
23
-
-
0041876229
-
Evidence that nonsteroidal anti-inflammatory drugs decrease amyloid β42 production by direct modulation of γ-secretase activity
-
DOI 10.1074/jbc.M303592200
-
Weggen S, Eriksen JL, Sagi SA, et al Evidence that nonsteroidal anti-inflammatory drugs decrease amyloid beta 42 production by direct modulation of gamma-secretase activity. J Biol Chem 2003;278:31831-7 (Pubitemid 37048365)
-
(2003)
Journal of Biological Chemistry
, vol.278
, Issue.34
, pp. 31831-31837
-
-
Weggen, S.1
Eriksen, J.L.2
Sagi, S.A.3
Pietrzik, C.U.4
Ozols, V.5
Fauq, A.6
Golde, T.E.7
Koo, E.H.8
-
24
-
-
24744448213
-
1-42 secretion
-
DOI 10.1021/jm0502541
-
Peretto I, Radaelli S, Parini C, et al Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1-42) secretion. J Med Chem 2005;48:5705-20 (Pubitemid 41298345)
-
(2005)
Journal of Medicinal Chemistry
, vol.48
, Issue.18
, pp. 5705-5720
-
-
Peretto, I.1
Radaelli, S.2
Parini, C.3
Zandi, M.4
Raveglia, L.F.5
Dondio, G.6
Fontanella, L.7
Misiano, P.8
Bigogno, C.9
Rizzi, A.10
Riccardi, B.11
Biscaioli, M.12
Marchetti, S.13
Puccini, P.14
Catinella, S.15
Rondelli, I.16
Cenacchi, V.17
Bolzoni, P.T.18
Caruso, P.19
Villetti, G.20
Facchinetti, F.21
Del Giudice, E.22
Moretto, N.23
Imbimbo, B.P.24
more..
-
25
-
-
43249122280
-
Efficacy and safety of tarenflurbil in mild to moderate Alzheimer's disease: A randomised phase II trial
-
Wilcock GK, Black SE, Hendrix SB, et al Efficacy and safety of tarenflurbil in mild to moderate Alzheimer's disease: A randomised phase II trial. Lancet Neurol 2008;7:483-93
-
(2008)
Lancet Neurol
, vol.7
, pp. 483-493
-
-
Wilcock, G.K.1
Black, S.E.2
Hendrix, S.B.3
-
26
-
-
68049148021
-
Why did tarenflurbil fail in Alzheimer's disease?
-
Imbimbo BP. Why did tarenflurbil fail in Alzheimer's disease? J Alzheimers Dis 2009;17:757-60
-
(2009)
J Alzheimers Dis
, vol.17
, pp. 757-760
-
-
Imbimbo, B.P.1
-
27
-
-
36349011989
-
1-(3′,4′-Dichloro-2-fluoro[1,1′-biphenyl]-4-yl) -cyclopropanecarboxylic acid (CHF5074), a novel γ-secretase modulator, reduces brain β-amyloid pathology in a transgenic mouse model of Alzheimer's disease without causing peripheral toxicity
-
DOI 10.1124/jpet.107.129007
-
Imbimbo BP, Del Giudice E, Colavito D, et al 1-(3',4'-Dichloro-2- fluoro[1,1'-biphenyl]-4-yl)- cyclopropanecarboxylic acid (CHF5074), a novel gamma-secretase modulator, reduces brain beta-amyloid pathology in a transgenic mouse model of Alzheimer's disease without causing peripheral toxicity. J Pharmacol Exp Ther 2007;323:822-30 (Pubitemid 350146064)
-
(2007)
Journal of Pharmacology and Experimental Therapeutics
, vol.323
, Issue.3
, pp. 822-830
-
-
Imbimbo, B.P.1
Del Giudice, E.2
Colavito, D.3
D'Arrigo, A.4
Dalle Carbonare, M.5
Villetti, G.6
Facchinetti, F.7
Volta, R.8
Pietrini, V.9
Baroc, M.F.10
Serneels, L.11
De Strooper, B.12
Leon, A.13
-
28
-
-
79952919812
-
-
Safety, pharmacokinetics and pharmacodynamics study of treatment with CHF5074 in healthy young male subjects. Available from [Last accessed 29 October 2010]
-
Safety, pharmacokinetics and pharmacodynamics study of treatment with CHF5074 in healthy young male subjects. Available from: Www.clinicaltrials.gov/ ct2/show/ NCT00954252?term=CHF5074&rank=2 [Last accessed 29 October 2010]
-
-
-
-
29
-
-
0038719688
-
Sulindac sulfide is a noncompetitive γ-secretase inhibitor that preferentially reduces Aβ42 generation
-
DOI 10.1074/jbc.M301619200
-
Takahashi Y, Hayashi I, Tominari Y, et al Sulindac sulfide is a noncompetitive gamma-secretase inhibitor that preferentially reduces Abeta 42 generation. J Biol Chem 2003;278:18664-70 (Pubitemid 36799494)
-
(2003)
Journal of Biological Chemistry
, vol.278
, Issue.20
, pp. 18664-18670
-
-
Takahashi, Y.1
Hayashi, I.2
Tominari, Y.3
Rikimaru, K.4
Morohashi, Y.5
Kan, T.6
Natsugari, H.7
Fukuyama, T.8
Tomita, T.9
Iwatsubo, T.10
-
30
-
-
6344233805
-
Selected non-steroidal anti-inflammatory drugs and their derivatives target γ-secretase at a novel site: Evidence for an allosteric mechanism
-
DOI 10.1074/jbc.M404937200
-
Beher D, Clarke EE, Wrigley JD, et al Selected non-steroidal anti-inflammatory drugs and their derivatives target gamma-secretase at a novel site. Evidence for an allosteric mechanism. J Biol Chem 2004;279:43419-26 (Pubitemid 39390641)
-
(2004)
Journal of Biological Chemistry
, vol.279
, Issue.42
, pp. 43419-43426
-
-
Beher, D.1
Clarke, E.E.2
Wrigley, J.D.J.3
Martin, A.C.L.4
Nadin, A.5
Churcher, I.6
Shearman, M.S.7
-
31
-
-
77956187227
-
Exploring the chemical space of gamma-secretase modulators
-
Zettl H, Weggen S, Schneider P, et al Exploring the chemical space of gamma-secretase modulators. Trends Pharmacol Sci 2010;31:402-10
-
(2010)
Trends Pharmacol Sci
, Issue.31
, pp. 402-410
-
-
Zettl, H.1
Weggen, S.2
Schneider, P.3
-
32
-
-
45149105232
-
Substrate-targeting gamma-secretase modulators
-
Kukar TL, Ladd TB, Bann MA, et al Substrate-targeting gamma-secretase modulators. Nature 2008;453:925-9
-
(2008)
Nature
, vol.453
, pp. 925-929
-
-
Kukar, T.L.1
Ladd, T.B.2
Bann, M.A.3
-
33
-
-
72449208456
-
Nonspecificity of binding of gamma-secretase modulators to the amyloid precursor protein
-
Beel AJ, Barrett P, Schnier PD, et al Nonspecificity of binding of gamma-secretase modulators to the amyloid precursor protein. Biochemistry 2009;48:11837-9
-
(2009)
Biochemistry
, vol.48
, pp. 11837-11839
-
-
Beel, A.J.1
Barrett, P.2
Schnier, P.D.3
-
34
-
-
77952947184
-
Beta-amyloid precursor protein mutants respond to gamma-secretase modulators
-
Page RM, Gutsmiedl A, Fukumori A, et al Beta-amyloid precursor protein mutants respond to gamma-secretase modulators. J Biol Chem 2010;285:17798-810
-
(2010)
J Biol Chem
, Issue.285
, pp. 17798-17810
-
-
Page, R.M.1
Gutsmiedl, A.2
Fukumori, A.3
-
35
-
-
33646353694
-
Secretion of the Notch-1 Aβ-like peptide during Notch signaling
-
DOI 10.1074/jbc.M513250200
-
Okochi M, Fukumori A, Jiang J, et al Secretion of the Notch-1 Abeta-like peptide during Notch signaling. J Biol Chem 2006;281:7890-8 (Pubitemid 43847405)
-
(2006)
Journal of Biological Chemistry
, vol.281
, Issue.12
, pp. 7890-7898
-
-
Okochi, M.1
Fukumori, A.2
Jiang, J.3
Itoh, N.4
Kimura, R.5
Steiner, H.6
Haass, C.7
Tagami, S.8
Takeda, M.9
-
36
-
-
77957096840
-
Amyloid beta 42 peptide-lowering compounds directly bind to Abeta and interfere with amyloid precursor protein (APP) transmembrane dimerization
-
Richter L, Munter LM, Ness J, et al Amyloid beta 42 peptide-lowering compounds directly bind to Abeta and interfere with amyloid precursor protein (APP) transmembrane dimerization. Proc Natl Acad Sci USA 2010;107:14597-602
-
(2010)
Proc Natl Acad Sci USA
, Issue.107
, pp. 14597-14602
-
-
Richter, L.1
Munter, L.M.2
Ness, J.3
-
37
-
-
7044254509
-
42 and change presenilin 1 conformation
-
DOI 10.1038/nm1112
-
Lleo A, Berezovska O, Herl L, et al Nonsteroidal anti-inflammatory drugs lower Abeta42 and change presenilin 1 conformation. Nat Med 2004;10:1065-6 (Pubitemid 39424866)
-
(2004)
Nature Medicine
, vol.10
, Issue.10
, pp. 1065-1066
-
-
Lleo, A.1
Berezovska, O.2
Herl, L.3
Raju, S.4
Deng, A.5
Bacskai, B.J.6
Frosch, M.P.7
Irizarry, M.8
Hyman, B.T.9
-
38
-
-
78650047391
-
Substrate docking to gamma-secretase allows access of gamma-secretase modulators to an allosteric site
-
Uemura K, Farner KC, Hashimoto T, et al Substrate docking to gamma-secretase allows access of gamma-secretase modulators to an allosteric site. Nat Commun 2010;1:130
-
(2010)
Nat Commun
, Issue.1
, pp. 130
-
-
Uemura, K.1
Farner, K.C.2
Hashimoto, T.3
-
39
-
-
79952932971
-
-
Neurogenetics Inc WO04110350
-
Neurogenetics, Inc. WO04110350; 2004
-
(2004)
-
-
-
40
-
-
79952981949
-
-
Eisai Co. Ltd. WO05115990
-
Eisai Co., Ltd. WO05115990; 2005
-
(2005)
-
-
-
42
-
-
79952925223
-
-
Recruiting a randomized, double-blind, placebo-controlled, sequential ascending, single-dose study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of E2212 in healthy subjects. Available from: [Last accessed 29 October 2010]
-
Recruiting a randomized, double-blind, placebo-controlled, sequential ascending, single-dose study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of E2212 in healthy subjects. Available from: Www. clinicaltrials.gov/ct2/results?term=E2212 [Last accessed 29 October 2010]
-
-
-
-
43
-
-
77957257809
-
Acute effect on the Abeta isoform pattern in CSF in response to gamma-secretase modulator and inhibitor treatment in dogs
-
Portelius E, Van Broeck B, Andreasson U, et al Acute effect on the Abeta isoform pattern in CSF in response to gamma-secretase modulator and inhibitor treatment in dogs. J Alzheimers Dis 2010;21:1005-12
-
(2010)
J Alzheimers Dis
, Issue.21
, pp. 1005-1012
-
-
Portelius, E.1
Van Broeck, B.2
Andreasson, U.3
-
44
-
-
77956311201
-
Modulation of gamma-secretase reduces beta-amyloid deposition in a transgenic mouse model of Alzheimer's disease
-
Kounnas MZ, Danks AM, Cheng S, et al Modulation of gamma-secretase reduces beta-amyloid deposition in a transgenic mouse model of Alzheimer's disease. Neuron 2010;67:769-80
-
(2010)
Neuron
, Issue.67
, pp. 769-780
-
-
Kounnas, M.Z.1
Danks, A.M.2
Cheng, S.3
-
45
-
-
48049097077
-
Patents targeting gamma-secretase inhibition and modulation for the treatment of Alzheimer's disease: 2004-2008
-
Garofalo AW. Patents targeting gamma-secretase inhibition and modulation for the treatment of Alzheimer's disease: 2004-2008. Expert Opin Ther Pat 2008;18:693-703
-
Expert Opin Ther Pat
, vol.2008
, Issue.18
, pp. 693-703
-
-
Garofalo, A.W.1
-
46
-
-
39449105778
-
Predicting key example compounds in competitors' patent applications using structural information alone
-
DOI 10.1021/ci7002686
-
Hattori K, Wakabayashi H, Tamaki K. Predicting key example compounds in competitors' patent applications using structural information alone. J Chem Inf Model 2008;48:135-42 (Pubitemid 351271058)
-
(2008)
Journal of Chemical Information and Modeling
, vol.48
, Issue.1
, pp. 135-142
-
-
Hattori, K.1
Wakabayashi, H.2
Tamaki, K.3
-
47
-
-
79952932109
-
-
Myriad Genetics Inc. US080249135
-
Myriad Genetics, Inc. US080249135; 2008
-
(2008)
-
-
-
48
-
-
79952952940
-
-
Merck & Co., Inc. WO08085301
-
Merck & Co., Inc. WO08085301; 2008
-
(2008)
-
-
-
49
-
-
72249100345
-
Fluorinated piperidine acetic acids as gamma-secretase modulators
-
Stanton MG, Hubbs J, Sloman D, et al Fluorinated piperidine acetic acids as gamma-secretase modulators. Bioorg Med Chem Lett 2010;20:755-8
-
(2010)
Bioorg Med Chem Lett
, Issue.20
, pp. 755-758
-
-
Stanton, M.G.1
Hubbs, J.2
Sloman, D.3
-
51
-
-
79952959978
-
-
EnVivo Pharmaceuticals Inc. WO09036428
-
EnVivo Pharmaceuticals, Inc. WO09036428; 2009
-
(2009)
-
-
-
52
-
-
79952906342
-
-
EnVivo Pharmaceuticals Inc. WO09086277
-
EnVivo Pharmaceuticals, Inc. WO09086277; 2009
-
(2009)
-
-
-
53
-
-
79952904147
-
-
Janssen Pharmaceutica N.V. WO09051948
-
Janssen Pharmaceutica, N.V. WO09051948; 2009
-
(2009)
-
-
-
54
-
-
79952964653
-
-
Janssen Pharmaceutica, N.V. WO09052079
-
Janssen Pharmaceutica, N.V. WO09052079; 2009
-
(2009)
-
-
-
55
-
-
79952958001
-
-
Janssen Pharmaceutica N.V. WO09052126
-
Janssen Pharmaceutica, N.V. WO09052126; 2009
-
(2009)
-
-
-
56
-
-
79952981558
-
-
Janssen Pharmaceutica N.V. WO09052334
-
Janssen Pharmaceutica, N.V. WO09052334; 2009
-
(2009)
-
-
-
57
-
-
79952957993
-
-
Janssen Pharmaceutica N.V. WO09052350
-
Janssen Pharmaceutica, N.V. WO09052350; 2009
-
(2009)
-
-
-
58
-
-
79952933414
-
-
Janssen Pharmaceutica N.V. WO10011626
-
Janssen Pharmaceutica, N.V. WO10011626; 2010
-
(2010)
-
-
-
59
-
-
79952948120
-
-
Eisai Co. Ltd. US060004013
-
Eisai Co., Ltd. US060004013; 2006
-
(2006)
-
-
-
60
-
-
79952965236
-
-
Eisai Co. Ltd. WO06046575
-
Eisai Co., Ltd. WO06046575; 2006
-
(2006)
-
-
-
61
-
-
79952950224
-
-
Eisai R&D Management Co. Ltd. WO07058305
-
Eisai R&D Management Co., Ltd. WO07058305; 2007
-
(2007)
-
-
-
62
-
-
79952919363
-
-
Eisai R&D Management Co. Ltd. WO08140111
-
Eisai R&D Management Co., Ltd. WO08140111; 2008
-
(2008)
-
-
-
63
-
-
79952978384
-
-
Eisai R&D Management Co. Ltd. WO07058304
-
Eisai R&D Management Co., Ltd. WO07058304; 2007
-
(2007)
-
-
-
64
-
-
62249157012
-
Alzheimer's disease: Gamma-secretase inhibitors
-
Imbimbo BP. Alzheimer's disease: Gamma-secretase inhibitors. Drug Discov Today Ther Strateg 2008;5:169-75
-
(2008)
Drug Discov Today Ther Strateg
, vol.5
, pp. 169-175
-
-
Imbimbo, B.P.1
-
65
-
-
40349111175
-
Therapeutic potential of γ-secretase inhibitors and modulators
-
DOI 10.2174/156802608783334015
-
Imbimbo BP. Therapeutic potential of gamma-secretase inhibitors and modulators. Curr Top Med Chem 2008;8:54-61 (Pubitemid 351791047)
-
(2008)
Current Topics in Medicinal Chemistry
, vol.8
, Issue.1
, pp. 54-61
-
-
Imbimbo, B.P.1
-
66
-
-
79952958738
-
-
18 December, Eisai Co., Ltd. Available from, [Last accessed 23 October 2010]
-
FY2009 Product Creation Meeting, 18 December 2009, Eisai Co., Ltd. Available from: Www.eisai.co.jp/pdf/ eir/emat/material20091218e.pdf, [Last accessed 23 October 2010]
-
(2009)
FY2009 Product Creation Meeting
-
-
-
67
-
-
79952979271
-
-
Eisai R&D Management Co. Ltd. US070117839
-
Eisai R&D Management Co., Ltd. US070117839; 2007
-
(2007)
-
-
-
68
-
-
79952975239
-
-
Eisai R&D Management Co. Ltd. US070117798
-
Eisai R&D Management Co., Ltd. US070117798; 2007
-
(2007)
-
-
-
69
-
-
79952953355
-
-
Eisai R&D Management Co. Ltd. US080207900
-
Eisai R&D Management Co., Ltd. US080207900; 2008
-
(2008)
-
-
-
70
-
-
79952983631
-
-
Eisai R&D Management Co. Ltd. WO07102580
-
Eisai R&D Management Co., Ltd. WO07102580; 2007
-
(2007)
-
-
-
71
-
-
79952909046
-
-
Eisai R&D Management Co. Ltd. WO09028588
-
Eisai R&D Management Co., Ltd. WO09028588; 2009
-
(2009)
-
-
-
72
-
-
79952924822
-
-
Eisai R&D Management Co. Ltd. US090062529
-
Eisai R&D Management Co., Ltd. US090062529; 2009
-
(2009)
-
-
-
73
-
-
79952921986
-
-
Eisai R&D Management Co. Ltd. WO10025197
-
Eisai R&D Management Co., Ltd. WO10025197; 2010
-
(2010)
-
-
-
74
-
-
79952973373
-
-
Eisai R&D Management Co. Ltd. WO10098496
-
Eisai R&D Management Co., Ltd. WO10098496; 2010
-
(2010)
-
-
-
75
-
-
79952977529
-
-
Eisai R&D Management Co. Ltd. WO10098332
-
Eisai R&D Management Co., Ltd. WO10098332; 2010
-
(2010)
-
-
-
76
-
-
79952972582
-
-
Eisai R&D Management Co. Ltd. WO10098490
-
Eisai R&D Management Co., Ltd. WO10098490; 2010
-
(2010)
-
-
-
77
-
-
79952926060
-
-
Eisai R&D Management Co. Ltd. WO10098495
-
Eisai R&D Management Co., Ltd. WO10098495; 2010
-
(2010)
-
-
-
78
-
-
79952922811
-
-
Calculated using clogP v4.3. BioByte Corporation, Claremont, CA
-
Calculated using clogP v4.3. (2008) BioByte Software, BioByte Corporation, Claremont, CA
-
(2008)
BioByte Software
-
-
-
79
-
-
79952920632
-
-
Merck & Co., Inc. WO08097538
-
Merck & Co., Inc. WO08097538; 2008
-
(2008)
-
-
-
80
-
-
79952930435
-
-
Schering Corp WO09005729
-
Schering Corp. WO09005729; 2009
-
(2009)
-
-
-
81
-
-
79952933416
-
-
Schering Corp WO09045314
-
Schering Corp. WO09045314; 2009
-
(2009)
-
-
-
82
-
-
79952974818
-
-
Schering Corp WO09020580
-
Schering Corp. WO09020580; 2009
-
(2009)
-
-
-
83
-
-
79952945280
-
-
Schering Corp WO08153792
-
Schering Corp. WO08153792; 2008
-
(2008)
-
-
-
84
-
-
79952981948
-
-
Schering Corp WO08153793
-
Schering Corp. WO08153793; 2008
-
(2008)
-
-
-
85
-
-
79952905463
-
-
Schering Corp WO10054067
-
Schering Corp. WO10054067; 2010
-
(2010)
-
-
-
86
-
-
79952964184
-
-
Schering Corp WO08137139
-
Schering Corp. WO08137139; 2008
-
(2008)
-
-
-
87
-
-
79952938398
-
-
Schering Corp WO10054078
-
Schering Corp. WO10054078; 2010
-
(2010)
-
-
-
88
-
-
79952983253
-
-
Schering Corp WO10054064
-
Schering Corp. WO10054064; 2010
-
(2010)
-
-
-
89
-
-
79952939250
-
-
Schering Corp WO09061699
-
Schering Corp. WO09061699; 2009
-
(2009)
-
-
-
91
-
-
77249100811
-
Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I-inhibitor design and validation
-
Zhu Z, Sun ZY, Ye Y, et al Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I-inhibitor design and validation. J Med Chem 2010;53:951-65
-
(2010)
J Med Chem
, Issue.53
, pp. 951-965
-
-
Zhu, Z.1
Sun, Z.Y.2
Ye, Y.3
-
92
-
-
79952910643
-
-
Dosed orally at 10 mg/kg. Brain concentration at 6 h for 35 and 37 were 914 and 275 ng/g, respectively
-
Dosed orally at 10 mg/kg. Brain concentration at 6 h for 35 and 37 were 914 and 275 ng/g, respectively
-
-
-
-
93
-
-
79952938395
-
-
Schering Corp WO10075203
-
Schering Corp. WO10075203; 2010
-
(2010)
-
-
-
94
-
-
79952981556
-
-
Schering Corp WO10075204
-
Schering Corp. WO10075204; 2010
-
(2010)
-
-
-
95
-
-
79952974410
-
-
Schering Corp WO09108766
-
Schering Corp. WO09108766; 2009
-
(2009)
-
-
-
96
-
-
79952915598
-
-
Schering Corp WO09032277
-
Schering Corp. WO09032277; 2009
-
(2009)
-
-
-
97
-
-
77955869481
-
The discovery of pyridone and pyridazone heterocycles as gamma-secretase modulators
-
Huang X, Aslanian R, Zhou W, et al The discovery of pyridone and pyridazone heterocycles as gamma-secretase modulators. ACS Med Chem Lett 2010;1:184-7
-
(2010)
ACS Med Chem Lett
, Issue.1
, pp. 184-187
-
-
Huang, X.1
Aslanian, R.2
Zhou, W.3
-
98
-
-
79952911475
-
-
Schering Corp WO09076337
-
Schering Corp. WO09076337; 2009
-
(2009)
-
-
-
99
-
-
79952972184
-
-
Schering Corp US100137320
-
Schering Corp. US100137320; 2010
-
(2010)
-
-
-
100
-
-
79952927399
-
-
Schering Corp WO09076352
-
Schering Corp. WO09076352; 2009
-
(2009)
-
-
-
101
-
-
79952947303
-
-
Schering Corp WO09073779
-
Schering Corp. WO09073779; 2009
-
(2009)
-
-
-
102
-
-
79952935394
-
-
Merck & Co., Inc. WO08156580
-
Merck & Co., Inc. WO08156580; 2008
-
(2008)
-
-
-
103
-
-
79952923222
-
-
Merck & Co., Inc. WO10071741
-
Merck & Co., Inc. WO10071741; 2010
-
(2010)
-
-
-
104
-
-
79952961676
-
-
Merck & Co., Inc. WO10077582
-
Merck & Co., Inc. WO10077582; 2010
-
(2010)
-
-
-
105
-
-
79952966537
-
-
Eisai R&D Management Co. Ltd. WO10098488
-
Eisai R&D Management Co., Ltd. WO10098488; 2010
-
(2010)
-
-
-
106
-
-
79952970671
-
-
Glaxo Group Ltd WO09050227
-
Glaxo Group Ltd. WO09050227; 2009
-
(2009)
-
-
-
107
-
-
79952942339
-
-
Hoffmann-La Roche Inc. US080280948
-
Hoffmann-La Roche, Inc. US080280948; 2008
-
(2008)
-
-
-
108
-
-
79952967789
-
-
Hoffmann-La Roche Inc. WO09087127
-
Hoffmann-La Roche, Inc. WO09087127; 2009
-
(2009)
-
-
-
109
-
-
79952943142
-
-
Hoffmann-La Roche Inc. WO09103652
-
Hoffmann-La Roche, Inc. WO09103652; 2009
-
(2009)
-
-
-
110
-
-
79952982823
-
-
Hoffmann-La Roche Inc. WO10040661
-
Hoffmann-La Roche, Inc. WO10040661; 2010
-
(2010)
-
-
-
111
-
-
79952948121
-
-
Hoffmann-La Roche Inc. WO10052199
-
Hoffmann-La Roche, Inc. WO10052199; 2010
-
(2010)
-
-
-
112
-
-
79952925634
-
-
AstraZeneca AB WO10053438
-
AstraZeneca AB. WO10053438; 2010
-
(2010)
-
-
-
113
-
-
79952940184
-
-
Ortho-McNeil-Janssen Pharmaceuticals Inc. WO10070008
-
Ortho-McNeil-Janssen Pharmaceuticals, Inc. WO10070008; 2010
-
(2010)
-
-
-
114
-
-
79952947699
-
-
Ortho-McNeil-Janssen Pharmaceuticals Inc. WO10089292
-
Ortho-McNeil-Janssen Pharmaceuticals, Inc. WO10089292; 2010
-
(2010)
-
-
-
115
-
-
79952964182
-
-
Ortho-McNeil-Janssen Pharmaceuticals Inc. WO10094647
-
Ortho-McNeil-Janssen Pharmaceuticals, Inc. WO10094647; 2010
-
(2010)
-
-
-
116
-
-
79952971334
-
-
Bristol-Myers Squibb Co WO10083141
-
Bristol-Myers Squibb Co. WO10083141; 2010
-
(2010)
-
-
-
117
-
-
79952910215
-
-
Eisai R&D Management Co. Ltd. WO07135969
-
Eisai R&D Management Co., Ltd. WO07135969; 2007
-
(2007)
-
-
-
118
-
-
79952918537
-
-
TorreyPines Therapeutics Inc. WO08137102
-
TorreyPines Therapeutics, Inc. WO08137102; 2008
-
(2008)
-
-
-
119
-
-
79952905058
-
-
Amgen Inc WO09137404
-
Amgen, Inc. WO09137404; 2009
-
(2009)
-
-
-
120
-
-
79952936712
-
-
Amgen Inc WO09075874
-
Amgen, Inc. WO09075874; 2009
-
(2009)
-
-
-
121
-
-
79952933783
-
-
Pfizer Inc WO10100606
-
Pfizer, Inc. WO10100606; 2010
-
(2010)
-
-
-
122
-
-
79952972581
-
-
Merck & Co., Inc. WO08100412
-
Merck & Co., Inc. WO08100412; 2008
-
(2008)
-
-
-
123
-
-
79952954220
-
-
Merck & Co., Inc. WO08099210
-
Merck & Co., Inc. WO08099210; 2008
-
(2008)
-
-
-
124
-
-
79952926059
-
-
Merck & Co., Inc. WO10019392
-
Merck & Co., Inc. WO10019392; 2010
-
(2010)
-
-
-
125
-
-
79952935808
-
-
Merck & Co., Inc. WO10019393
-
Merck & Co., Inc. WO10019393; 2010
-
(2010)
-
-
-
126
-
-
74049093168
-
Piperazinyl pyrimidine derivatives as potent gamma-secretase modulators
-
Rivkin A, Ahearn SP, Chichetti SM, et al Piperazinyl pyrimidine derivatives as potent gamma-secretase modulators. Bioorg Med Chem Lett 2010;20:1269-71
-
(2010)
Bioorg Med Chem Lett
, Issue.20
, pp. 1269-1271
-
-
Rivkin, A.1
Ahearn, S.P.2
Chichetti, S.M.3
-
127
-
-
77949490327
-
Purine derivatives as potent gamma-secretase modulators
-
Rivkin A, Ahearn SP, Chichetti SM, et al Purine derivatives as potent gamma-secretase modulators. Bioorg Med Chem Lett 2010;20:2279-82
-
(2010)
Bioorg Med Chem Lett
, Issue.20
, pp. 2279-2282
-
-
Rivkin, A.1
Ahearn, S.P.2
Chichetti, S.M.3
-
128
-
-
77953680038
-
Defining desirable central nervous system drug space through the alignment of molecular properties, in vitro ADME, and safety attributes
-
Wager TT, Ramalakshmi YC, Hou X, et al Defining desirable central nervous system drug space through the alignment of molecular properties, in vitro ADME, and safety attributes. ACS Chem Neurosci 2010;1:420-35
-
(2010)
ACS Chem Neurosci
, Issue.1
, pp. 420-435
-
-
Wager, T.T.1
Ramalakshmi, Y.C.2
Hou, X.3
-
129
-
-
33646715920
-
The influence of target family and functional activity on the physicochemical properties of pre-clinical compounds
-
Morphy R. The influence of target family and functional activity on the physicochemical properties of pre-clinical compounds. J Med Chem 2006;49:2969-78
-
(2006)
J Med Chem
, vol.49
, pp. 2969-2978
-
-
Morphy, R.1
-
130
-
-
49849094738
-
Physiochemical drug properties associated with in vivo toxicological outcomes
-
Hughes JD, Blagg J, Price DA, et al Physiochemical drug properties associated with in vivo toxicological outcomes. Bioorg Med Chem Lett 2008;18:4872-5
-
(2008)
Bioorg Med Chem Lett
, vol.18
, pp. 4872-485
-
-
Hughes, J.D.1
Blagg, J.2
Price, D.A.3
|