-
1
-
-
5644239087
-
Alzheimer disease: Mechanistic understanding predicts novel therapies
-
Selkoe DJ. Alzheimer disease: mechanistic understanding predicts novel therapies. Ann Intern Med 2004; 140: 627-38.
-
(2004)
Ann. Intern. Med.
, vol.140
, pp. 627-638
-
-
Selkoe, D.J.1
-
2
-
-
1442286389
-
Management of mild to moderate Alzheimer disease: Defining the role of rivastigmine
-
Plosker GL, Keating GM. Management of mild to moderate Alzheimer disease: defining the role of rivastigmine. Disease Management & Health Outcomes 2004; 12: 55-72.
-
(2004)
Disease Management & Health Outcomes
, vol.12
, pp. 55-72
-
-
Plosker, G.L.1
Keating, G.M.2
-
4
-
-
0036653703
-
Recent advances in the development of g-secretase inhibitors
-
Josien H. Recent advances in the development of g-secretase inhibitors. Curr Opin Drug Discov Devel 2002; 5: 513-25.
-
(2002)
Curr. Opin. Drug Discov. Devel.
, vol.5
, pp. 513-525
-
-
Josien, H.1
-
5
-
-
0142092495
-
Human beta-secretase (BACE) and BACE inhibitors
-
John V, Beck James P, Bienkowski Michael J, Sinha S, Heinrikson Robert L. Human beta-secretase (BACE) and BACE inhibitors. J Med Chem 2003; 46: 4625-30.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 4625-4630
-
-
John, V.1
Beck James, P.2
Bienkowski Michael, J.3
Sinha, S.4
Heinrikson Robert, L.5
-
6
-
-
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 USA 2000; 97: 1456-60.
-
(2000)
Proc. Natl. Acad. Sci. USA
, vol.97
, pp. 1456-1460
-
-
Lin, X.1
Koelsch, G.2
Wu, S.3
Downs, D.4
Dashti, A.5
Tang, J.6
-
7
-
-
0033382226
-
Identification of a Novel Aspartic Protease (Asp 2) as β-Secretase
-
Hussain I, Powell D, Howlett DR, Tew DG, Meek TD, Chapman C, et al. Identification of a Novel Aspartic Protease (Asp 2) as β-Secretase. Mol Cell Neurosci 1999; 14: 419-27.
-
(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
-
8
-
-
0033518264
-
Membrane-anchored aspartyl protease with Alzheimer's disease β-secretase activity
-
Yan R, Bienkowski MJ, Shuck ME, Miao H, Tory MC, Pauley AM, et al. Membrane-anchored aspartyl protease with Alzheimer's disease β-secretase activity. Nature (London) 1999; 402: 533-7.
-
(1999)
Nature (London)
, 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
-
9
-
-
0033518251
-
Purification and cloning of amyloid precursor protein β-secretase from human brain
-
Sinha S, Anderson JP; Barbour R, Basi GS, Caccavello R, Davis D, et al. Purification and cloning of amyloid precursor protein β-secretase from human brain. Nature (London) 1999; 402: 537-40.
-
(1999)
Nature (London)
, 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
-
10
-
-
0033595706
-
β-Secretase cleavage of Alzheimer's amyloid precursor protein by the transmembrane aspartic protease BACE
-
Vassar R, Bennett BD, Babu-Khan S, Kahn S, Mendiaz EA, Denis P, et al. β-Secretase cleavage of Alzheimer's amyloid precursor protein by the transmembrane aspartic protease BACE. Science (Washington, D. C.) 1999; 286: 735-41.
-
(1999)
Science (Washington, D. C.)
, 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
-
11
-
-
0035965275
-
The transmembrane domain of the Alzheimer's β-secretase (BACE1) determines its late Golgi localization and access to β-amyloid precursor protein (APP) substrate
-
Yan R, Han P, Miao H, Greengard P, Xu H. The transmembrane domain of the Alzheimer's β-secretase (BACE1) determines its late Golgi localization and access to β-amyloid precursor protein (APP) substrate. J Biol Chem 2001; 276: 36788-96.
-
(2001)
J. Biol. Chem.
, vol.276
, pp. 36788-36796
-
-
Yan, R.1
Han, P.2
Miao, H.3
Greengard, P.4
Xu, H.5
-
12
-
-
0034721842
-
Maturation and endosomal targeting of β-site amyloid precursor protein-cleaving enzyme. The Alzheimer's disease β-secretase
-
Huse JT, Pijak DS, Leslie GJ, Lee VMY, Doms RW. Maturation and endosomal targeting of β-site amyloid precursor protein-cleaving enzyme. The Alzheimer's disease β-secretase. J Biol Chem 2000; 275: 33729-37.
-
(2000)
J. Biol. Chem.
, vol.275
, pp. 33729-33737
-
-
Huse, J.T.1
Pijak, D.S.2
Leslie, G.J.3
Lee, V.M.Y.4
Doms, R.W.5
-
13
-
-
0842309491
-
β-Secretase inhibition for the treatment of Alzheimer's disease - Promise and challenge
-
Citron M. β-Secretase inhibition for the treatment of Alzheimer's disease - promise and challenge. Trends Pharmacol Sci 2004; 25: 92-7.
-
(2004)
Trends Pharmacol. Sci.
, vol.25
, pp. 92-97
-
-
Citron, M.1
-
14
-
-
0036861132
-
Emerging Alzheimer's disease therapies: Inhibition of β-secretase
-
Citron M. Emerging Alzheimer's disease therapies: inhibition of β-secretase. Neurobiol Aging 2002; 23: 1017-22.
-
(2002)
Neurobiol. Aging
, vol.23
, pp. 1017-1022
-
-
Citron, M.1
-
15
-
-
4344630985
-
BACE1. The β-secretase enzyme in Alzheimer's disease
-
Vassar R. BACE1. The β-secretase enzyme in Alzheimer's disease. J Mol Neurosci 2004; 23: 105-13.
-
(2004)
J. Mol. Neurosci.
, vol.23
, pp. 105-113
-
-
Vassar, R.1
-
16
-
-
0037038816
-
β-Secretase (BACE) as a drug target for Alzheimer's disease
-
Vassar R. β-Secretase (BACE) as a drug target for Alzheimer's disease. Adv Drug Deliv Rev 2002; 54: 1589-602.
-
(2002)
Adv. Drug Deliv. Rev.
, vol.54
, pp. 1589-1602
-
-
Vassar, R.1
-
17
-
-
0034617199
-
Expression analysis of BACE2 in brain and peripheral tissues
-
Bennett BD, Babu-Khan S, Loeloff R, Louis J-C, Curran E, Citron M, et al. Expression analysis of BACE2 in brain and peripheral tissues. J Biol Chem 2000; 275: 20647-51.
-
(2000)
J. Biol. Chem.
, vol.275
, pp. 20647-20651
-
-
Bennett, B.D.1
Babu-Khan, S.2
Loeloff, R.3
Louis, J.-C.4
Curran, E.5
Citron, M.6
-
18
-
-
0033970139
-
The gene encoding DRAP (BACE2), a glycosylated transmembrane protein of the aspartic, protease family, maps to the Down critical region
-
Acquati F, Accarino M, Nucci C, Fumagalli P, Jovine L, Ottolenghi S, et al. The gene encoding DRAP (BACE2), a glycosylated transmembrane protein of the aspartic, protease family, maps to the Down critical region. FEBS Lett 2000; 468: 59-64.
-
(2000)
FEBS Lett.
, vol.468
, pp. 59-64
-
-
Acquati, F.1
Accarino, M.2
Nucci, C.3
Fumagalli, P.4
Jovine, L.5
Ottolenghi, S.6
-
19
-
-
0034662929
-
BACE2, a β-secretase homolog, cleaves at the β site and within the amyloid-β region of the amyloid-β precursor protein
-
Farzan M, Schnitzler CE, Vasilieva N, Leung D, Choe H. BACE2, a β-secretase homolog, cleaves at the β site and within the amyloid-β region of the amyloid-β precursor protein. Proc Natl Acad Sci USA 2000; 97: 9712-7.
-
(2000)
Proc. Natl. Acad. Sci. USA
, vol.97
, pp. 9712-9717
-
-
Farzan, M.1
Schnitzler, C.E.2
Vasilieva, N.3
Leung, D.4
Choe, H.5
-
20
-
-
0033819772
-
A new aspartyl protease on 21q22.3, BACE2, is highly similar to Alzheimer's amyloid precursor protein β-secretase
-
Solans A, Estivill X, de la Luna S. A new aspartyl protease on 21q22.3, BACE2, is highly similar to Alzheimer's amyloid precursor protein β-secretase. Cytogenet Cell Genet 2000; 89: 177-84.
-
(2000)
Cytogenet. Cell Genet.
, vol.89
, pp. 177-184
-
-
Solans, A.1
Estivill, X.2
de la Luna, S.3
-
21
-
-
0034533808
-
ASP1 (BACE2) Cleaves the Amyloid Precursor Protein at the β-Secretase Site
-
Hussain I, Powell DJ, Howlett DR, Chapman GA, Gilmour L Murdock PR, et al. ASP1 (BACE2) Cleaves the Amyloid Precursor Protein at the β-Secretase Site. Mol Cell Neurosci 2000; 16: 609-19.
-
(2000)
Mol. Cell Neurosci.
, vol.16
, pp. 609-619
-
-
Hussain, I.1
Powell, D.J.2
Howlett, D.R.3
Chapman, G.A.4
Gilmour, L.5
Murdock, P.R.6
-
22
-
-
0042334543
-
BACE1 (β-secretase) knockout mice do not acquire compensatory gene expression changes or develop neural lesions over time
-
Luo Y, Bolon B, Damore MA, Fitzpatrick D, Liu H, Zhang J, et al. BACE1 (β-secretase) knockout mice do not acquire compensatory gene expression changes or develop neural lesions over time. Neurobiol Dis 2003; 14: 81-8.
-
(2003)
Neurobiol. Dis.
, vol.14
, pp. 81-88
-
-
Luo, Y.1
Bolon, B.2
Damore, M.A.3
Fitzpatrick, D.4
Liu, H.5
Zhang, J.6
-
23
-
-
0033998647
-
Conformational flexibility of the catalytic Asp dyad in HIV-1 protease: An ab initio study on the free enzyme
-
Piana S, Carloni P. Conformational flexibility of the catalytic Asp dyad in HIV-1 protease: an ab initio study on the free enzyme. Proteins: Struct, Funct, Genet 2000; 39: 26-36.
-
(2000)
Proteins: Struct, Funct, Genet.
, vol.39
, pp. 26-36
-
-
Piana, S.1
Carloni, P.2
-
24
-
-
0034778987
-
Follow the protons: A low-barrier hydrogen bond unifies the mechanisms of the aspartic proteases
-
Northrop DB. Follow the protons: A low-barrier hydrogen bond unifies the mechanisms of the aspartic proteases. Acc Chem Res 2001; 34: 790-7.
-
(2001)
Acc. Chem. Res.
, vol.34
, pp. 790-797
-
-
Northrop, D.B.1
-
25
-
-
0033518251
-
Purification and cloning of amyloid precursor protein beta-secretase from human brain
-
Sinha S, Anderson JP, Barbour R, Basi GS, Caccavello R, Davis D, et al. Purification and cloning of amyloid precursor protein beta-secretase from human brain. Nature 1999; 402: 537-40.
-
(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
-
26
-
-
0037122704
-
Design of substrate-based inhibitors of human beta-secretase
-
Tung JS, Davis DL, Anderson JP, Walker DE, Mamo S, Jewett N, et al. Design of substrate-based inhibitors of human beta-secretase. J Med Chem 2002; 45: 259-62.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 259-262
-
-
Tung, J.S.1
Davis, D.L.2
Anderson, J.P.3
Walker, D.E.4
Mamo, S.5
Jewett, N.6
-
27
-
-
24944474956
-
Preparation of statine-derived tetrapeptides as inhibitors of β-secretase
-
2000077030
-
John V, Tung J, Fang L, Mamo SS. Preparation of statine-derived tetrapeptides as inhibitors of β-secretase. PCT Int Appl 2000077030.
-
PCT Int. Appl.
-
-
John, V.1
Tung, J.2
Fang, L.3
Mamo, S.S.4
-
28
-
-
2942615456
-
Synthesis and SAR of bis-statine based peptides as BACE 1 inhibitors
-
Hu B, Fan KY, Bridges K, Chopra R, Lovering F, Cole D, et al. Synthesis and SAR of bis-statine based peptides as BACE 1 inhibitors. Bioorg Med Chem Lett 2004; 14: 3457-60.
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 3457-3460
-
-
Hu, B.1
Fan, K.Y.2
Bridges, K.3
Chopra, R.4
Lovering, F.5
Cole, D.6
-
29
-
-
0037740743
-
Design and synthesis of statine-based cell-permeable peptidomimetic inhibitors of human beta-secretase
-
Hom RK, Fang LY, Mamo S, Tung JS, Guinn AC, Walker DE, et al. Design and synthesis of statine-based cell-permeable peptidomimetic inhibitors of human beta-secretase. J Med Chem 2003; 46: 1799-802.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 1799-1802
-
-
Hom, R.K.1
Fang, L.Y.2
Mamo, S.3
Tung, J.S.4
Guinn, A.C.5
Walker, D.E.6
-
30
-
-
0345358518
-
Design and synthesis of statine-Containing BACE inhibitors
-
Hu J, Cwi CL, Smiley DL, Timm D, Erickson JA, McGee JE, et al. Design and synthesis of statine-Containing BACE inhibitors. Bioorg Med Chem Lett 2003; 13: 4335-9.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 4335-4339
-
-
Hu, J.1
Cwi, C.L.2
Smiley, D.L.3
Timm, D.4
Erickson, J.A.5
McGee, J.E.6
-
31
-
-
0035855914
-
Design and Synthesis of Potent C2-Symmetric Diol-Based HIV-1 Protease Inhibitors: Effects of Fluoro Substitution
-
Pyring D, Lindberg J, Rosenquist A, Zuccarello G, Kvarnstroem I, Zhang H, et al. Design and Synthesis of Potent C2-Symmetric Diol-Based HIV-1 Protease Inhibitors: Effects of Fluoro Substitution. J Med Chem 2001; 44: 3083-91.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 3083-3091
-
-
Pyring, D.1
Lindberg, J.2
Rosenquist, A.3
Zuccarello, G.4
Kvarnstroem, I.5
Zhang, H.6
-
32
-
-
0028899247
-
Isophthalic acid derivatives: Amino acid surrogates for the inhibition of HIV-1 protease
-
Kaldor SW, Dressman BA, Hammond M, Appelt K, Burgess J, Lubbehusen PP, et al. Isophthalic acid derivatives: amino acid surrogates for the inhibition of HIV-1 protease. Bioorg Med Chem Lett 1995; 5: 721-6.
-
(1995)
Bioorg. Med. Chem. Lett.
, vol.5
, pp. 721-726
-
-
Kaldor, S.W.1
Dressman, B.A.2
Hammond, M.3
Appelt, K.4
Burgess, J.5
Lubbehusen, P.P.6
-
33
-
-
9144267815
-
Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase
-
Hom RK, Gailunas AF, Mamo S, Fang LY, Tung JS, Walker DE, et al. Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase. J Med Chem 2004; 47: 158-64.
-
(2004)
J. Med. Chem.
, vol.47
, pp. 158-164
-
-
Hom, R.K.1
Gailunas, A.F.2
Mamo, S.3
Fang, L.Y.4
Tung, J.S.5
Walker, D.E.6
-
34
-
-
24944534627
-
Preparation of statine derivatives for the treatment of Alzheimer's disease
-
2003006021
-
Schostarez HJ, Chrusciel RA. Preparation of statine derivatives for the treatment of Alzheimer's disease. PCT Int Appl 2003006021.
-
PCT Int. Appl.
-
-
Schostarez, H.J.1
Chrusciel, R.A.2
-
35
-
-
0028841007
-
3D-Quantitative Structure-Activity Relationships of Human Immunodeficiency Virus Type-1 Proteinase Inhibitors: Comparative Molecular Field Analysis of 2-Heterosubstituted Statine Derivatives-Implications for the Design of Novel Inhibitors
-
Kroemer RT, Ettmayer P, Hecht P. 3D-Quantitative Structure-Activity Relationships of Human Immunodeficiency Virus Type-1 Proteinase Inhibitors: Comparative Molecular Field Analysis of 2-Heterosubstituted Statine Derivatives-Implications for the Design of Novel Inhibitors. J Med Chem 1995; 38: 4917-28.
-
(1995)
J. Med. Chem.
, vol.38
, pp. 4917-4928
-
-
Kroemer, R.T.1
Ettmayer, P.2
Hecht, P.3
-
36
-
-
0028143193
-
Inhibitors of HIV-1 Proteinase Containing 2-Heterosubstituted 4-Amino-3-hydroxy-5-phenylpentanoic Acid: Synthesis, Enzyme Inhibition, and Antiviral Activity
-
Scholz D, Billich A, Charpiot B, Ettmayer P, Lehr P, Rosenwirth B, et al. Inhibitors of HIV-1 Proteinase Containing 2-Heterosubstituted 4-Amino-3-hydroxy-5-phenylpentanoic Acid: Synthesis, Enzyme Inhibition, and Antiviral Activity. J Med Chem 1994; 37: 3079-89.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 3079-3089
-
-
Scholz, D.1
Billich, A.2
Charpiot, B.3
Ettmayer, P.4
Lehr, P.5
Rosenwirth, B.6
-
37
-
-
0344927114
-
KMI-008, a novel beta-secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-state mimic: Design and synthesis of substrate-based octapeptides
-
Shuto D, Kasai S, Kimura T Liu P, Hidaka K, Hamada T, et al. KMI-008, a novel beta-secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-state mimic: design and synthesis of substrate-based octapeptides. Bioorg Med Chem Lett 2003; 13: 4273-6.
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 4273-4276
-
-
Shuto, D.1
Kasai, S.2
Kimura, T.3
Liu, P.4
Hidaka, K.5
Hamada, T.6
-
38
-
-
10744219775
-
KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine
-
Kimura T, Shuto D, Kasai S, Liu P, Hidaka K, Hamada T, et al. KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine. Bioorg Med Chem Lett 2004; 14: 1527-31.
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 1527-1531
-
-
Kimura, T.1
Shuto, D.2
Kasai, S.3
Liu, P.4
Hidaka, K.5
Hamada, T.6
-
39
-
-
0029801256
-
Synthesis and pharmacological evaluation of CGP 57813 and CGP 61755, HIV-1 protease inhibitors from the Phe-c-Phe peptidomimetic class
-
Cozens RM, Bold G, Capraro HG, Faessler A, Mestan J, Lang M, et al. Synthesis and pharmacological evaluation of CGP 57813 and CGP 61755, HIV-1 protease inhibitors from the Phe-c-Phe peptidomimetic class. Antiviral Chemistry & Chemotherapy 1996; 7: 294-9.
-
(1996)
Antiviral Chemistry & Chemotherapy
, vol.7
, pp. 294-299
-
-
Cozens, R.M.1
Bold, G.2
Capraro, H.G.3
Faessler, A.4
Mestan, J.5
Lang, M.6
-
40
-
-
0034639925
-
Design of potent inhibitors for human brain memapsin 2 (β-secretase)
-
Ghosh AK, Shin D, Downs D, Koelsch G, Lin X, Ermolieff J, et al. Design of potent inhibitors for human brain memapsin 2 (β-secretase). J Am Chem Soc 2000; 122: 3522-3.
-
(2000)
J. Am. Chem. Soc.
, vol.122
, pp. 3522-3523
-
-
Ghosh, A.K.1
Shin, D.2
Downs, D.3
Koelsch, G.4
Lin, X.5
Ermolieff, J.6
-
42
-
-
0034613320
-
Structure of the protease domain of memapsin 2 (β-secretase) complexed with inhibitor
-
Hong L, Koelsch G, Lin X, Wu S, Terzyan S, Ghosh AK, et al. Structure of the protease domain of memapsin 2 (β-secretase) complexed with inhibitor. Science (Washington, D. C.) 2000; 290: 150-3.
-
(2000)
Science (Washington, D. C.)
, vol.290
, pp. 150-153
-
-
Hong, L.1
Koelsch, G.2
Lin, X.3
Wu, S.4
Terzyan, S.5
Ghosh, A.K.6
-
43
-
-
0035833972
-
Subsite Specificity of Memapsin 2 (β-Secretase): Implications for Inhibitor Design
-
[Erratum for Volume 40, Number 34, August 28, 2001, pages 10001-10]
-
Turner RT III, Koelsch G, Hong L, Castanheira P, Ermolieff J, Ghosh AK, et al. Subsite Specificity of Memapsin 2 (β-Secretase): Implications for Inhibitor Design [Erratum for Volume 40, Number 34, August 28, 2001, pages 10001-10]. Biochemistry 2001; 40: 12230.
-
(2001)
Biochemistry
, vol.40
, pp. 12230
-
-
Turner III, R.T.1
Koelsch, G.2
Hong, L.3
Castanheira, P.4
Ermolieff, J.5
Ghosh, A.K.6
-
44
-
-
0035964269
-
Subsite specificity of memapsin 2 (beta-secretase): Implications for inhibitor design
-
Turner RT 3rd, Koelsch G, Hong L, Castanheira P, Ermolieff J, Ghosh AK, et al. Subsite specificity of memapsin 2 (beta-secretase): implications for inhibitor design. Biochemistry 2001; 40: 10001-6.
-
(2001)
Biochemistry
, vol.40
, pp. 10001-10006
-
-
Turner III, R.T.1
Koelsch, G.2
Hong, L.3
Castanheira, P.4
Ermolieff, J.5
Ghosh, A.K.6
-
45
-
-
0036714840
-
Crystal structure of memapsin 2 (beta-secretase) in complex with an inhibitor OM00-3
-
Hong L, Turner RT 3rd, Koelsch G, Shin D, Ghosh Arun K, Tang J. Crystal structure of memapsin 2 (beta-secretase) in complex with an inhibitor OM00-3. Biochemistry 2002; 41: 10963-7.
-
(2002)
Biochemistry
, vol.41
, pp. 10963-10967
-
-
Hong, L.1
Turner III, R.T.2
Koelsch, G.3
Shin, D.4
Ghosh Arun, K.5
Tang, J.6
-
46
-
-
0346256828
-
Phe*-Ala-based pentapeptide mimetics are BACE inhibitors: P2 and P3 SAR
-
Lamar J, Hu J, Bueno AB, Yang H-C, Guo D, Copp JD, et al. Phe*-Ala-based pentapeptide mimetics are BACE inhibitors: P2 and P3 SAR. Bioorg Med Chem Lett 2004; 14: 239-43.
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 239-243
-
-
Lamar, J.1
Hu, J.2
Bueno, A.B.3
Yang, H.-C.4
Guo, D.5
Copp, J.D.6
-
47
-
-
0037085353
-
Substrate and inhibitor profile of BACE (beta-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 (beta-secretase) and comparison with other mammalian aspartic proteases. J Biol Chem 2002; 277: 4687-93.
-
(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
-
48
-
-
0035974650
-
Structure-based design: Potent inhibitors of human brain memapsin 2 (beta-secretase)
-
Ghosh AK, Bilcer G, Harwood C, Kawahama R, Shin D, Hussain KA, et al. Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase). J Med Chem 2001; 44: 2865-8.
-
(2001)
J. Med. Chem.
, vol.44
, pp. 2865-2868
-
-
Ghosh, A.K.1
Bilcer, G.2
Harwood, C.3
Kawahama, R.4
Shin, D.5
Hussain, K.A.6
-
49
-
-
24944491853
-
Inhibitors of memapsin 2 and their use in Alzheimer's disease treatment
-
2002053594
-
Tang JJN, Koelsch G, Ghosh AK Inhibitors of memapsin 2 and their use in Alzheimer's disease treatment. PCT Int Appl 2002053594.
-
PCT Int. Appl.
-
-
Tang, J.J.N.1
Koelsch, G.2
Ghosh, A.K.3
-
50
-
-
24944530610
-
Design of β-secretase inhibitors for treatment of Alzheimer's disease based on crystal structures of β-secretase and side chain interactions in inhibitor complexes
-
2003039454
-
Ghosh AK, Tang J, Bilcer G, Chang W, Hong L, Koetsch G, et al. Design of β-secretase inhibitors for treatment of Alzheimer's disease based on crystal structures of β-secretase and side chain interactions in inhibitor complexes. PCT Int Appl 2003039454.
-
PCT Int. Appl.
-
-
Ghosh, A.K.1
Tang, J.2
Bilcer, G.3
Chang, W.4
Hong, L.5
Koetsch, G.6
-
52
-
-
0348147637
-
P3 cap modified Phe*-Ala series BACE inhibitors
-
Chen S-H, Lamar J, Guo D, Kohn T, Yang H-C, McGee J, et al. P3 cap modified Phe*-Ala series BACE inhibitors. Bioorg Med Chem Lett 2004; 14: 245-50.
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 245-250
-
-
Chen, S.-H.1
Lamar, J.2
Guo, D.3
Kohn, T.4
Yang, H.-C.5
McGee, J.6
-
53
-
-
1642477688
-
Rational design and synthesis of selective BACE-1 inhibitors
-
Brady SF, Singh S, Crouthamel M-C, Holloway MK, Coburn CA, Garsky VM, et al. Rational design and synthesis of selective BACE-1 inhibitors. Bioorg Med Chem Lett 2004; 14: 601-4.
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 601-604
-
-
Brady, S.F.1
Singh, S.2
Crouthamel, M.-C.3
Holloway, M.K.4
Coburn, C.A.5
Garsky, V.M.6
-
54
-
-
24944511711
-
Synthesis of β-secretase inhibitors for treating Alzheimer's disease
-
2003099202
-
Lai M-T, Crouthamel MC, Brady SF. Synthesis of β-secretase inhibitors for treating Alzheimer's disease. PCT Int Appl 2003099202.
-
PCT Int. Appl.
-
-
Lai, M.-T.1
Crouthamel, M.C.2
Brady, S.F.3
-
55
-
-
24944502420
-
Preparation of amino carboxamide derivatives as aspartyl protease inhibitors
-
2003106405
-
Yang W, Cary DR, Jacobs JW, Lu W, Lu Y, Sun J, et al. Preparation of amino carboxamide derivatives as aspartyl protease inhibitors. PCT Int Appl 2003106405.
-
PCT Int. Appl.
-
-
Yang, W.1
Cary, D.R.2
Jacobs, J.W.3
Lu, W.4
Lu, Y.5
Sun, J.6
-
56
-
-
24944461253
-
Hydroxyethylene compounds with Asp-2 inhibitory activity
-
2003045903
-
Faller A, Milner PH, Ward JG. Hydroxyethylene compounds with Asp-2 inhibitory activity. PCT Int Appl 2003045903.
-
PCT Int. Appl.
-
-
Faller, A.1
Milner, P.H.2
Ward, J.G.3
-
57
-
-
24944480097
-
Preparation of hydroxyethylenes with peptide subunits for pharmaceutical use in the treatment of Alzheimer's disease
-
2001070672
-
Hom R, Mamo S, Tung J, Gailunas A, John V, Fang L. Preparation of hydroxyethylenes with peptide subunits for pharmaceutical use in the treatment of Alzheimer's disease. PCT Int Appl 2001070672.
-
PCT Int. Appl.
-
-
Hom, R.1
Mamo, S.2
Tung, J.3
Gailunas, A.4
John, V.5
Fang, L.6
-
58
-
-
24944532294
-
Preparation of 5-amino-4-hydroxypentanoic acid derivatives for treating Alzheimer's disease
-
2003013881
-
Hom R, Mamo S, Tung J, Gailunas A, John V, Fang L. Preparation of 5-amino-4-hydroxypentanoic acid derivatives for treating Alzheimer's disease. U.S. Pat Appl Publ 2003013881.
-
U.S. Pat. Appl. Publ.
-
-
Hom, R.1
Mamo, S.2
Tung, J.3
Gailunas, A.4
John, V.5
Fang, L.6
-
59
-
-
0028222149
-
L-735, 524: An orally bioavailable human immunodeficiency virus type 1 protease inhibitor
-
Vacca JP, Dorsey BD, Schleif WA, Levin RB, McDaniel SL, Darke PL, et al. L-735, 524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor. Proc Natl Acad Sci USA 1994; 91: 4096-100.
-
(1994)
Proc. Natl. Acad. Sci. USA
, vol.91
, pp. 4096-4100
-
-
Vacca, J.P.1
Dorsey, B.D.2
Schleif, W.A.3
Levin, R.B.4
McDaniel, S.L.5
Darke, P.L.6
-
60
-
-
24944586529
-
Preparation of allylamides useful in the treatment of Alzheimer's disease
-
2003030886
-
Hom R. Preparation of allylamides useful in the treatment of Alzheimer's disease. PCT Int Appl 2003030886.
-
PCT Int. Appl.
-
-
Hom, R.1
-
61
-
-
0028846226
-
Crystal structure of HIV-1 protease in complex with VX-478, a potent and orally bioavailable inhibitor of the enzyme
-
Kim EE, Baker CT, Dwyer MD, Murcko MA, Rao BG, Tung RD, et al. Crystal structure of HIV-1 protease in complex with VX-478, a potent and orally bioavailable inhibitor of the enzyme. J Am Chem Soc 1995; 117: 1181-2.
-
(1995)
J. Am. Chem. Soc.
, vol.117
, pp. 1181-1182
-
-
Kim, E.E.1
Baker, C.T.2
Dwyer, M.D.3
Murcko, M.A.4
Rao, B.G.5
Tung, R.D.6
-
62
-
-
0037187402
-
Hydroxyethylamin Isostere of an HIV-1 Protease Inhibitor Prefers Its Amine to the Hydroxy Group in Binding to Catalytic Aspartates. A Synchrotron Study of HIV-1 Protease in Complex with a Peptidomimetic Inhibitor
-
Dohnalek J, Hasek J, Duskova J, Petrokova H, Hradilek M, Soucek M, et al. Hydroxyethylamin Isostere of an HIV-1 Protease Inhibitor Prefers Its Amine to the Hydroxy Group in Binding to Catalytic Aspartates. A Synchrotron Study of HIV-1 Protease in Complex with a Peptidomimetic Inhibitor. J Med Chem 2002; 45: 1432-8.
-
(2002)
J. Med. Chem.
, vol.45
, pp. 1432-1438
-
-
Dohnalek, J.1
Hasek, J.2
Duskova, J.3
Petrokova, H.4
Hradilek, M.5
Soucek, M.6
-
63
-
-
0141618463
-
Synthesis of potent beta-secretase inhibitors containing a hydroxyethylamine dipeptide isostere and their structure-activity relationship studies
-
Tamamura H, Kato T, Otaka A, Fujii N. Synthesis of potent beta-secretase inhibitors containing a hydroxyethylamine dipeptide isostere and their structure-activity relationship studies. Org Biomol Chem 2003; 1: 2468-73.
-
(2003)
Org. Biomol. Chem.
, vol.1
, pp. 2468-2473
-
-
Tamamura, H.1
Kato, T.2
Otaka, A.3
Fujii, N.4
-
64
-
-
24944485241
-
-
Press Release, Elan Corp. plc, August 10
-
Press Release, Elan Corp. plc, August 10, 2000.
-
(2000)
-
-
-
65
-
-
24944570281
-
Preparation of substituted amines to treat Alzheimer's disease
-
2002002512
-
Maillaird M, Hom C, Gailunas A, Jagodzinska B, Fang LY, John V, et al. Preparation of substituted amines to treat Alzheimer's disease. PCT Int Appl 2002002512.
-
PCT Int. Appl.
-
-
Maillaird, M.1
Hom, C.2
Gailunas, A.3
Jagodzinska, B.4
Fang, L.Y.5
John, V.6
-
66
-
-
24944589737
-
Preparation of substituted amines for treating Alzheimer's disease
-
2002002505
-
Fang LY, Hom R, John V, Maillaird M. Preparation of substituted amines for treating Alzheimer's disease. PCT Int Appl 2002002505.
-
PCT Int. Appl.
-
-
Fang, L.Y.1
Hom, R.2
John, V.3
Maillaird, M.4
-
67
-
-
24944587331
-
Compounds to treat Alzheimer's disease
-
2002002506
-
Fang LY. John V. Compounds to treat Alzheimer's disease. PCT Int Appl 2002002506.
-
PCT Int. Appl.
-
-
Fang, L.Y.1
John, V.2
-
68
-
-
24944502873
-
Preparation of disubstituted amines for treating Alzheimer's disease
-
2002002520
-
Beck JP, Gailunas A, Hom R, Jagodzinska B, John V, Maillaird M. Preparation of disubstituted amines for treating Alzheimer's disease. PCT Int Appl 2002002520.
-
PCT Int. Appl.
-
-
Beck, J.P.1
Gailunas, A.2
Hom, R.3
Jagodzinska, B.4
John, V.5
Maillaird, M.6
-
69
-
-
24944502873
-
Preparation of disubstituted amines for treating Alzheimer's disease
-
2002002518
-
Beck JP, Gailunas A, Hom R, Jagodzinska B, John V, Maillaird M. Preparation of disubstituted amines for treating Alzheimer's disease. PCT Int Appl 2002002518.
-
PCT Int. Appl.
-
-
Beck, J.P.1
Gailunas, A.2
Hom, R.3
Jagodzinska, B.4
John, V.5
Maillaird, M.6
-
70
-
-
2542428231
-
Atazanavir: Improving the HIV protcase inhibitor class
-
Becker S. Atazanavir: improving the HIV protcase inhibitor class. Expert Review of Anti-Infective Therapy 2003; 1: 403-13.
-
(2003)
Expert Review of Anti-Infective Therapy
, vol.1
, pp. 403-413
-
-
Becker, S.1
-
71
-
-
24944544086
-
Preparation of substituted amines prodrugs useful in treating Alzheimer's disease
-
2003072535
-
Varghese J, Jagodzinska B, Maillard M, Beck JP, Tenbrink RE, Getman D. Preparation of substituted amines prodrugs useful in treating Alzheimer's disease. PCT Int Appl 2003072535.
-
PCT Int. Appl.
-
-
Varghese, J.1
Jagodzinska, B.2
Maillard, M.3
Beck, J.P.4
Tenbrink, R.E.5
Getman, D.6
-
72
-
-
24944483322
-
Preparation of 1, 3-diamino-2-hydroxypropane derivatives as beta-secretase enzyme inhibitors
-
2004022523
-
Fobian YM, Freskos JN, Jagodzinska BA. Preparation of 1, 3-diamino-2-hydroxypropane derivatives as beta-secretase enzyme inhibitors. PCT Int Appl 2004022523.
-
PCT Int. Appl.
-
-
Fobian, Y.M.1
Freskos, J.N.2
Jagodzinska, B.A.3
-
73
-
-
0027210633
-
Orally active water-soluble N, O-acyl transfer products of a β, γ-bishydroxyl amide containing renin inhibitor
-
Hurley TR, Colson CE, Hicks G, Ryan MJ. Orally active water-soluble N, O-acyl transfer products of a β, γ-bishydroxyl amide containing renin inhibitor. J Med Chem 1993; 36: 1496-8.
-
(1993)
J. Med. Chem.
, vol.36
, pp. 1496-1498
-
-
Hurley, T.R.1
Colson, C.E.2
Hicks, G.3
Ryan, M.J.4
-
74
-
-
0032873518
-
Design of small peptidomimetic HIV-1 protease inhibitors and prodrug forms
-
Kiso Y, Matsumoto H, Yamaguchi S, Kimura T. Design of small peptidomimetic HIV-1 protease inhibitors and prodrug forms. Lett Pep Sci 1999; 6: 275-81.
-
(1999)
Lett. Pep. Sci.
, vol.6
, pp. 275-281
-
-
Kiso, Y.1
Matsumoto, H.2
Yamaguchi, S.3
Kimura, T.4
-
75
-
-
0036973331
-
New water-soluble prodrugs of HIV protease inhibitors based on O -> N intramolecular acyl migration
-
Hamada Y, Ohtake J, Sohma Y, Kimura T, Hayashi Y, Kiso Y. New water-soluble prodrugs of HIV protease inhibitors based on O -> N intramolecular acyl migration. Bioorg Med Chem 2002; 10: 4155-67.
-
(2002)
Bioorg. Med. Chem.
, vol.10
, pp. 4155-4167
-
-
Hamada, Y.1
Ohtake, J.2
Sohma, Y.3
Kimura, T.4
Hayashi, Y.5
Kiso, Y.6
-
76
-
-
0346671290
-
Water-soluble prodrugs of dipeptide HIV protease inhibitors based on O-> N intramolecular acyl migration: Design, synthesis and kinetic study
-
Hamada Y, Matsumoto H, Yamaguchi S, Kimura T, Hayashi Y, Kiso Y. Water-soluble prodrugs of dipeptide HIV protease inhibitors based on O-> N intramolecular acyl migration: Design, synthesis and kinetic study. Bioorg Med Chem 2004; 12: 159-70.
-
(2004)
Bioorg. Med. Chem.
, vol.12
, pp. 159-170
-
-
Hamada, Y.1
Matsumoto, H.2
Yamaguchi, S.3
Kimura, T.4
Hayashi, Y.5
Kiso, Y.6
-
78
-
-
24944435629
-
Preparation of peptide-related hydrazine derivatives for treating Alzheimer's disease
-
2002100410
-
Schostarez H, Chrusciel RA. Preparation of peptide-related hydrazine derivatives for treating Alzheimer's disease. PCT Int Appl 2002100410.
-
PCT Int. Appl.
-
-
Schostarez, H.1
Chrusciel, R.A.2
-
80
-
-
24944516356
-
Preparation of N-(3-amino-2-hydroxy-propyl) substituted alkanamides as inhibitors of the beta secretase enzyme for treating Alzheimer's disease
-
2003006421
-
Gailunas A, Hom R, John V, Maillard M, Chrusciel RA, Fisher J, et al. Preparation of N-(3-amino-2-hydroxy-propyl) substituted alkanamides as inhibitors of the beta secretase enzyme for treating Alzheimer's disease. PCT Int Appl 2003006421
-
PCT Int. Appl.
-
-
Gailunas, A.1
Hom, R.2
John, V.3
Maillard, M.4
Chrusciel, R.A.5
Fisher, J.6
-
81
-
-
24944565448
-
Preparation of N, N′-substituted-1, 3-diamino-2-hydroxy-propanes for treating Alzheimer's disease
-
2003040096
-
John V, Maillard M, Jagodzinska B, Beck JP, Gailunas A, Fang L, et al. Preparation of N, N′-substituted-1, 3-diamino-2-hydroxy-propanes for treating Alzheimer's disease. PCT Int Appl 2003040096.
-
PCT Int. Appl.
-
-
John, V.1
Maillard, M.2
Jagodzinska, B.3
Beck, J.P.4
Gailunas, A.5
Fang, L.6
-
84
-
-
0026726041
-
Peptoids: A modular approach to drug discovery
-
Simon RJ, Kania RS, Zuckermann RN, Huebner VD, Jewell DA, Banville S, et al. Peptoids: a modular approach to drug discovery. Proc Natl Acad Sci USA 1992; 89: 9367-71.
-
(1992)
Proc. Natl. Acad. Sci. USA
, vol.89
, pp. 9367-9371
-
-
Simon, R.J.1
Kania, R.S.2
Zuckermann, R.N.3
Huebner, V.D.4
Jewell, D.A.5
Banville, S.6
-
85
-
-
24944495035
-
Preparation of hydroxyaminopropyl-benzamides for the treatment of Alzheimer's disease
-
2004029019
-
Hom R, Varghese J. Preparation of hydroxyaminopropyl-benzamides for the treatment of Alzheimer's disease. PCT Int Appl 2004029019.
-
PCT Int. Appl.
-
-
Hom, R.1
Varghese, J.2
-
86
-
-
24944530121
-
Preparation of (hydroxyethyl)ureas as inhibitors of Alzheimer's β-amyloid production
-
2002014264
-
Wolfe MS, Selkoe DJ. Preparation of (hydroxyethyl)ureas as inhibitors of Alzheimer's β-amyloid production. PCT Int Appl 2002014264.
-
PCT Int. Appl.
-
-
Wolfe, M.S.1
Selkoe, D.J.2
-
87
-
-
0023237365
-
Renin inhibitors. Design of angiotensinogen transition-state analogs containing novel (2R, 3R, 4R, 5S)-5-amino-3, 4-dihydroxy-2-isopropyl-7-methyloctanoic acid
-
Thaisrivongs S, Pals DT, Kroll LT, Turner SR, Han FS. Renin inhibitors. Design of angiotensinogen transition-state analogs containing novel (2R, 3R, 4R, 5S)-5-amino-3, 4-dihydroxy-2-isopropyl-7-methyloctanoic acid. J Med Chem 1987; 30: 976-82.
-
(1987)
J. Med. Chem.
, vol.30
, pp. 976-982
-
-
Thaisrivongs, S.1
Pals, D.T.2
Kroll, L.T.3
Turner, S.R.4
Han, F.S.5
-
88
-
-
0025169561
-
An inhibitor of the protease blocks maturation of human and simian immunodeficiency viruses and spread of infection
-
Ashorn P, McQuade TJ, Thaisrivongs S, Tomasselli AG, Tarpley WG, Moss B. An inhibitor of the protease blocks maturation of human and simian immunodeficiency viruses and spread of infection. Proc Natl Acad Sci USA 1990; 87: 7472-6.
-
(1990)
Proc. Natl. Acad. Sci. USA
, vol.87
, pp. 7472-7476
-
-
Ashorn, P.1
McQuade, T.J.2
Thaisrivongs, S.3
Tomasselli, A.G.4
Tarpley, W.G.5
Moss, B.6
-
89
-
-
0025994827
-
Inhibitors of the protease from human immunodeficiency virus: Design and modeling of a compound containing a dihydroxyethylene isostere insert with high binding affinity and effective antiviral activity
-
Thaisrivongs S, Tomasselli AG, Moon JB, Hui J, McQuade TJ, Turner SR, et al. Inhibitors of the protease from human immunodeficiency virus: design and modeling of a compound containing a dihydroxyethylene isostere insert with high binding affinity and effective antiviral activity. J Med Chem 1991; 34: 2344-56.
-
(1991)
J. Med. Chem.
, vol.34
, pp. 2344-2356
-
-
Thaisrivongs, S.1
Tomasselli, A.G.2
Moon, J.B.3
Hui, J.4
McQuade, T.J.5
Turner, S.R.6
-
90
-
-
24944533154
-
Preparation of amine diols as β-secretase inhibitors for the treatment of Alzheimer's disease
-
2003006453
-
Schostarez HJ, Chrusciel RA. Preparation of amine diols as β-secretase inhibitors for the treatment of Alzheimer's disease. PCT Int Appl 2003006453.
-
PCT Int. Appl.
-
-
Schostarez, H.J.1
Chrusciel, R.A.2
-
91
-
-
24944581826
-
Preparation of amine 1, 2- and 1, 3-diol alditols and their use for treatment of Alzheimer's disease
-
2003043975
-
Romero AG, Schostarez H, Roels CM. Preparation of amine 1, 2- and 1, 3-diol alditols and their use for treatment of Alzheimer's disease. PCT Int Appl 2003043975.
-
PCT Int. Appl.
-
-
Romero, A.G.1
Schostarez, H.2
Roels, C.M.3
-
92
-
-
24944460428
-
Preparation of aminediols as β-secretase inhibitors for the treatment of Alzheimer's and other diseases characterized by deposition of Ab peptide
-
2002100818
-
Schostarez HJ, Chrusciel RA. Preparation of aminediols as β-secretase inhibitors for the treatment of Alzheimer's and other diseases characterized by deposition of Ab peptide. PCT Int Appl 2002100818.
-
PCT Int. Appl.
-
-
Schostarez, H.J.1
Chrusciel, R.A.2
-
93
-
-
24944535460
-
Preparation of hydroxy substituted indanylamides for the treatment of Alzheimer's disease
-
2003037325
-
Beck JP. Preparation of hydroxy substituted indanylamides for the treatment of Alzheimer's disease. PCT Int Appl 2003037325.
-
PCT Int. Appl.
-
-
Beck, J.P.1
-
94
-
-
24944451610
-
Preparation of quinaldoyl amine derivatives of oxo- and hydroxy-substituted hydrocarbons for treating Alzheimer's disease
-
2003020370
-
Schostarez HJ. Preparation of quinaldoyl amine derivatives of oxo- and hydroxy-substituted hydrocarbons for treating Alzheimer's disease. PCT Int Appl 2003020370.
-
PCT Int. Appl.
-
-
Schostarez, H.J.1
-
95
-
-
24944496981
-
Substituted peptides useful in the treatment of Alzheimer's disease, and. Preparation thereof
-
2004037179
-
Beck JT. Substituted peptides useful in the treatment of Alzheimer's disease, and. Preparation thereof. PCT Int Appl 2004037179.
-
PCT Int. Appl.
-
-
Beck, J.T.1
-
96
-
-
24944444446
-
Methods for treating Alzheimer's disease using hydroxyethylene compounds containing a heterocyclic amide bond isostere
-
2004002478
-
John V. Methods for treating Alzheimer's disease using hydroxyethylene compounds containing a heterocyclic amide bond isostere. PCT Int Appl 2004002478.
-
PCT Int. Appl.
-
-
John, V.1
-
97
-
-
24944496980
-
Hydroxypropyl amides for the treatment of Alzheimer's disease
-
Tucker JA, Sherer BA, Xu YZ, Brogley L, Pulley SR, Jacobs JS, et al. Hydroxypropyl amides for the treatment of Alzheimer's disease. U.S. Pat Appl Publ 20040039034.
-
U.S. Pat. Appl. Publ. 20040039034
-
-
Tucker, J.A.1
Sherer, B.A.2
Xu, Y.Z.3
Brogley, L.4
Pulley, S.R.5
Jacobs, J.S.6
-
98
-
-
24944484364
-
Preparation of arylhydroxypropylamines used for treatment of Alzheimer's disease and to reduce amyloid beta peptide formation
-
2003029169
-
Fisher JF, Jacobs JS, Scherer BA. Preparation of arylhydroxypropylamines used for treatment of Alzheimer's disease and to reduce amyloid beta peptide formation. PCT Int Appl 2003029169.
-
PCT Int. Appl.
-
-
Fisher, J.F.1
Jacobs, J.S.2
Scherer, B.A.3
-
99
-
-
24944541649
-
Preparation of diamine diols as β-secretase inhibitors for the treatment of Alzheimer's disease
-
2003006013
-
Schostarez HJ, Chrusciel RA. Preparation of diamine diols as β-secretase inhibitors for the treatment of Alzheimer's disease. PCT Int Appl 2003006013.
-
PCT Int. Appl.
-
-
Schostarez, H.J.1
Chrusciel, R.A.2
-
100
-
-
24944548445
-
Preparation of substituted amino carboxamides for the treatment of Alzheimer's disease
-
2003057721
-
Jagodzinska B, Warpehoski MA. Preparation of substituted amino carboxamides for the treatment of Alzheimer's disease. PCT Int Appl 2003057721.
-
PCT Int. Appl.
-
-
Jagodzinska, B.1
Warpehoski, M.A.2
-
101
-
-
24944504566
-
Preparation of peptide isosteres containing a heterocycle useful in the treatment of Alzheimer's disease
-
2003047576
-
John V. Preparation of peptide isosteres containing a heterocycle useful in the treatment of Alzheimer's disease. PCT Int Appl 2003047576.
-
PCT Int. Appl.
-
-
John, V.1
-
102
-
-
24944463475
-
Preparation of β-hydroxyamine derivatives for the treatment of Alzheimer's disease
-
2003002122
-
John V, Hom R, Tucker J. Preparation of β-hydroxyamine derivatives for the treatment of Alzheimer's disease. PCT Int Appl 2003002122.
-
PCT Int. Appl.
-
-
John, V.1
Hom, R.2
Tucker, J.3
-
103
-
-
24944450811
-
Preparation of phenethylamines for the treatment of Alzheimer's disease
-
2003027068
-
Gailunas A, Tucker JA, John V. Preparation of phenethylamines for the treatment of Alzheimer's disease. PCT Int Appl 2003027068.
-
PCT Int. Appl.
-
-
Gailunas, A.1
Tucker, J.A.2
John, V.3
-
104
-
-
24944445790
-
Preparation of ring-containing aminoether carboxamides as β-secretase inhibitors for treating Alzheimer's disease and other diseases characterized by deposition of Ab-peptide
-
2004024675
-
Beck JP, Drowns M, Warpehoski MA. Preparation of ring-containing aminoether carboxamides as β-secretase inhibitors for treating Alzheimer's disease and other diseases characterized by deposition of Ab-peptide. PCT Int Appl 2004024675.
-
PCT Int. Appl.
-
-
Beck, J.P.1
Drowns, M.2
Warpehoski, M.A.3
-
105
-
-
24944457910
-
Preparation of ring-containing N-acetyl 2-hydroxy-1, 3-diaminoalkanes as β-secretase inhibitors for treating Alzheimer's disease and other diseases characterized by deposition of Ab-peptide
-
2004024081
-
Maillard M, Baldwin ET, Beck JT, Hughes R, John V, Pulley SR, et al. Preparation of ring-containing N-acetyl 2-hydroxy-1, 3-diaminoalkanes as β-secretase inhibitors for treating Alzheimer's disease and other diseases characterized by deposition of Ab-peptide. PCT Int Appl 2004024081.
-
PCT Int. Appl.
-
-
Maillard, M.1
Baldwin, E.T.2
Beck, J.T.3
Hughes, R.4
John, V.5
Pulley, S.R.6
-
106
-
-
0026439296
-
Synthesis and biological activity of new conformationally restricted analogs of pepstatin
-
Szewczuk Z, Rebholz KL, Rich DH. Synthesis and biological activity of new conformationally restricted analogs of pepstatin. Int J Pept Protein Res 1992; 40: 233-42.
-
(1992)
Int. J. Pept. Protein Res.
, vol.40
, pp. 233-242
-
-
Szewczuk, Z.1
Rebholz, K.L.2
Rich, D.H.3
-
108
-
-
0028020289
-
Design, Synthesis, and Conformational Analysis of a Novel Macrocyclic HIV-Protease Inhibitor
-
Podlogar BL, Farr RA, Friedrich D, Tarnus C, Huber EW, Cregge RJ, et al. Design, Synthesis, and Conformational Analysis of a Novel Macrocyclic HIV-Protease Inhibitor. J Med Chem 1994; 37: 3684-92.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 3684-3692
-
-
Podlogar, B.L.1
Farr, R.A.2
Friedrich, D.3
Tarnus, C.4
Huber, E.W.5
Cregge, R.J.6
-
109
-
-
0028096657
-
Design, synthesis, and activity of conformationally-constrained macrocyclic peptide-based inhibitors of HIV protease
-
Smith RA, Coles PJ, Chen JJ, Robinson VJ, MacDonald ID, Carriere J, et al. Design, synthesis, and activity of conformationally-constrained macrocyclic peptide-based inhibitors of HIV protease. Bioorg Med Chem Lett 1994; 4: 2217-22.
-
(1994)
Bioorg. Med. Chem. Lett.
, vol.4
, pp. 2217-2222
-
-
Smith, R.A.1
Coles, P.J.2
Chen, J.J.3
Robinson, V.J.4
MacDonald, I.D.5
Carriere, J.6
-
110
-
-
0029872870
-
Synthesis and activity of conformationally-constrained macrocyclic norstatine-based inhibitors of HIV protease
-
Chen JJ, Coles PJ, Arnold LD, Smith RA, MacDonald ID, Carriere J, et al. Synthesis and activity of conformationally-constrained macrocyclic norstatine-based inhibitors of HIV protease. Bioorg Med Chem Lett 1996; 6: 435-8.
-
(1996)
Bioorg. Med. Chem. Lett.
, vol.6
, pp. 435-438
-
-
Chen, J.J.1
Coles, P.J.2
Arnold, L.D.3
Smith, R.A.4
MacDonald, I.D.5
Carriere, J.6
-
111
-
-
16044374201
-
Structure-activity relationships for macrocyclic peptidomimetic inhibitors of HIV-1 protease
-
Abbenante G, Bergman DA, Brinkworth RI, March DR, Reid RC, Hunt PA, et al. Structure-activity relationships for macrocyclic peptidomimetic inhibitors of HIV-1 protease. Bioorg Med Chem Lett 1996, 6: 2531-6.
-
(1996)
Bioorg. Med. Chem. Lett.
, vol.6
, pp. 2531-2536
-
-
Abbenante, G.1
Bergman, D.A.2
Brinkworth, R.I.3
March, D.R.4
Reid, R.C.5
Hunt, P.A.6
-
114
-
-
0023880207
-
New inhibitors of human renin that contain novel Leu-Val replacements. Examination of the P1 site
-
Luly JR, Bolis G, BaMaung N, Soderquist J, Dellaria JF, Stein H, et al. New inhibitors of human renin that contain novel Leu-Val replacements. Examination of the P1 site. J Med Chem 1988; 31: 532-9.
-
(1988)
J. Med. Chem.
, vol.31
, pp. 532-539
-
-
Luly, J.R.1
Bolis, G.2
BaMaung, N.3
Soderquist, J.4
Dellaria, J.F.5
Stein, H.6
-
115
-
-
0027453879
-
Peptidomimetic inhibitors of renin incorporating topographically modified isosteres spanning the P1(->P3)-P1 sites
-
Plummer M, Hamby JM, Hingorani G, Batley BL, Rapundalo ST. Peptidomimetic inhibitors of renin incorporating topographically modified isosteres spanning the P1(->P3)-P1 sites. Bioorg Med Chem Lett 1993; 3: 2119-24.
-
(1993)
Bioorg. Med. Chem. Lett.
, vol.3
, pp. 2119-2124
-
-
Plummer, M.1
Hamby, J.M.2
Hingorani, G.3
Batley, B.L.4
Rapundalo, S.T.5
-
116
-
-
0033941893
-
Structure-based drug design: The discovery of novel nonpeptide orally active inhibitors of human renin
-
Rahuel J, Rasetti V, Maibaum J, Rueger H, Goschke R, Cohen NC, et al. Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin. Chem Biol 2000; 7: 493-504.
-
(2000)
Chem. Biol.
, vol.7
, pp. 493-504
-
-
Rahuel, J.1
Rasetti, V.2
Maibaum, J.3
Rueger, H.4
Goschke, R.5
Cohen, N.C.6
-
117
-
-
0347479295
-
Blood pressure lowering in essential hypertension with an oral renin inhibitor, aliskiren
-
Stanton A, Jensen C, Nussberger J, O'Brien E. Blood pressure lowering in essential hypertension with an oral renin inhibitor, aliskiren. Hypertension 2003; 42: 1137-43.
-
(2003)
Hypertension
, vol.42
, pp. 1137-1143
-
-
Stanton, A.1
Jensen, C.2
Nussberger, J.3
O'Brien, E.4
-
118
-
-
0036372173
-
Angiotensin II suppression in humans by the orally active renin inhibitor aliskiren (SPP100). Comparison with enalapril
-
Nussberger J, Wuerzner G, Jensen C, Brunner HR. Angiotensin II suppression in humans by the orally active renin inhibitor aliskiren (SPP100). Comparison with enalapril. Hypertension 2002; 39: e1-e8.
-
(2002)
Hypertension
, vol.39
-
-
Nussberger, J.1
Wuerzner, G.2
Jensen, C.3
Brunner, H.R.4
-
119
-
-
0042661157
-
Structure-based design of aliskiren, a novel orally effective renin inhibitor
-
Wood JM, Maibaum J, Rahuel J, Gruetter MG, Cohen N-C, Rasetti V, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor. Biochem Biophys Res Commun 2003; 308: 698-705.
-
(2003)
Biochem. Biophys. Res. Commun.
, vol.308
, pp. 698-705
-
-
Wood, J.M.1
Maibaum, J.2
Rahuel, J.3
Gruetter, M.G.4
Cohen, N.-C.5
Rasetti, V.6
-
120
-
-
24944478899
-
Methods of treating Alzheimer's disease using and method of preparing d-amino-γ-hydroxy-ω-arylalkanoic acid amides
-
2003103653
-
John V, Maillard M. Methods of treating Alzheimer's disease using and method of preparing d-amino-γ-hydroxy-ω-arylalkanoic acid amides. PCT Int Appl 2003103653.
-
PCT Int. Appl.
-
-
John, V.1
Maillard, M.2
-
121
-
-
24944479741
-
Methods of treating Alzheimers disease using aromatically substituted ω-amino-alkanoic acid amides and alkanoic acid diamides
-
2003103652
-
Maillard M, Varghese J. Methods of treating Alzheimers disease using aromatically substituted ω-amino-alkanoic acid amides and alkanoic acid diamides. PCT Int Appl 2003103652.
-
PCT Int. Appl.
-
-
Maillard, M.1
Varghese, J.2
-
122
-
-
24944459614
-
Preparation of substituted hydroxyethylamines as β-secretase inhibitors
-
2003050073
-
Tenbrink R, Maillard M, Warpehoski M. Preparation of substituted hydroxyethylamines as β-secretase inhibitors. PCT Int Appl 2003050073.
-
PCT Int. Appl.
-
-
Tenbrink, R.1
Maillard, M.2
Warpehoski, M.3
-
123
-
-
0033102135
-
Renin inhibition by substituted piperidines: A novel paradigm for the inhibition of monomeric aspartic proteinases?
-
Oefner C, Binggeli A, Breu V, Bur D, Clozel JP, D'Arcy A, et al. Renin inhibition by substituted piperidines: a novel paradigm for the inhibition of monomeric aspartic proteinases? Chemistry & Biology 1999; 6: 127-31.
-
(1999)
Chemistry & Biology
, vol.6
, pp. 127-131
-
-
Oefner, C.1
Binggeli, A.2
Breu, V.3
Bur, D.4
Clozel, J.P.5
D'Arcy, A.6
-
124
-
-
0035273245
-
Piperidine renin inhibitors: From leads to drug candidates
-
Marki HP, Binggeli A, Bittner B, Bohner-Lang V, Breu V, Bur D, et al. Piperidine renin inhibitors: from leads to drug candidates. Farmaco 2001; 56: 21-7.
-
(2001)
Farmaco
, vol.56
, pp. 21-27
-
-
Marki, H.P.1
Binggeli, A.2
Bittner, B.3
Bohner-Lang, V.4
Breu, V.5
Bur, D.6
-
125
-
-
0033577692
-
Substituted piperidines - Highly potent renin inhibitors due to induced fit adaptation of the active site
-
Vieira E, Binggeli A, Breu V, Bur D, Fischli W, Guller R, et al. Substituted piperidines - highly potent renin inhibitors due to induced fit adaptation of the active site. Bioorg Med Chem Lett 1999; 9: 1397-402.
-
(1999)
Bioorg. Med. Chem. Lett.
, vol.9
, pp. 1397-1402
-
-
Vieira, E.1
Binggeli, A.2
Breu, V.3
Bur, D.4
Fischli, W.5
Guller, R.6
-
126
-
-
0003694381
-
Piperidine-renin inhibitors compounds with improved physicochemical properties
-
Guller R, Binggeli A, Breu V, Bur D, Fischli W, Hirth G, et al. Piperidine-renin inhibitors compounds with improved physicochemical properties. Bioorg Med Chem Lett 1999; 9: 1403-8.
-
(1999)
Bioorg. Med. Chem. Lett.
, vol.9
, pp. 1403-1408
-
-
Guller, R.1
Binggeli, A.2
Breu, V.3
Bur, D.4
Fischli, W.5
Hirth, G.6
-
127
-
-
0035954893
-
From Peptides to Non-Peptide Peptidomimetics: Design and Synthesis of New Piperidine Inhibitors of Aspartic Peptidases
-
Bursavich MG, West CW, Rich DH. From Peptides to Non-Peptide Peptidomimetics: Design and Synthesis of New Piperidine Inhibitors of Aspartic Peptidases. Org Lett 2001; 3: 2317-20.
-
(2001)
Org. Lett.
, vol.3
, pp. 2317-2320
-
-
Bursavich, M.G.1
West, C.W.2
Rich, D.H.3
-
128
-
-
24944558693
-
Preparation of β-carbolines and other inhibitors of BACE-1 aspartic proteinase useful against Alzheimer's and other BACE-mediated diseases
-
2002088101
-
Bhisetti GR, Saunders JO, Murcko MA, Lepre CA, Britt SD, Come JH, et al. Preparation of β-carbolines and other inhibitors of BACE-1 aspartic proteinase useful against Alzheimer's and other BACE-mediated diseases. PCT Int Appl 2002088101.
-
PCT Int. Appl.
-
-
Bhisetti, G.R.1
Saunders, J.O.2
Murcko, M.A.3
Lepre, C.A.4
Britt, S.D.5
Come, J.H.6
-
129
-
-
24944458746
-
Methods of treating or preventing Alzheimer's disease using 4-aryl-3-aralkoxypiperidines and -azabicyclooctanes
-
2002076440
-
Nieman JA, Fang L, Jagodzinska B. Methods of treating or preventing Alzheimer's disease using 4-aryl-3-aralkoxypiperidines and -azabicyclooctanes. PCT Int Appl 2002076440.
-
PCT Int. Appl.
-
-
Nieman, J.A.1
Fang, L.2
Jagodzinska, B.3
-
130
-
-
24944581471
-
Preparation of substituted piperidines and piperazines useful as β-secretase inhibitors against Alzheimer's disease
-
2003043987
-
John V, Moon JB, Pulley SR, Rich DH, Brown DL, Jagodzinska B, et al. Preparation of substituted piperidines and piperazines useful as β-secretase inhibitors against Alzheimer's disease. PCT Int Appl 2003043987.
-
PCT Int. Appl.
-
-
John, V.1
Moon, J.B.2
Pulley, S.R.3
Rich, D.H.4
Brown, D.L.5
Jagodzinska, B.6
-
131
-
-
24944532808
-
Preparation of substituted 3- and 4-(aminomethyl)piperidines for use as β-secretase inhibitors in the treatment of Alzheimer's disease
-
2004002483
-
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. PCT Int Appl 2004002483.
-
PCT Int. Appl.
-
-
Boss, C.1
Bur, D.2
Fischli, W.3
Jenck, F.4
Weller, T.5
-
132
-
-
24944504218
-
Preparation of piperidines for the treatment of central nervous system disorders
-
2004009549
-
Boss C, Bur D, Fischli W, Jenck F, Weller T. Preparation of piperidines for the treatment of central nervous system disorders. PCT Int Appl 2004009549.
-
PCT Int. Appl.
-
-
Boss, C.1
Bur, D.2
Fischli, W.3
Jenck, F.4
Weller, T.5
-
133
-
-
24944537745
-
Preparation of piperazines as β-amyloid converting enzyme (BACE) inhibitors for the treatment of Alzheimer's disease
-
2004020422
-
Willems H. Preparation of piperazines as β-amyloid converting enzyme (BACE) inhibitors for the treatment of Alzheimer's disease. PCT Int Appl 2004020422.
-
PCT Int. Appl.
-
-
Willems, H.1
-
134
-
-
1542374176
-
A beta-Secretase (BACE1) Inhibitor Hispidin from the Mycelial Cultures of Phellinus linteus
-
Park I-H, Jeon S-Y, Lee H-J, Kim S-I, Song K-S. A beta-Secretase (BACE1) Inhibitor Hispidin from the Mycelial Cultures of Phellinus linteus. Planta Med 2004; 70: 143-6.
-
(2004)
Planta Med.
, vol.70
, pp. 143-146
-
-
Park, I.-H.1
Jeon, S.-Y.2
Lee, H.-J.3
Kim, S.-I.4
Song, K.-S.5
-
136
-
-
24944565766
-
Preparation and use of aza-bicyclononanes for the treatment of Alzheimer's disease
-
2003000261
-
Beck JP. Preparation and use of aza-bicyclononanes for the treatment of Alzheimer's disease. PCT Int Appl 2003000261.
-
PCT Int. Appl.
-
-
Beck, J.P.1
-
137
-
-
24944542608
-
β-secretase inhibitors for use in treatment of diseases caused by deposits of β-amyloid peptides
-
2003059346
-
Dietrich A, Nimz O, Rester U, Fecke W, Haemmerle M, Baier F. β-secretase inhibitors for use in treatment of diseases caused by deposits of β-amyloid peptides. PCT Int Appl 2003059346.
-
PCT Int. Appl.
-
-
Dietrich, A.1
Nimz, O.2
Rester, U.3
Fecke, W.4
Haemmerle, M.5
Baier, F.6
-
138
-
-
24944568030
-
Preparation of N-sulfonyl amino acid derivatives for the treatment of Alzheimer's disease
-
2004020402
-
Willems H, Harris WH. Preparation of N-sulfonyl amino acid derivatives for the treatment of Alzheimer's disease. PCT Int Appl 2004020402.
-
PCT Int. Appl.
-
-
Willems, H.1
Harris, W.H.2
-
139
-
-
24944556369
-
Protected amino acid derivatives for the treatment of Alzheimer's disease
-
2392443
-
Willems H, Gordon R. Protected amino acid derivatives for the treatment of Alzheimer's disease. Brit UK Pat Appl 2392443.
-
Brit. UK Pat. Appl.
-
-
Willems, H.1
Gordon, R.2
-
140
-
-
24944447649
-
Preparation of hydroxysuccinamide compounds for the treatment of Alzheimer's disease
-
2391547
-
Willems H, Porter B. Preparation of hydroxysuccinamide compounds for the treatment of Alzheimer's disease. Brit UK Pat Appl 2391547.
-
Brit. UK Pat. Appl.
-
-
Willems, H.1
Porter, B.2
-
141
-
-
24944550695
-
Preparation of hydroxyalkanoyl aminopyrazoles and related compounds for inhibiting β-amyloid peptide release
-
2003064396
-
Tung JS, Guinn AC, Thorsett G, Pleiss MA. Preparation of hydroxyalkanoyl aminopyrazoles and related compounds for inhibiting β-amyloid peptide release. PCT Int Appl 2003064396.
-
PCT Int. Appl.
-
-
Tung, J.S.1
Guinn, A.C.2
Thorsett, G.3
Pleiss, M.A.4
-
142
-
-
1542351969
-
Preparation of 2-[2-amino- or 2-(N-heterocyclyl)ethyl]-6-(4-biphenylylmethoxy) tetralin derivatives as β-secretase inhibitors
-
2001087293
-
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. PCT Int Appl 2001087293.
-
PCT Int. Appl.
-
-
Miyamoto, M.1
Matsui, J.2
Fukumoto, H.3
Tarui, N.4
-
143
-
-
24944535944
-
Preparation of phosphinylmethyl and phosphorylmethyl succinic and glutaric acid analogs as β-secretase inhibitors useful in the treatment of Alzheimer's disease
-
2002096897
-
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. PCT Int Appl 2002096897.
-
PCT Int. Appl.
-
-
Qiao, L.1
Etcheberrigaray, R.2
-
144
-
-
0037239852
-
Emerging beta-amyloid therapies for the treatment of Alzheimer's disease
-
Conway KA, Baxter EW, Felsenstein KM, Reitz AB. Emerging beta-amyloid therapies for the treatment of Alzheimer's disease. Curr Pharm Design 2003; 9(6): 427-47.
-
(2003)
Curr. Pharm. Design.
, vol.9
, Issue.6
, pp. 427-447
-
-
Conway, K.A.1
Baxter, E.W.2
Felsenstein, K.M.3
Reitz, A.B.4
-
145
-
-
0037242768
-
Peptidases, proteases and amyloid beta-peptide catabolism
-
Hersh LB. Peptidases, proteases and amyloid beta-peptide catabolism. Curr Pharm Design 2003; 9(6): 449-54.
-
(2003)
Curr. Pharm. Design.
, vol.9
, Issue.6
, pp. 449-454
-
-
Hersh, L.B.1
-
146
-
-
2342446265
-
Imaging beta-amyloid plaques and neurofibrillary tangles in the aging human brain
-
Mathis CA, Wang Y, Klunk WE. Imaging beta-amyloid plaques and neurofibrillary tangles in the aging human brain. Curr Pharm Design 2004; 10(13): 1469-92.
-
(2004)
Curr. Pharm. Design.
, vol.10
, Issue.13
, pp. 1469-1492
-
-
Mathis, C.A.1
Wang, Y.2
Klunk, W.E.3
|