-
2
-
-
0034054051
-
-
Dymock B.W., Jones P.S., Wilson F.X., Antiviral Chem. Chemother., 2000, 11, 79.
-
(2000)
Antiviral Chem. Chemother.
, vol.11
, pp. 79
-
-
Dymock, B.W.1
Jones, P.S.2
Wilson, F.X.3
-
3
-
-
0030778811
-
-
(a) For recent reviews, see: Dymock B.W. Emerging Drugs. 6:2001;13 (b) Dymock B.W., Jones P.S., Wilson F.X. Antiviral Chem. Chemother. 11:2000;79 (c) Clarke B. J. Gen. Virol. 78:1997;2397.
-
(1997)
J. Gen. Virol.
, vol.78
, pp. 2397
-
-
Clarke, B.1
-
4
-
-
0032547938
-
-
McHutchison J.G., Gordon S.C., Schiff E.R., Shiffman M.L., Lee W.M., Rustgi V.K., Goodman Z.D., Ling M.-H., Cort S., Albrecht J.K. New Engl. J. Med. 339:1998;1485.
-
(1998)
New Engl. J. Med.
, vol.339
, pp. 1485
-
-
McHutchison, J.G.1
Gordon, S.C.2
Schiff, E.R.3
Shiffman, M.L.4
Lee, W.M.5
Rustgi, V.K.6
Goodman, Z.D.7
Ling, M.-H.8
Cort, S.9
Albrecht, J.K.10
-
5
-
-
0034619946
-
-
Zeuzem S., Feinman V., Rasenack J., Heathcote E.J., Lai M.-Y., Gane E., O'Grady J., Reichen J., Diago M., Lin A., Hoffman J., Brunda M.J. New Engl. J. Med. 343:2000;1666.
-
(2000)
New Engl. J. Med.
, vol.343
, pp. 1666
-
-
Zeuzem, S.1
Feinman, V.2
Rasenack, J.3
Heathcote, E.J.4
Lai, M.-Y.5
Gane, E.6
O'Grady, J.7
Reichen, J.8
Diago, M.9
Lin, A.10
Hoffman, J.11
Brunda, M.J.12
-
6
-
-
0034619980
-
-
Heathcote E.J., Shiffman M.L., Cooksley W.G.E., Dusheiko G.M., Lee S.S., Balart L., Reindollar R., Reddy R.K., Wright T.L., Lin A., Hoffman J., De Pamphilis J. New Engl. J. Med. 343:2000;1673.
-
(2000)
New Engl. J. Med.
, vol.343
, pp. 1673
-
-
Heathcote, E.J.1
Shiffman, M.L.2
Cooksley, W.G.E.3
Dusheiko, G.M.4
Lee, S.S.5
Balart, L.6
Reindollar, R.7
Reddy, R.K.8
Wright, T.L.9
Lin, A.10
Hoffman, J.11
De Pamphilis, J.12
-
8
-
-
0032400892
-
-
Kwong A.D., Kim J.L., Rao G., Lipovsek D., Raybuck S.A. Antiviral Res. 40:1998;1.
-
(1998)
Antiviral Res.
, vol.40
, pp. 1
-
-
Kwong, A.D.1
Kim, J.L.2
Rao, G.3
Lipovsek, D.4
Raybuck, S.A.5
-
9
-
-
85030918436
-
-
PCT Patent (Vertex) WO/98/17679, 10/18/1996 PCT Patent (Vertex): WO/99/50230, 3/31/1998
-
(a) Peptidyl aldehydes: Tung, R.; Harbeson, S. L.; Deininger, D. D.; Murcko, M. A.; Bhisetti, G. R.; Farmer, L. J. PCT Patent (Vertex) WO/98/17679, 10/18/1996.
-
-
-
Tung, R.1
Harbeson, S.L.2
Deininger, D.D.3
Murcko, M.A.4
Bhisetti, G.R.5
Farmer, L.J.6
-
10
-
-
0347809950
-
-
(b) PCT Patent (Vertex): WO/99/50230, 3/31/1998. (c) Perni R.B., Britt S.D., Court J.C., Courtney L.F., Deininger D.D., Farmer L.J., Gates C.A., Harbeson S.L., Kim J.L., Landro J.A., Levin R.B., Luong Y.-P., O'Malley E.T., Pitlik J., Rao G., Schairer W.C., Thomson J.A., Tung R.D., Van Drie J.H., Wei Y. Bioorg. Med. Chem. 13:2003;4059.
-
(2003)
Bioorg. Med. Chem.
, vol.13
, pp. 4059
-
-
Perni, R.B.1
Britt, S.D.2
Court, J.C.3
Courtney, L.F.4
Deininger, D.D.5
Farmer, L.J.6
Gates, C.A.7
Harbeson, S.L.8
Kim, J.L.9
Landro, J.A.10
Levin, R.B.11
Luong, Y.-P.12
O'Malley, E.T.13
Pitlik, J.14
Rao, G.15
Schairer, W.C.16
Thomson, J.A.17
Tung, R.D.18
Van Drie, J.H.19
Wei, Y.20
more..
-
11
-
-
0032821515
-
-
Attwood M.R., Bennett J.M., Campbell A.D., Canning G.G.M., Carr M.G., Conway E., Dunsdon R.M., Greening J.R., Jones P.S., Kay P.B., Handa B.K., Hurst D.N., Jennings N.S., Jordan S., Keech E., O'Brien M.A., Overton H.A., King-Underwood J., Raynham T.M., Stenson K.P., Wilkinson C.S., Wilkinson T.C.I., Wilson F.X., Antiviral Chem. Chemother., 1999, 10, 259.
-
(1999)
Antiviral Chem. Chemother.
, vol.10
, pp. 259
-
-
Attwood, M.R.1
Bennett, J.M.2
Campbell, A.D.3
Canning, G.G.M.4
Carr, M.G.5
Conway, E.6
Dunsdon, R.M.7
Greening, J.R.8
Jones, P.S.9
Kay, P.B.10
Handa, B.K.11
Hurst, D.N.12
Jennings, N.S.13
Jordan, S.14
Keech, E.15
O'Brien, M.A.16
Overton, H.A.17
King-Underwood, J.18
Raynham, T.M.19
Stenson, K.P.20
Wilkinson, C.S.21
Wilkinson, T.C.I.22
Wilson, F.X.23
more..
-
12
-
-
0034609661
-
-
Boronic acids: and references cited therein
-
(a) Boronic acids: Attwood M.R., Bennett J.M., Campbell A.D., Canning G.G.M., Carr M.G., Conway E., Dunsdon R.M., Greening J.R., Jones P.S., Kay P.B., Handa B.K., Hurst D.N., Jennings N.S., Jordan S., Keech E., O'Brien M.A., Overton H.A., King-Underwood J., Raynham T.M., Stenson K.P., Wilkinson C.S., Wilkinson T.C.I., Wilson F.X. Antiviral Chem. Chemother. 10:1999;259. and references cited therein (b) Priestley E.S., Decicco C.P. Org. Lett. 2:2000;3095.
-
(2000)
Org. Lett.
, vol.2
, pp. 3095
-
-
Priestley, E.S.1
Decicco, C.P.2
-
13
-
-
85030932161
-
-
Phosphonates: PCT Patent (BI): WO/99/07734, 11/8/1997
-
Phosphonates: PCT Patent (BI): WO/99/07734, 11/8/1997.
-
-
-
-
14
-
-
85030932150
-
-
Peptidyl acids: (1) PCT Patent (BI): WO/99/07733, 11/08/1997
-
Peptidyl acids: (1) PCT Patent (BI): WO/99/07733, 11/08/1997.
-
-
-
-
15
-
-
85030934120
-
-
PCT Patent (BI): WO/00/09543, 10/8/1998
-
(b) PCT Patent (BI): WO/00/09543, 10/8/1998.
-
-
-
-
16
-
-
0035854304
-
-
(c) Poupart M.-A., Cameron D.R., Chabot C., Ghiro E., Goudreau N., Goulet S., Poirier M., Tsantrizos Y.S. J. Org. Chem. 66:2001;4743.
-
(2001)
J. Org. Chem.
, vol.66
, pp. 4743
-
-
Poupart, M.-A.1
Cameron, D.R.2
Chabot, C.3
Ghiro, E.4
Goudreau, N.5
Goulet, S.6
Poirier, M.7
Tsantrizos, Y.S.8
-
17
-
-
85030928224
-
-
α-Ketoacids: PCT Patent: WO/99/64442, 10/6/1998
-
α-Ketoacids: PCT Patent: WO/99/64442, 10/6/1998.
-
-
-
-
18
-
-
0035847669
-
-
α-Ketoamides:
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(a) α-Ketoamides: Bennett J.M., Campbell A.D., Campbell A.J., Carr M.G., Dunsdon R.M., Greening J.R., Hurst D.N., Jennings N.S., Jones P.S., Jordan S., Kay P.B., O'Brien M.A., King-Underwood J., Raynham T.M., Wilkinson C.S., Wilkinson T.C.I., Wilson F.X. Bioorg. Med. Chem. Lett. 11:2001;355
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 355
-
-
Bennett, J.M.1
Campbell, A.D.2
Campbell, A.J.3
Carr, M.G.4
Dunsdon, R.M.5
Greening, J.R.6
Hurst, D.N.7
Jennings, N.S.8
Jones, P.S.9
Jordan, S.10
Kay, P.B.11
O'Brien, M.A.12
King-Underwood, J.13
Raynham, T.M.14
Wilkinson, C.S.15
Wilkinson, T.C.I.16
Wilson, F.X.17
-
20
-
-
85030929557
-
-
PCT Patent (BI): WO/99/07733, 11/8/1997
-
(c) PCT Patent (BI): WO/99/07733, 11/8/1997.
-
-
-
-
21
-
-
85030921847
-
-
US Patent (Vertex): 6,265,380 B1, 7/24/2001
-
(d) Tung, R.; Harbeson, S. L.; Deininger, D. D.; Murcko, M. A.; Bhisetti, G. R.; Farmer, L. J. US Patent (Vertex): 6,265,380 B1, 7/24/2001.
-
-
-
Tung, R.1
Harbeson, S.L.2
Deininger, D.D.3
Murcko, M.A.4
Bhisetti, G.R.5
Farmer, L.J.6
-
22
-
-
85030933317
-
-
PCT Patent (Eli Lilly): WO/02/18369 A2, Mar. 7, 2002
-
PCT Patent (Eli Lilly): WO/02/18369 A2, Mar. 7, 2002.
-
-
-
-
23
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0037197701
-
-
Prime site inhibitors: Ingallinella P., Fattori D., Altamura S., Steinkuler C., Koch U., Cirero D., Bazzo R., Cortese R., Bianchi E., Pessi A. Biochemistry. 41:2002;5483.
-
(2002)
Biochemistry
, vol.41
, pp. 5483
-
-
Ingallinella, P.1
Fattori, D.2
Altamura, S.3
Steinkuler, C.4
Koch, U.5
Cirero, D.6
Bazzo, R.7
Cortese, R.8
Bianchi, E.9
Pessi, A.10
-
24
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0033612107
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HOAT/DCC(DIC) was used to minimize racemization occurred at α-carbon during peptide coupling; cf.:
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HOAT/DCC(DIC) was used to minimize racemization occurred at α-carbon during peptide coupling; cf.: Carpino L.A., El-Faham A. Tetrahedron. 55:1999;6813.
-
(1999)
Tetrahedron
, vol.55
, pp. 6813
-
-
Carpino, L.A.1
El-Faham, A.2
-
25
-
-
0000191714
-
-
For the synthesis of racemic form of compound II, see: Monn J.A., Valli M.J. J. Org. Chem. 59:1994;2773. The enantiomerically pure version of compound II was obtained via chiral HPLC separation.
-
(1994)
J. Org. Chem.
, vol.59
, pp. 2773
-
-
Monn, J.A.1
Valli, M.J.2
-
26
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85030915225
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note
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P1-Nva α-hydroxyacid was prepared from Z-Val(H) via its corresponding cyanohydrin intermediate.
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28
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0014454095
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note
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i values were calculated from rate versus (inhibitor) plots, at fixed concentrations of enzyme and substrate, by a nonlinear least squares fit of the data to the equation of Morrison for tight binding competitive inhibition: Morrison, J. F. Biochim. Biophys. Acta 1969, 185, 269. The Prism program (GraphPad Software) was used for this procedure.
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29
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85030930790
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note
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A panel of 10 human serine and cysteine proteases including elastase, chymotrypsin, trypsin, kallikrein, plasmin, thrombin, Factor Xa, and cathepsins B, G, and L were selected. Assays were performed using the conditions substrates suggested by the manufacturer.
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30
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0345188811
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-
Lohmann V., Korner F., Koch J.-O., Herian U., Theilmann L., Bartenschlager R., Science, 1999, 285, 110.
-
(1999)
Science
, vol.285
, pp. 110
-
-
Lohmann, V.1
Korner, F.2
Koch, J.-O.3
Herian, U.4
Theilmann, L.5
Bartenschlager, R.6
-
31
-
-
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-
-
(a) Replicon assay: Lohmann V., Korner F., Koch J.-O., Herian U., Theilmann L., Bartenschlager R. Science. 285:1999;110 (b) Blight K., Kolykhalov A., Rice C. Science. 290:2000;1972.
-
(2000)
Science
, vol.290
, pp. 1972
-
-
Blight, K.1
Kolykhalov, A.2
Rice, C.3
-
33
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85030926349
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note
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Four-step sequence overall yields for 4a: 51%; 4b: 70%; 5a: 65%; 5b: 71%; 5c: 52%; 6a: 51%; 6b: 59%; 6c: 20%; 6d: 31%; 7b: 44%; 7c: 23%; 7d: 32%; 8a: 42%; 8c: 44%.
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