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Klein S.I., Czekaj M., Gardner C.J., Guertin K., Cheney D.L., Spada A.P., Bolton S.A., Brown K., Colussi D., Heran C.L., Morgan S.R., Leadley R.J., Dunwiddie C.T., Perrone M.H., Chu V. J. Med. Chem. 41:1998;437.
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Brown, K.8
Colussi, D.9
Heran, C.L.10
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0009319033
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218th National Meeting of the American Chemical Society, New Orleans, LA, 22-26 Aug., 1999; American Chemical Society, Washington, DC, MEDI 32
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Czekaj, M.; Klein, S. I.; Gardner, C. J.; Guertin, K. R.; Zulli, A. L.; Pauls, H.; Spada, A. P.; Chu, V.; Brown, K.; Colussi, D.; Leadley, R. J.; Dunwiddie, C. T.; Morgan, S. R.; Heran, C. L.; Perrone, M. H.; Maignan, S.; Guilloteau, J. P.; Liang, G. Abstracts of Papers, 218th National Meeting of the American Chemical Society, New Orleans, LA, 22-26 Aug., 1999; American Chemical Society, Washington, DC, 1999; MEDI 32.
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Abstracts of Papers
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Czekaj, M.1
Klein, S.I.2
Gardner, C.J.3
Guertin, K.R.4
Zulli, A.L.5
Pauls, H.6
Spada, A.P.7
Chu, V.8
Brown, K.9
Colussi, D.10
Leadley, R.J.11
Dunwiddie, C.T.12
Morgan, S.R.13
Heran, C.L.14
Perrone, M.H.15
Maignan, S.16
Guilloteau, J.P.17
Liang, G.18
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12
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15144344269
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Related factor Xa inhibitors, with a similar motif, have also demonstrated an ester function dependence for optimal activity:
-
Related factor Xa inhibitors, with a similar motif, have also demonstrated an ester function dependence for optimal activity: Maduskuie, T. P. Jr.; McNamara, K. J.; Ru, Y.; Knabb, R. M.; Stouten, P. F. W. J. Med. Chem. 1998, 41, 53.
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Maduskuie T.P. Jr1
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Stouten, P.F.W.5
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Fevig J.M., Cacciola J., Alexander R.S., Knabb R.M., Lam G.N., Wong P.C., Wexler R.R. Bioorg. Med. Chem. Lett. 8:1998;3143.
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16
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0032505156
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Philips G.B., Buckman B.O., Davey D.D., Eagen K.A., Guilford W.J., Hinchman J., Ho E., Koovakkat S., Liang A., Light D.R., Mohan R., Ng H.P., Post J.M., Shaw K.J., Smith D., Subramanayam B., Sullivan M.E., Trinh L., Vergona R., Walters J., White K., Whitlow M., Wu S., Xu W., Morrissey M.M. J. Med. Chem. 41:1998;3557.
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Hinchman, J.6
Ho, E.7
Koovakkat, S.8
Liang, A.9
Light, D.R.10
Mohan, R.11
Ng, H.P.12
Post, J.M.13
Shaw, K.J.14
Smith, D.15
Subramanayam, B.16
Sullivan, M.E.17
Trinh, L.18
Vergona, R.19
Walters, J.20
White, K.21
Whitlow, M.22
Wu, S.23
Xu, W.24
Morrissey, M.M.25
more..
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17
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0033539030
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Choi-Sledeski Y.M., McGarry D., Green D., Mason H., Becker M., Davis R., Ewing W.R., Dankulich W.P., Manetta V., Morris R.L., Spada A., Cheney D., Brown K., Colussi D., Chu V., Heran C.L., Morgan S., Bentley R., Leadley R., Maignan S., Guilloteau J.P., Dunwiddie C., Pauls H.W. J. Med. Chem. 42:1999;3572.
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Choi-Sledeski, Y.M.1
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Green, D.3
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Becker, M.5
Davis, R.6
Ewing, W.R.7
Dankulich, W.P.8
Manetta, V.9
Morris, R.L.10
Spada, A.11
Cheney, D.12
Brown, K.13
Colussi, D.14
Chu, V.15
Heran, C.L.16
Morgan, S.17
Bentley, R.18
Leadley, R.19
Maignan, S.20
Guilloteau, J.P.21
Dunwiddie, C.22
Pauls, H.W.23
more..
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18
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0345613886
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215th National Meeting of the American Chemical Society, Dallas, TX, 29 Mar.-2 Apr., 1998; American Chemical Society, Washington, DC, MEDI 203
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Ewing, W.R.; Choi, Y.M.; Becker, M.; Manetta, V.; Green, D.; Davis, R.; Mason, H.; Ly, C.; Cha, D.; McGarry, D.; Dankulich, W.P.; Spada, A.; Cheney, D.; Mason, J.; Brown, K.; Colussi, D.; Chu, V.; Bentley, R.; Morgan, S.; Heran, C.; Leadley, R.; Dunwiddie, C.; Perrone, M.; Pauls, H. Abstracts of Papers, 215th National Meeting of the American Chemical Society, Dallas, TX, 29 Mar.-2 Apr., 1998; American Chemical Society, Washington, DC, 1998; MEDI 203.
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(1998)
Abstracts of Papers
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Ewing, W.R.1
Choi, Y.M.2
Becker, M.3
Manetta, V.4
Green, D.5
Davis, R.6
Mason, H.7
Ly, C.8
Cha, D.9
McGarry, D.10
Dankulich, W.P.11
Spada, A.12
Cheney, D.13
Mason, J.14
Brown, K.15
Colussi, D.16
Chu, V.17
Bentley, R.18
Morgan, S.19
Heran, C.20
Leadley, R.21
Dunwiddie, C.22
Perrone, M.23
Pauls, H.24
more..
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19
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0343291789
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1H NMR and MS: PCT Int. Appl. WO9900356, 1999
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1H NMR and MS: Klein, S. I.; Guertin, K. R.; Spada, A. P.; Pauls, H. W.; Gong, Y.; McGarry, D. G. PCT Int. Appl. WO9900356, 1999; Chem. Abstr. 1999, 130, 110161.
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Klein, S.I.1
Guertin, K.R.2
Spada, A.P.3
Pauls, H.W.4
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McGarry, D.G.6
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20
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0343727248
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Vorbruggen, H.; Krolikiewicz, K. Synth. 1983, 316
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Vorbruggen, H.; Krolikiewicz, K. Synth. 1983, 316.
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21
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0025979697
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Francis J.E., Cash W.D., Barbaz B.S., Bernard P.S., Lovel R.A., Mazzenga G.C., Friedman R.C., Hyun J.L., Braunwalder A.F., Loo P.S., Bennett D.A. J. Med. Chem. 34:1991;281.
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Loo, P.S.10
Bennett, D.A.11
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Dann, O.1
Char, H.2
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25
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0032892181
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In vitro enzyme assays were run in triplicate as per:
-
In vitro enzyme assays were run in triplicate as per: Bostwick, J. S.; Bentley, R.; Morgan, S.; Brown, K.; Chu, V.; Ewing, W. R.; Spada, A.; Pauls, H.; Perrone, M.; Dunwiddie, C. T.; Leadley, R. J. Thromb. Haemost. 1999, 81, 157.
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Bostwick, J.S.1
Bentley, R.2
Morgan, S.3
Brown, K.4
Chu, V.5
Ewing, W.R.6
Spada, A.7
Pauls, H.8
Perrone, M.9
Dunwiddie, C.T.10
Leadley, R.J.11
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26
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0342422175
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In contrast no enhancement of activity was observed when representative β-aminoesters were substituted with para-hydroxybenzamidines
-
In contrast no enhancement of activity was observed when representative β-aminoesters were substituted with para-hydroxybenzamidines:
-
-
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27
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0027304964
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The binding model was constructed with Chem-X/DiR and InsightII/Discover Software using the published X-ray structure:
-
The binding model was constructed with Chem-X/DiR and InsightII/Discover Software using the published X-ray structure: Tulinsky, A., Padmanbhan, K., Padmanbhan, K. P., Park, C. H., Bode, W., Huber, R., Blankenship, D. T., Cardin, A. D., Kiesel, W. J. Mol. Biol. 1993, 232, 947.
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Tulinsky, A.1
Padmanbhan, K.2
Padmanbhan, K.P.3
Park, C.H.4
Bode, W.5
Huber, R.6
Blankenship, D.T.7
Cardin, A.D.8
Kiesel, W.9
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28
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0041523185
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New Orleans, LA, Aug. 1999; American Chemical Society, Washington, DC, MEDI 20
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Maignan, S.; Guilloteau, J. P.; Mikol, V.; Choi-Sledeski, Y. M.; Becker, M.; Klein, S. I.; Ewing, W. R.; Pauls, H. W.; Spada, A. 218th National Meeting of the American Chemical Society, New Orleans, LA, Aug. 1999; American Chemical Society, Washington, DC, 1999; MEDI 20.
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(1999)
218th National Meeting of the American Chemical Society
-
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Maignan, S.1
Guilloteau, J.P.2
Mikol, V.3
Choi-Sledeski, Y.M.4
Becker, M.5
Klein, S.I.6
Ewing, W.R.7
Pauls, H.W.8
Spada, A.9
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29
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17644432096
-
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This biaryl P-4 unit has been used extensively by Dupont in their fXa inhibitors:
-
This biaryl P-4 unit has been used extensively by Dupont in their fXa inhibitors: Quan, M. L., Wityak, J., Dominguez, C., Duncia, J. V., Kettner, C. A., Ellis, C. D., Liauw, A. Y., Park, J. M., Santella, J. B., Knabb, R. M., Thoolen, M. J., Weber, P. C., Wexler, R. R. Bioorg. Med. Chem. Lett. 1997, 7, 1595.
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Bioorg. Med. Chem. Lett.
, vol.7
, pp. 1595
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-
Quan, M.L.1
Wityak, J.2
Dominguez, C.3
Duncia, J.V.4
Kettner, C.A.5
Ellis, C.D.6
Liauw, A.Y.7
Park, J.M.8
Santella, J.B.9
Knabb, R.M.10
Thoolen, M.J.11
Weber, P.C.12
Wexler, R.R.13
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30
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0342422174
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Activated partial thromboplastin time (APTT) was measured with a MLA Electra 800 automatic coagulation timer (Orthodiagnostics, NJ) as described in reference 17
-
Activated partial thromboplastin time (APTT) was measured with a MLA Electra 800 automatic coagulation timer (Orthodiagnostics, NJ) as described in reference 17.
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32
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0343291766
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Selected members from this series were found to be effective in animal models of thrombosis upon iv dosing; this data will be published separately
-
Selected members from this series were found to be effective in animal models of thrombosis upon iv dosing; this data will be published separately.
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