-
3
-
-
0026652586
-
-
Schaffer L.W., Davidson J.T., Vlasuk G.P., Dunwiddie C.T., and Siegl P.K.S. Arterioscler. Thromb. 12 (1992) 879
-
(1992)
Arterioscler. Thromb.
, vol.12
, pp. 879
-
-
Schaffer, L.W.1
Davidson, J.T.2
Vlasuk, G.P.3
Dunwiddie, C.T.4
Siegl, P.K.S.5
-
5
-
-
0036762612
-
-
Linkins L.-A., Julian J.A., Rischke J., Hirsh J., and Weitz J.I. Thromb. Res. 105 (2002) 241
-
(2002)
Thromb. Res.
, vol.105
, pp. 241
-
-
Linkins, L.-A.1
Julian, J.A.2
Rischke, J.3
Hirsh, J.4
Weitz, J.I.5
-
11
-
-
24944536065
-
-
Roehrig S., Straub A., Pohlmann J., Lampe T., Pererstorfer J., Schlemmer K.-H., Reinemer P., and Perzborn E. J. Med. Chem 48 (2005) 5900
-
(2005)
J. Med. Chem
, vol.48
, pp. 5900
-
-
Roehrig, S.1
Straub, A.2
Pohlmann, J.3
Lampe, T.4
Pererstorfer, J.5
Schlemmer, K.-H.6
Reinemer, P.7
Perzborn, E.8
-
12
-
-
22844442726
-
-
Perzborn E., Strassburger J., Wilmen A., Pohlmann J., Roehrig S., Schlemmer K.-H., and Straub A. J. Thromb. Haemostasis 3 (2005) 514
-
(2005)
J. Thromb. Haemostasis
, vol.3
, pp. 514
-
-
Perzborn, E.1
Strassburger, J.2
Wilmen, A.3
Pohlmann, J.4
Roehrig, S.5
Schlemmer, K.-H.6
Straub, A.7
-
13
-
-
33644867218
-
-
Eriksson B.L., Borris L., Dahl O.E., Haas S., Huisman M.V., and Kakkar A.K. J. Thromb. Haemostasis 4 (2006) 121
-
(2006)
J. Thromb. Haemostasis
, vol.4
, pp. 121
-
-
Eriksson, B.L.1
Borris, L.2
Dahl, O.E.3
Haas, S.4
Huisman, M.V.5
Kakkar, A.K.6
-
14
-
-
20144374942
-
-
Quan M.L., Lam P.Y.S., Han Q., Pinto D.J.P., He M.Y., Li R., Ellis C.D., Clark C.G., Teleha C.A., Sun J.-H., Alexander R.S., Bai S., Luettegn J.M., Knabb R.M., Wong P.C., and Wexler R.R. J. Med. Chem 48 (2005) 1729
-
(2005)
J. Med. Chem
, vol.48
, pp. 1729
-
-
Quan, M.L.1
Lam, P.Y.S.2
Han, Q.3
Pinto, D.J.P.4
He, M.Y.5
Li, R.6
Ellis, C.D.7
Clark, C.G.8
Teleha, C.A.9
Sun, J.-H.10
Alexander, R.S.11
Bai, S.12
Luettegn, J.M.13
Knabb, R.M.14
Wong, P.C.15
Wexler, R.R.16
-
15
-
-
34249705694
-
-
Wong P.C., Crain E.J., Watson C.A., Wexler R.R., Lam P.Y.S., Quan M.L., and Knabb R.M. J. Thromb. Thrombolysis 24 (2007) 43
-
(2007)
J. Thromb. Thrombolysis
, vol.24
, pp. 43
-
-
Wong, P.C.1
Crain, E.J.2
Watson, C.A.3
Wexler, R.R.4
Lam, P.Y.S.5
Quan, M.L.6
Knabb, R.M.7
-
16
-
-
35848929515
-
-
Pinto D.J.P., Orwat M.J., Koch S., Rossi K.A., Alexander R.S., Smallwood A., Wong P.C., Rendina A.R., Luettgen J.M., Knabb R.M., He K., Xin B., Wexler R.R., and Lam P.Y.S. J. Med. Chem 50 (2007) 5339
-
(2007)
J. Med. Chem
, vol.50
, pp. 5339
-
-
Pinto, D.J.P.1
Orwat, M.J.2
Koch, S.3
Rossi, K.A.4
Alexander, R.S.5
Smallwood, A.6
Wong, P.C.7
Rendina, A.R.8
Luettgen, J.M.9
Knabb, R.M.10
He, K.11
Xin, B.12
Wexler, R.R.13
Lam, P.Y.S.14
-
17
-
-
49849099533
-
-
Furugohri T., Isobe K., Honda Y., Kamisato-Matsumoto C., Sugiyama N., Nagahara T., Morishima Y., and Shibano T. J. Thromb. Haemostasis 6 (2008) 1542
-
(2008)
J. Thromb. Haemostasis
, vol.6
, pp. 1542
-
-
Furugohri, T.1
Isobe, K.2
Honda, Y.3
Kamisato-Matsumoto, C.4
Sugiyama, N.5
Nagahara, T.6
Morishima, Y.7
Shibano, T.8
-
19
-
-
63149179306
-
-
Zhang, P.; Bao, L.; Zuckett, J. F.; Jia, Z. J.; Sinha, U.; Park, G.; Hutchaleelaha, A.; Scarborough, R. M.; Zhu, B.-Y. Bioorg. Med. Chem. Lett. 2009, 19, 2186, the preceding communication, doi:10.1016/j.bmcl.2009.02.114.
-
Zhang, P.; Bao, L.; Zuckett, J. F.; Jia, Z. J.; Sinha, U.; Park, G.; Hutchaleelaha, A.; Scarborough, R. M.; Zhu, B.-Y. Bioorg. Med. Chem. Lett. 2009, 19, 2186, the preceding communication, doi:10.1016/j.bmcl.2009.02.114.
-
-
-
-
20
-
-
0034696927
-
-
50 values were determined by the method described in:
-
50 values were determined by the method described in:. Sinha U., Ku P., Malinowski J., Zhu B.Y., Scarborough R.M., Marlowe C.K., Wong P.W., Lin P.H., and Hollenbach S.J. Eur. J. Pharmacol. 395 (2000) 51
-
(2000)
Eur. J. Pharmacol.
, vol.395
, pp. 51
-
-
Sinha, U.1
Ku, P.2
Malinowski, J.3
Zhu, B.Y.4
Scarborough, R.M.5
Marlowe, C.K.6
Wong, P.W.7
Lin, P.H.8
Hollenbach, S.J.9
-
21
-
-
0033517788
-
-
i values were determined by the method described in:
-
i values were determined by the method described in:. Betz A., Wong P.W., and Sinha U. Biochemistry 38 (1999) 14582
-
(1999)
Biochemistry
, vol.38
, pp. 14582
-
-
Betz, A.1
Wong, P.W.2
Sinha, U.3
-
22
-
-
12444287963
-
-
For description of our human plasma-based thrombin generation assay (2×TG), see:
-
For description of our human plasma-based thrombin generation assay (2×TG), see:. Sinha U., Lin P.H., Edwards S.T., Wong P.W., Zhu B., Scarborough R.M., Su T., Jia Z.J., Song Y., Zhang P., Clizbe L., Park G., Reed A., Hollenbach S.J., Malinowski J., and Arfsten A.E. Arterioscler. Thromb. Vas. Biol. 23 (2003) 1098
-
(2003)
Arterioscler. Thromb. Vas. Biol.
, vol.23
, pp. 1098
-
-
Sinha, U.1
Lin, P.H.2
Edwards, S.T.3
Wong, P.W.4
Zhu, B.5
Scarborough, R.M.6
Su, T.7
Jia, Z.J.8
Song, Y.9
Zhang, P.10
Clizbe, L.11
Park, G.12
Reed, A.13
Hollenbach, S.J.14
Malinowski, J.15
Arfsten, A.E.16
-
23
-
-
0034624694
-
-
Several other laboratories have also investigated anthranilamide-derived fXa inhibitors:
-
Several other laboratories have also investigated anthranilamide-derived fXa inhibitors:. Yee Y.K., Tebbe A.L., Linebarger J.H., Beight D.W., Craft T.J., Gifford-Moore D., Goodson Jr. T., Herron D.K., Klimkowski V.J., Kyle J.A., Sawyer J.S., Smith G.F., Tinsley J.M., Towner R.D., Weir L., and Wiley M.R. J. Med. Chem. 43 (2000) 873
-
(2000)
J. Med. Chem.
, vol.43
, pp. 873
-
-
Yee, Y.K.1
Tebbe, A.L.2
Linebarger, J.H.3
Beight, D.W.4
Craft, T.J.5
Gifford-Moore, D.6
Goodson Jr., T.7
Herron, D.K.8
Klimkowski, V.J.9
Kyle, J.A.10
Sawyer, J.S.11
Smith, G.F.12
Tinsley, J.M.13
Towner, R.D.14
Weir, L.15
Wiley, M.R.16
-
24
-
-
0035939308
-
-
Shrader W.D., Young W.B., Sprengler P.A., Sangalang J.C., Elrod K., and Carr G. Bioorg. Med. Chem. Lett. 11 (2001) 1801
-
(2001)
Bioorg. Med. Chem. Lett.
, vol.11
, pp. 1801
-
-
Shrader, W.D.1
Young, W.B.2
Sprengler, P.A.3
Sangalang, J.C.4
Elrod, K.5
Carr, G.6
-
25
-
-
0037328153
-
-
Chou Y.-L., Davey D.D., Eagen K.A., Griedel B.D., Karanjawala R., Philips G.B., Sacchi K.L., Shaw K.J., Wu S.C., Lentz D., Liang A.M., Trin L., Morrissey M.M., and Kochanny M.J. Bioorg. Med. Chem. Lett. 13 (2003) 507
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 507
-
-
Chou, Y.-L.1
Davey, D.D.2
Eagen, K.A.3
Griedel, B.D.4
Karanjawala, R.5
Philips, G.B.6
Sacchi, K.L.7
Shaw, K.J.8
Wu, S.C.9
Lentz, D.10
Liang, A.M.11
Trin, L.12
Morrissey, M.M.13
Kochanny, M.J.14
-
26
-
-
33846617308
-
-
Kochanny M.J., Alder M., Ewing J., Griedel B.D., Ho E., Karanjawala R., Lee W., Lentz D., Liang A.M., Morrissey M.M., Phillips G.B., Post J., Sacchi K.L., Sakata S.T., Subramanyam B., Vergona R., Walters J., White K.A., Whitlow M., Ye B., Zhao Z., and Shaw K.J. Bioorg. Med. Chem. 15 (2007) 2127
-
(2007)
Bioorg. Med. Chem.
, vol.15
, pp. 2127
-
-
Kochanny, M.J.1
Alder, M.2
Ewing, J.3
Griedel, B.D.4
Ho, E.5
Karanjawala, R.6
Lee, W.7
Lentz, D.8
Liang, A.M.9
Morrissey, M.M.10
Phillips, G.B.11
Post, J.12
Sacchi, K.L.13
Sakata, S.T.14
Subramanyam, B.15
Vergona, R.16
Walters, J.17
White, K.A.18
Whitlow, M.19
Ye, B.20
Zhao, Z.21
Shaw, K.J.22
more..
-
27
-
-
34347213453
-
-
Ye B., Arniaz D.O., Chuo Y.-L., Griedel B.D., Karanjawala R., Lee W., Morrissey M.M., Sacchi K.L., Sakata S.T., Shaw K.J., Wu S.C., Zhao Z., Adler M., Cheeseman S., Dole W.P., Ewing J., Fitch R., Lentz D., Liang A., Light D., Morser J., Post J., Rumennik G., Subramanyam B., Sullivan M.E., Vergona R., Walters J., Wang Y.-X., White K.A., Whitlow M., and Kochanny M.J. J. Med. Chem. 50 (2007) 2967
-
(2007)
J. Med. Chem.
, vol.50
, pp. 2967
-
-
Ye, B.1
Arniaz, D.O.2
Chuo, Y.-L.3
Griedel, B.D.4
Karanjawala, R.5
Lee, W.6
Morrissey, M.M.7
Sacchi, K.L.8
Sakata, S.T.9
Shaw, K.J.10
Wu, S.C.11
Zhao, Z.12
Adler, M.13
Cheeseman, S.14
Dole, W.P.15
Ewing, J.16
Fitch, R.17
Lentz, D.18
Liang, A.19
Light, D.20
Morser, J.21
Post, J.22
Rumennik, G.23
Subramanyam, B.24
Sullivan, M.E.25
Vergona, R.26
Walters, J.27
Wang, Y.-X.28
White, K.A.29
Whitlow, M.30
Kochanny, M.J.31
more..
-
28
-
-
34547542123
-
-
Mendel D., Marquart A.L., Joseph S., Waid P., Yee Y.K., Tebbe A.L., Ratz A.M., Herron D.K., Goodson T., Masters J.J., Franciskovich J.B., Tinsley J.M., Wiley M.R., Weir L.C., Kyle J.A., Klimkowski V.J., Smith G.F., Towner R.D., Froelich L.L., Buben J., and Craft T.J. Bioorg. Med. Chem. Lett. 17 (2007) 4832
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 4832
-
-
Mendel, D.1
Marquart, A.L.2
Joseph, S.3
Waid, P.4
Yee, Y.K.5
Tebbe, A.L.6
Ratz, A.M.7
Herron, D.K.8
Goodson, T.9
Masters, J.J.10
Franciskovich, J.B.11
Tinsley, J.M.12
Wiley, M.R.13
Weir, L.C.14
Kyle, J.A.15
Klimkowski, V.J.16
Smith, G.F.17
Towner, R.D.18
Froelich, L.L.19
Buben, J.20
Craft, T.J.21
more..
-
29
-
-
42949134940
-
-
Corte J.R., Fang T., Pinto D.J.P., Han W., Hu Z., Jiang X.-J., Li Y.-L., Gauuan J.F., Hadden M., Orton D., Rendina A.R., Luettgen J.M., Wong P.C., He K., Morin P.E., Chang C.-W., Cheney D.L., Knabb R.M., Wexler R.R., and Lam P.Y.S. Bioorg. Med. Chem. Lett. 18 (2008) 2845
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 2845
-
-
Corte, J.R.1
Fang, T.2
Pinto, D.J.P.3
Han, W.4
Hu, Z.5
Jiang, X.-J.6
Li, Y.-L.7
Gauuan, J.F.8
Hadden, M.9
Orton, D.10
Rendina, A.R.11
Luettgen, J.M.12
Wong, P.C.13
He, K.14
Morin, P.E.15
Chang, C.-W.16
Cheney, D.L.17
Knabb, R.M.18
Wexler, R.R.19
Lam, P.Y.S.20
more..
-
30
-
-
0031552362
-
-
Jones G., Willet P., Glen R.C., Leach A.R., and Taylor R. J. Mol. Biol. 267 (1997) 727
-
(1997)
J. Mol. Biol.
, vol.267
, pp. 727
-
-
Jones, G.1
Willet, P.2
Glen, R.C.3
Leach, A.R.4
Taylor, R.5
-
31
-
-
0037207123
-
-
Adler M., Kochanny M.J., Ye B., Rumennik G., Light D.R., Biancalana S., and Whitlow M. Biochemistry 41 (2002) 15514
-
(2002)
Biochemistry
, vol.41
, pp. 15514
-
-
Adler, M.1
Kochanny, M.J.2
Ye, B.3
Rumennik, G.4
Light, D.R.5
Biancalana, S.6
Whitlow, M.7
-
32
-
-
63149131512
-
-
note
-
In vitro liver metabolic stability was determined using liver S9 fractions and expressed as half-life: Compounds (1 μM) were incubated with liver S9 proteins (1 mg/mL) and a NADPH regenerating system (NADP + glucose-6-phosphate) suspended in phosphate buffer (100 mM). Samples were taken at t = 0, 5, 10, 15 and 60 min. and added to an organic solvent to terminate the reaction. After adding an internal standard, the mixtures were centrifuged and the supernatant transferred to HPLC vials. Samples were analyzed by tandem-mass spectrometry. The change in area ratio (substrate/internal standard) between t = 0 and 15 min was used to estimate half-life. Coumarin 7-hydroxylase (CYP2A6), caffeine demethylase (CYP1A2), verapamil (CYP3A4) and/or propanolol (CYP3A4) were used as positive control. For negative controls, substrates were incubated with heat inactivated (60 min at 60 °C) liver S9 fractions.
-
-
-
-
33
-
-
10744221472
-
-
Jia Z.J., Wu Y., Huang W., Zhang P., Song Y., Woolfrey J., Sinha U., Arfsten A.E., Edwards S.T., Hutchaleelaha A., Hollenbach S.J., Lambing J.L., Scarborough R.M., and Zhu B.-Y. Bioorg. Med. Chem. Lett. 14 (2004) 1229
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 1229
-
-
Jia, Z.J.1
Wu, Y.2
Huang, W.3
Zhang, P.4
Song, Y.5
Woolfrey, J.6
Sinha, U.7
Arfsten, A.E.8
Edwards, S.T.9
Hutchaleelaha, A.10
Hollenbach, S.J.11
Lambing, J.L.12
Scarborough, R.M.13
Zhu, B.-Y.14
-
34
-
-
11144357441
-
-
Jia Z.J., Su T., Zuckett J.F., Wu Y., Goldman E.A., Li W., Zhang P., Clizbe L.A., Song Y., Bauer S.M., Huang W., Woolfrey J., Sinha U., Arfsten A.E., Hutchaleelaha A., Hollenbach S.J., Lambing J.L., Scarborough R.M., and Zhu B.-Y. Bioorg. Med. Chem. Lett. 14 (2004) 2073
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 2073
-
-
Jia, Z.J.1
Su, T.2
Zuckett, J.F.3
Wu, Y.4
Goldman, E.A.5
Li, W.6
Zhang, P.7
Clizbe, L.A.8
Song, Y.9
Bauer, S.M.10
Huang, W.11
Woolfrey, J.12
Sinha, U.13
Arfsten, A.E.14
Hutchaleelaha, A.15
Hollenbach, S.J.16
Lambing, J.L.17
Scarborough, R.M.18
Zhu, B.-Y.19
-
35
-
-
33748770143
-
-
Zhu B.-Y., Jia Z.J., Zhang P., Su T., Huang W., Goldman E., Tumas D., Kadambi V., Eddy P., Sinha U., Scarborough R.M., and Song Y. Bioorg. Med. Chem. Lett. 16 (2006) 5507
-
(2006)
Bioorg. Med. Chem. Lett.
, vol.16
, pp. 5507
-
-
Zhu, B.-Y.1
Jia, Z.J.2
Zhang, P.3
Su, T.4
Huang, W.5
Goldman, E.6
Tumas, D.7
Kadambi, V.8
Eddy, P.9
Sinha, U.10
Scarborough, R.M.11
Song, Y.12
-
36
-
-
0035955293
-
-
Finalayson K., Turnbull L., January C.T., Sharkey J., and Kelly J.S. Eur. J. Pharmacol. 430 (2001) 147
-
(2001)
Eur. J. Pharmacol.
, vol.430
, pp. 147
-
-
Finalayson, K.1
Turnbull, L.2
January, C.T.3
Sharkey, J.4
Kelly, J.S.5
-
37
-
-
0036258115
-
-
De Ponti F., Poluzzi E., Cavalli A., Recanatini M., and Montanaro N. Drug Saf. 25 (2002) 263
-
(2002)
Drug Saf.
, vol.25
, pp. 263
-
-
De Ponti, F.1
Poluzzi, E.2
Cavalli, A.3
Recanatini, M.4
Montanaro, N.5
-
39
-
-
0344492207
-
-
Redfern W.S., Carlsson L., Davis A.S., Lynch W.G., Mackenzie I., Palethorpe S., Siegl P.K.S., Strang I., Sullivan A.T., Wallis R., Camm A.J., and Hammond T.G. Cardiovas. Res. 58 (2003) 32
-
(2003)
Cardiovas. Res.
, vol.58
, pp. 32
-
-
Redfern, W.S.1
Carlsson, L.2
Davis, A.S.3
Lynch, W.G.4
Mackenzie, I.5
Palethorpe, S.6
Siegl, P.K.S.7
Strang, I.8
Sullivan, A.T.9
Wallis, R.10
Camm, A.J.11
Hammond, T.G.12
-
43
-
-
63149099847
-
-
Abstract 907
-
Sinha U., Edwards S.T., Wong P.W., Delaney S.M., Nanda N., Marzec U.M., Pak Y., Hollenbach S.J., Hanson S.R., and Scarborough R.M. Blood 108 (2006) Abstract 907
-
(2006)
Blood
, vol.108
-
-
Sinha, U.1
Edwards, S.T.2
Wong, P.W.3
Delaney, S.M.4
Nanda, N.5
Marzec, U.M.6
Pak, Y.7
Hollenbach, S.J.8
Hanson, S.R.9
Scarborough, R.M.10
-
44
-
-
63149104131
-
-
Abstract 901
-
Abe K., Siu G., Edwards S., Lin P.H., Zhu B.-Y., Marzec U.M., Hanson S.R., Pak Y., Hollenbach S.J., and Sinha U. Blood 108 (2006) Abstract 901
-
(2006)
Blood
, vol.108
-
-
Abe, K.1
Siu, G.2
Edwards, S.3
Lin, P.H.4
Zhu, B.-Y.5
Marzec, U.M.6
Hanson, S.R.7
Pak, Y.8
Hollenbach, S.J.9
Sinha, U.10
-
45
-
-
63149138310
-
-
note
-
The rabbit 2×PT values were determined by the method described in Ref. 5(b).
-
-
-
-
46
-
-
63149134395
-
-
note
-
Human plasma protein binding, expressed as unbound fraction, was determined by this protocol: The compound stock solutions were diluted in 1.0 M HEPES (pH 7.4) to yield a 1.0 mM working solution. The working solution was added to plasma samples (EDTA was used as anticoagulant) in a ratio of 1/100 yielding a final concentration of 10 μM. The mixture was gently mixed and incubated at 37 °C for 30 min. At the conclusion of the incubation 3 aliquots (450 μL) each were added to a centrifugal filter device fitted to a 96 well plate. Standards were prepared in protein free human plasma and transferred to the centrifugal filter device fitted to the same plate. The plates were centrifuged for 25 min at 32 °C in a centrifuge. 15 μL each of the filtrate was transferred to a round bottom 96 well plate and 15 μL of acetonitrile including KN1022 (1 μg/mL) as internal standard was added followed by 60 μL of DI water. Plates were placed on a Multi-Tube Vortexer for 30 s and vortexed. Concentrations in the filtrate were determined by LC/MS/MS and using standard curves prepared in ultra filtrated plasma.
-
-
-
-
47
-
-
0031982513
-
-
Kr current generated under normoxic conditions. Interference of the potassium channel suggests that the compound could modify (shorten or prolong) the electrocardiographic (ECG) QT interval.
-
Kr current generated under normoxic conditions. Interference of the potassium channel suggests that the compound could modify (shorten or prolong) the electrocardiographic (ECG) QT interval. Zhou Z., Gong Q., Ye B., Fan Z., Makielski J.C., Robertson G.A., and January C.T. Biophys. J. 74 (1998) 230
-
(1998)
Biophys. J.
, vol.74
, pp. 230
-
-
Zhou, Z.1
Gong, Q.2
Ye, B.3
Fan, Z.4
Makielski, J.C.5
Robertson, G.A.6
January, C.T.7
-
48
-
-
0013483205
-
-
Zhou Z., Gong Q., Ye B., Fan F., Makielski J.C., Robertson G.A., and January C.T. Biophys. J. 72 (1997) A225
-
(1997)
Biophys. J.
, vol.72
-
-
Zhou, Z.1
Gong, Q.2
Ye, B.3
Fan, F.4
Makielski, J.C.5
Robertson, G.A.6
January, C.T.7
-
51
-
-
60849097858
-
-
Turpie A.G.G., Bauer K.A., Davidson B.L., Fisher W.D., Gent M., Huo M.H., Sinha U., and Gretlet D.D. Thromb. Haemostasis 101 (2009) 68
-
(2009)
Thromb. Haemostasis
, vol.101
, pp. 68
-
-
Turpie, A.G.G.1
Bauer, K.A.2
Davidson, B.L.3
Fisher, W.D.4
Gent, M.5
Huo, M.H.6
Sinha, U.7
Gretlet, D.D.8
|