-
1
-
-
85031154986
-
-
Thrombosis in Cardiovascular Disorders; Fuster, V., Verstraete, M., Eds.; W.B. Saunders: Philadelphia, 1992.
-
Thrombosis in Cardiovascular Disorders; Fuster, V., Verstraete, M., Eds.; W.B. Saunders: Philadelphia, 1992.
-
-
-
-
2
-
-
85031158630
-
-
Parenteral administration of low molecular weight heparin and intense patient monitoring required with warfarin limit their chronic utility.
-
-
-
-
4
-
-
0001780059
-
-
Coburn C.A. Exp. Opin. Ther. Patents. 11:2001;1 Sanderson P.E.J. Annu. Rep. Med. Chem. 36:2001;79 Vacca J.P. Annu. Rep. Med. Chem. 33:1998;81.
-
(2001)
Exp. Opin. Ther. Patents
, vol.11
, pp. 1
-
-
Coburn, C.A.1
-
5
-
-
0002362826
-
-
Coburn C.A. Exp. Opin. Ther. Patents. 11:2001;1 Sanderson P.E.J. Annu. Rep. Med. Chem. 36:2001;79 Vacca J.P. Annu. Rep. Med. Chem. 33:1998;81.
-
(2001)
Annu. Rep. Med. Chem.
, vol.36
, pp. 79
-
-
Sanderson, P.E.J.1
-
6
-
-
77956716245
-
-
Coburn C.A. Exp. Opin. Ther. Patents. 11:2001;1 Sanderson P.E.J. Annu. Rep. Med. Chem. 36:2001;79 Vacca J.P. Annu. Rep. Med. Chem. 33:1998;81.
-
(1998)
Annu. Rep. Med. Chem.
, vol.33
, pp. 81
-
-
Vacca, J.P.1
-
7
-
-
15444357642
-
-
(a) Tucker T.J., Brady S.F., Lumma W.C., Lewis S.D., Gardell S.J., Naylor-Olsen A.M., Yan Y., Sisko J.T., Stauffer K.J., Lucas B.J., Lynch J.J., Cook J.J., Stranieri M.T., Holahan M., Lyle E.A., Baskin E.P., Chen I.W., Dancheck K.B., Krueger J.A., Cooper C.M., Vacca J.P. J. Med. Chem. 41:1998;3210
-
(1998)
J. Med. Chem.
, vol.41
, pp. 3210
-
-
Tucker, T.J.1
Brady, S.F.2
Lumma, W.C.3
Lewis, S.D.4
Gardell, S.J.5
Naylor-Olsen, A.M.6
Yan, Y.7
Sisko, J.T.8
Stauffer, K.J.9
Lucas, B.J.10
Lynch, J.J.11
Cook, J.J.12
Stranieri, M.T.13
Holahan, M.14
Lyle, E.A.15
Baskin, E.P.16
Chen, I.W.17
Dancheck, K.B.18
Krueger, J.A.19
Cooper, C.M.20
Vacca, J.P.21
more..
-
8
-
-
0030895222
-
-
(b) Tucker T.J., Lumma W.C., Mulichak A.M., Chen Z., Naylor-Olsen A.M., Lewis S.D., Lucas B.J., Freidinger R.M., Kuo L.C. J. Med. Chem. 40:1997;830.
-
(1997)
J. Med. Chem.
, vol.40
, pp. 830
-
-
Tucker, T.J.1
Lumma, W.C.2
Mulichak, A.M.3
Chen, Z.4
Naylor-Olsen, A.M.5
Lewis, S.D.6
Lucas, B.J.7
Freidinger, R.M.8
Kuo, L.C.9
-
9
-
-
0037434510
-
-
Burgey C.S., Robinson K.A., Lyle T.A., Sanderson P.E.J., Lewis S.D., Lucas B.J., Krueger J.A., Lyle E.A., Stranieri M.T., Holahan M., Sitko G.R., Cook J.J., Wallace A.A., Clayton F., Bohn D., Leonard Y., Detwiler T., Lynch J.J., Williams P.D., Coburn C.A., Dorsey B.D., McMasters D.R., McDonough C.M., Sanders W.M., Gardell S.J., Shafer J.A., Vacca J.P. J. Med. Chem. 46:2003;461.
-
(2003)
J. Med. Chem.
, vol.46
, pp. 461
-
-
Burgey, C.S.1
Robinson, K.A.2
Lyle, T.A.3
Sanderson, P.E.J.4
Lewis, S.D.5
Lucas, B.J.6
Krueger, J.A.7
Lyle, E.A.8
Stranieri, M.T.9
Holahan, M.10
Sitko, G.R.11
Cook, J.J.12
Wallace, A.A.13
Clayton, F.14
Bohn, D.15
Leonard, Y.16
Detwiler, T.17
Lynch, J.J.18
Williams, P.D.19
Coburn, C.A.20
Dorsey, B.D.21
McMasters, D.R.22
McDonough, C.M.23
Sanders, W.M.24
Gardell, S.J.25
Shafer, J.A.26
Vacca, J.P.27
more..
-
10
-
-
85031148484
-
-
4.
-
-
-
-
13
-
-
0030591845
-
-
(c) Greco M.N., Powell E.T., Hecker L.R., Andrade-Gordon P., Kauffman J.A., Lewis J.M., Ganesh V., Tulinsky A., Maryanoff B.E. Bioorg. Med. Chem. Lett. 6:1996;2947
-
(1996)
Bioorg. Med. Chem. Lett.
, vol.6
, pp. 2947
-
-
Greco, M.N.1
Powell, E.T.2
Hecker, L.R.3
Andrade-Gordon, P.4
Kauffman, J.A.5
Lewis, J.M.6
Ganesh, V.7
Tulinsky, A.8
Maryanoff, B.E.9
-
14
-
-
0029133970
-
-
(d) Maryanoff B.E., Zhang H.C., Greco M.N., Glover K.A., Kauffman J.A., Andrade-Gordon P. Bioorg. Med. Chem. 3:1995;1025.
-
(1995)
Bioorg. Med. Chem.
, vol.3
, pp. 1025
-
-
Maryanoff, B.E.1
Zhang, H.C.2
Greco, M.N.3
Glover, K.A.4
Kauffman, J.A.5
Andrade-Gordon, P.6
-
15
-
-
0026092714
-
-
Horwell D.C., Hugues J., Hunter J.C., Pritchard M.C., Richardson R.S., Roberts E., Woodruff G.N. J. Med. Chem. 34:1991;404.
-
(1991)
J. Med. Chem.
, vol.34
, pp. 404
-
-
Horwell, D.C.1
Hugues, J.2
Hunter, J.C.3
Pritchard, M.C.4
Richardson, R.S.5
Roberts, E.6
Woodruff, G.N.7
-
18
-
-
0028824368
-
-
Lewis S.D., Ng A.S., Lyle E.A., Mellott M.J., Appelby S.D., Brady S.F., Stauffer K.S., Sisko J.T., Mao S.-S., Veber D.F., Nutt R.F., Lynch J.J., Cook J.J., Gardell S.J., Shafer J.A. Thromb. Haemost. 74:1995;1107.
-
(1995)
Thromb. Haemost.
, vol.74
, pp. 1107
-
-
Lewis, S.D.1
Ng, A.S.2
Lyle, E.A.3
Mellott, M.J.4
Appelby, S.D.5
Brady, S.F.6
Stauffer, K.S.7
Sisko, J.T.8
Mao, S.-S.9
Veber, D.F.10
Nutt, R.F.11
Lynch, J.J.12
Cook, J.J.13
Gardell, S.J.14
Shafer, J.A.15
-
19
-
-
0343443219
-
-
Tucker T.J., Lumma W.C., Lewis S.D., Gardell S.J., Lucas B.J., Baskin E.P., Woltmann R., Lynch J.J., Lyle E.A., Appleby S.D., Chen I.-W., Dancheck K.B., Vacca J.P. J. Med. Chem. 40:1997;1565.
-
(1997)
J. Med. Chem.
, vol.40
, pp. 1565
-
-
Tucker, T.J.1
Lumma, W.C.2
Lewis, S.D.3
Gardell, S.J.4
Lucas, B.J.5
Baskin, E.P.6
Woltmann, R.7
Lynch, J.J.8
Lyle, E.A.9
Appleby, S.D.10
Chen, I.-W.11
Dancheck, K.B.12
Vacca, J.P.13
-
20
-
-
85031161505
-
-
Calculated LogP (ChemDraw) for 20 and 23 are 3.7 and 2.6. respectively.
-
-
-
-
21
-
-
15444357766
-
-
Lumma W.C., Witherup K.M., Tucker T.J., Brady S.F., Sisko J.T., Naylor-Olsen A.M., Lewis S.D., Lucas B.J., Vacca J.P. J. Med. Chem. 41:1998;1011.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 1011
-
-
Lumma, W.C.1
Witherup, K.M.2
Tucker, T.J.3
Brady, S.F.4
Sisko, J.T.5
Naylor-Olsen, A.M.6
Lewis, S.D.7
Lucas, B.J.8
Vacca, J.P.9
-
22
-
-
84986437005
-
-
Multiple conformations of the macrocycles were generated using the metric matrix distance geometry algorithm JG (S. Kearsley, Merck & Co., Inc., unpublished). The generated conformers were energy-minimized within the thrombin active site using MacroModel (ref 17b) with the MMFF force field, and allowing Glu192 to adjust to the inhibitor.
-
(a) Multiple conformations of the macrocycles were generated using the metric matrix distance geometry algorithm JG (S. Kearsley, Merck & Co., Inc., unpublished). The generated conformers were energy-minimized within the thrombin active site using MacroModel (ref 17b) with the MMFF force field, and allowing Glu192 to adjust to the inhibitor. (b) Mohamadi F., Richards N.G.J., Guida W.C., Liskamp R., Lipton M., Caufield C., Chang G., Hendrickson T., Still W.C. J. Comput. Chem. 11:1990;440.
-
(1990)
J. Comput. Chem.
, vol.11
, pp. 440
-
-
Mohamadi, F.1
Richards, N.G.J.2
Guida, W.C.3
Liskamp, R.4
Lipton, M.5
Caufield, C.6
Chang, G.7
Hendrickson, T.8
Still, W.C.9
-
23
-
-
0032558382
-
-
Differences in electrostatic potential caused by E/Q192 have been proposed as an important factor in the selective binding of PAI-1 to tPA versus thrombin.
-
Differences in electrostatic potential caused by E/Q192 have been proposed as an important factor in the selective binding of PAI-1 to tPA versus thrombin. Rezaie A.R. Biochemistry. 37:1998;13138.
-
(1998)
Biochemistry
, vol.37
, pp. 13138
-
-
Rezaie, A.R.1
|