-
1
-
-
0030671160
-
Antithrombotic Agents and Thromboembolic Disease
-
Ewenstein, B. M. Antithrombotic Agents and Thromboembolic Disease. N. Engl. J. Med. 1997, 337, 1383-1384.
-
(1997)
N. Engl. J. Med.
, vol.337
, pp. 1383-1384
-
-
Ewenstein, B.M.1
-
3
-
-
0030693694
-
Small-Molecule Direct Thrombin Inhibitors
-
Wiley, M. R.; Fisher, M. J. Small-Molecule Direct Thrombin Inhibitors. Exp. Opin. Ther. Patents 1997, 7, 1265-1282.
-
(1997)
Exp. Opin. Ther. Patents
, vol.7
, pp. 1265-1282
-
-
Wiley, M.R.1
Fisher, M.J.2
-
4
-
-
19244378454
-
Discovery and Development of the Novel Potent Orally Active Thrombin Inhibitor N-(9- hydroxy-9-fluorenylcarboxy)-prolyl trans-4-Aminocyclohexylmethyl Amide (L-372,460): Coapplication of Structure-Based Design and Rapid Multiple Analogue Synthesis on Solid Support
-
Brady, S. F.; Stauffer, K. J.; Lumma, W. C.; Smith, G. M.; Ramjit, H.; Lewis, S. D.; Lucas, B. J.; Gardell, S. J.; Lyle, E. A.; Appleby, S. D.; Cook, J. J.; Holahan, M. A.; Stranieri, M. T.; Lynch, J. J.; Lin, J. H.; Chen, I-W.; Varstag, K.; Naylor-Olsen, A. M.; Vacca, J. P. Discovery and Development of the Novel Potent Orally Active Thrombin Inhibitor N-(9- Hydroxy-9-fluorenylcarboxy)-prolyl trans-4-Aminocyclohexylmethyl Amide (L-372,460): Coapplication of Structure-Based Design and Rapid Multiple Analogue Synthesis on Solid Support. J. Med. Chem. 1998, 41, 401-406.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 401-406
-
-
Brady, S.F.1
Stauffer, K.J.2
Lumma, W.C.3
Smith, G.M.4
Ramjit, H.5
Lewis, S.D.6
Lucas, B.J.7
Gardell, S.J.8
Lyle, E.A.9
Appleby, S.D.10
Cook, J.J.11
Holahan, M.A.12
Stranieri, M.T.13
Lynch, J.J.14
Lin, J.H.15
Chen, I.-W.16
Varstag, K.17
Naylor-Olsen, A.M.18
Vacca, J.P.19
-
5
-
-
0031984477
-
Effects of Melagatran, a New Low-molecular- weight Thrombin Inhibitor, on Thrombin and Fibrinolytic Enzymes
-
Gustafsson, D.; Antonsson, T.; Bylund, R.; Eriksson, U.; Gyzander, E.; Nilsson, I.; Elg, M.; Mattsson, C.; Deinum, J.; Pehrsson, S.; Karlsson, O.; Nilsson, A.; Sorensen, H. Effects of Melagatran, a New Low-molecular- weight Thrombin Inhibitor, on Thrombin and Fibrinolytic Enzymes. Thromb. Haemost. 1998, 79, 110-118.
-
(1998)
Thromb. Haemost.
, vol.79
, pp. 110-118
-
-
Gustafsson, D.1
Antonsson, T.2
Bylund, R.3
Eriksson, U.4
Gyzander, E.5
Nilsson, I.6
Elg, M.7
Mattsson, C.8
Deinum, J.9
Pehrsson, S.10
Karlsson, O.11
Nilsson, A.12
Sorensen, H.13
-
6
-
-
0031025330
-
CVS-1123, A Direct Thrombin Inhibitor, Prevents Occlusive Arterial and Venous Thrombosis in a Canine Model of Vascular Injury
-
Rebello, S. S.; Miller, B. V.; Basler, G. C.; Lucchesi, B. R. CVS-1123, A Direct Thrombin Inhibitor, Prevents Occlusive Arterial and Venous Thrombosis in a Canine Model of Vascular Injury. J. Cardiovasc. Pharmacol. 1997, 29, 240-249. Cousins, G. R.; Friedrichs, G. S.; Sudo, Y.; Rebello, S. S.; Rote, W. E.; Vlasuk, G. P.; Nolan, T. G.; Mendoza, M.; Lucchesi, B. R. Orally Effective CVS-1123 Prevents Coronary Artery Thrombosis in the Conscious Dog. Circulation 1996, 94, 1705-1712.
-
(1997)
J. Cardiovasc. Pharmacol.
, vol.29
, pp. 240-249
-
-
Rebello, S.S.1
Miller, B.V.2
Basler, G.C.3
Lucchesi, B.R.4
-
7
-
-
0029778319
-
Orally Effective CVS-1123 Prevents Coronary Artery Thrombosis in the Conscious Dog
-
Rebello, S. S.; Miller, B. V.; Basler, G. C.; Lucchesi, B. R. CVS-1123, A Direct Thrombin Inhibitor, Prevents Occlusive Arterial and Venous Thrombosis in a Canine Model of Vascular Injury. J. Cardiovasc. Pharmacol. 1997, 29, 240-249. Cousins, G. R.; Friedrichs, G. S.; Sudo, Y.; Rebello, S. S.; Rote, W. E.; Vlasuk, G. P.; Nolan, T. G.; Mendoza, M.; Lucchesi, B. R. Orally Effective CVS-1123 Prevents Coronary Artery Thrombosis in the Conscious Dog. Circulation 1996, 94, 1705-1712.
-
(1996)
Circulation
, vol.94
, pp. 1705-1712
-
-
Cousins, G.R.1
Friedrichs, G.S.2
Sudo, Y.3
Rebello, S.S.4
Rote, W.E.5
Vlasuk, G.P.6
Nolan, T.G.7
Mendoza, M.8
Lucchesi, B.R.9
-
8
-
-
0032492658
-
L-374,087, An Efficacious, Orally Bioavailable, Pyridinone Acetamide Thrombin Inhibitor
-
Sanderson, P. E. J.; Cutrona, K. J.; Dorsey, B. D.; Dyer, D. L.; McDonough, C. M.; Naylor-Olsen, A. M.; Chen, I-W.; Chen, Z.; Cook, J. J.; Gardell, S. J.; Krueger, J. A.; Lewis, S. D.; Lin, J. H.; Lucas, B. J.; Lyle, E. A.; Lynch, J. J.; Stranieri, M. T.; Vastag, K.; Shafer, J. A.; Vacca, J. P. L-374,087, An Efficacious, Orally Bioavailable, Pyridinone Acetamide Thrombin Inhibitor. Bioorg. Med. Chem. Lett. 1998, 8, 817-822.
-
(1998)
Bioorg. Med. Chem. Lett.
, vol.8
, pp. 817-822
-
-
Sanderson, P.E.J.1
Cutrona, K.J.2
Dorsey, B.D.3
Dyer, D.L.4
McDonough, C.M.5
Naylor-Olsen, A.M.6
Chen, I.-W.7
Chen, Z.8
Cook, J.J.9
Gardell, S.J.10
Krueger, J.A.11
Lewis, S.D.12
Lin, J.H.13
Lucas, B.J.14
Lyle, E.A.15
Lynch, J.J.16
Stranieri, M.T.17
Vastag, K.18
Shafer, J.A.19
Vacca, J.P.20
more..
-
9
-
-
0028245052
-
Design of Orally Active, Non-Peptidic Inhibitors of Human Leukocyte Elastase
-
Brown, F. J.; Andisik, D. W.; Bernstein, P. R.; Bryant, C. B.; Ceccarelli, C.; Damewood, J. R.; Edwards, P. D.; Earley, R. A.; Feeney, S.; Green, R. C.; Gomes, B.; Kosmider, B. J.; Krell, R. D.; Shaw, A.; Steelman, G. B.; Thomas, R. M.; Vacek, E. P.; Veale, C. A.; Tuthill, P. A.; Warner, P.; Williams, J. C.; Wolanin, D. J.; Woolson, S. A. Design of Orally Active, Non-Peptidic Inhibitors of Human Leukocyte Elastase. J. Med. Chem. 1994, 37, 1259-1261. Warner, P.; Green, R. C.; Gomes, B.; Strimpler, A. M. Nonpeptidic Inhibitors of Human Leukocyte Elastase. 1. The Design and Synthesis of Pyridone-Containing Inhibitors. J. Med. Chem. 1994, 37, 3090-3099.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 1259-1261
-
-
Brown, F.J.1
Andisik, D.W.2
Bernstein, P.R.3
Bryant, C.B.4
Ceccarelli, C.5
Damewood, J.R.6
Edwards, P.D.7
Earley, R.A.8
Feeney, S.9
Green, R.C.10
Gomes, B.11
Kosmider, B.J.12
Krell, R.D.13
Shaw, A.14
Steelman, G.B.15
Thomas, R.M.16
Vacek, E.P.17
Veale, C.A.18
Tuthill, P.A.19
Warner, P.20
Williams, J.C.21
Wolanin, D.J.22
Woolson, S.A.23
more..
-
10
-
-
0027996496
-
Nonpeptidic Inhibitors of Human Leukocyte Elastase. 1. The Design and Synthesis of Pyridone-Containing Inhibitors
-
Brown, F. J.; Andisik, D. W.; Bernstein, P. R.; Bryant, C. B.; Ceccarelli, C.; Damewood, J. R.; Edwards, P. D.; Earley, R. A.; Feeney, S.; Green, R. C.; Gomes, B.; Kosmider, B. J.; Krell, R. D.; Shaw, A.; Steelman, G. B.; Thomas, R. M.; Vacek, E. P.; Veale, C. A.; Tuthill, P. A.; Warner, P.; Williams, J. C.; Wolanin, D. J.; Woolson, S. A. Design of Orally Active, Non-Peptidic Inhibitors of Human Leukocyte Elastase. J. Med. Chem. 1994, 37, 1259-1261. Warner, P.; Green, R. C.; Gomes, B.; Strimpler, A. M. Nonpeptidic Inhibitors of Human Leukocyte Elastase. 1. The Design and Synthesis of Pyridone-Containing Inhibitors. J. Med. Chem. 1994, 37, 3090-3099.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 3090-3099
-
-
Warner, P.1
Green, R.C.2
Gomes, B.3
Strimpler, A.M.4
-
11
-
-
0028143534
-
Design and Synthesis of Potent and Highly Selective Thrombin Inhibitors
-
For the nomenclature, see: Hilpert, K.; Ackermann, J.; Banner, D. W.; Gast, A.; Gubernator, K.; Hadvary, P.; Labler, L.; Muller, K.; Schmid, G.; Tschopp, T. B.; van de Waterbeemd, H. Design and Synthesis of Potent and Highly Selective Thrombin Inhibitors. J. Med. Chem. 1994, 37, 3889-3901.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 3889-3901
-
-
Hilpert, K.1
Ackermann, J.2
Banner, D.W.3
Gast, A.4
Gubernator, K.5
Hadvary, P.6
Labler, L.7
Muller, K.8
Schmid, G.9
Tschopp, T.B.10
Van de Waterbeemd, H.11
-
12
-
-
9844234264
-
Discovery of a Novel, Selective and Orally Bioavailable Class of Thrombin Inhibitors Incorporating Aminopyridyl Moieties in the P1 Position
-
For prior use of related peptidyl aminopyridines, see: Feng, D.-M.; Gardell, S. J.; Lewis, S. D.; Bock, M. G.; Chen, Z.; Freidinger, R. M.; Naylor-Olsen, A. M.; Ramjit, H. G.; Woltmann, R.; Baskin, E. P.; Lynch, J. J.; Lucas, R.; Shafer, J. A.; Dancheck, K. B.; Chen, I-W.; Mao, S.-S.; Krueger, J. A.; Hare, T. R.; Mulichak, A. M.; Vacca, J. P. Discovery of a Novel, Selective and Orally Bioavailable Class Of Thrombin Inhibitors Incorporating Aminopyridyl Moieties in the P1 Position. J. Med. Chem. 1997, 40, 3726-3733.
-
(1997)
J. Med. Chem.
, vol.40
, pp. 3726-3733
-
-
Feng, D.-M.1
Gardell, S.J.2
Lewis, S.D.3
Bock, M.G.4
Chen, Z.5
Freidinger, R.M.6
Naylor-Olsen, A.M.7
Ramjit, H.G.8
Woltmann, R.9
Baskin, E.P.10
Lynch, J.J.11
Lucas, R.12
Shafer, J.A.13
Dancheck, K.B.14
Chen, I.-W.15
Mao, S.-S.16
Krueger, J.A.17
Hare, T.R.18
Mulichak, A.M.19
Vacca, J.P.20
more..
-
13
-
-
18344417195
-
L-373,890, An Achiral, Noncovalent, Subnanomolar Thrombin Inhibitor
-
Sanderson, P. E. J.; Dyer, D. L.; Naylor-Olsen, A. M.; Vacca, J. P.; Gardell, S. J.; Lewis, S. D.; Lucas, B. J.; Lyle, E. A.; Lynch, J. J.; Mulichak, A. M. L-373,890, An Achiral, Noncovalent, Subnanomolar Thrombin Inhibitor. Bioorg. Med. Chem. Lett. 1997, 7, 1497-1500.
-
(1997)
Bioorg. Med. Chem. Lett.
, vol.7
, pp. 1497-1500
-
-
Sanderson, P.E.J.1
Dyer, D.L.2
Naylor-Olsen, A.M.3
Vacca, J.P.4
Gardell, S.J.5
Lewis, S.D.6
Lucas, B.J.7
Lyle, E.A.8
Lynch, J.J.9
Mulichak, A.M.10
-
14
-
-
15144357557
-
-
Int. Pat. Appl. WO 97/40024, Oct 30
-
Sanderson, P. E. J.; Lyle, T. A.; Dorsey, B. D.; Varsalona, R. J. Pyrazinone Thrombin Inhibitors. Int. Pat. Appl. WO 97/40024, Oct 30, 1997.
-
(1997)
Pyrazinone Thrombin Inhibitors
-
-
Sanderson, P.E.J.1
Lyle, T.A.2
Dorsey, B.D.3
Varsalona, R.J.4
-
15
-
-
0031001455
-
Design and Synthesis of a Novel Class of Thrombin Inhibitors Incorporating Heterocyclic Dipeptide Surrogates
-
For an alternative synthesis of this intermediate, see: Tamura, S. Y.; Semple, J. E.; Reiner, J. E.; Goldman, E. A.; Brunck, T. K.; Lim-Wilby, M. S.; Carpenter, S. H.; Rote, W. E.; Oldeshulte, G. L.; Richard, B. M.; Nutt, R. F.; Ripka, W. C. Design and Synthesis of a Novel Class of Thrombin Inhibitors Incorporating Heterocyclic Dipeptide Surrogates. Bioorg. Med. Chem. Lett. 1997, 7, 1543-1548.
-
(1997)
Bioorg. Med. Chem. Lett.
, vol.7
, pp. 1543-1548
-
-
Tamura, S.Y.1
Semple, J.E.2
Reiner, J.E.3
Goldman, E.A.4
Brunck, T.K.5
Lim-Wilby, M.S.6
Carpenter, S.H.7
Rote, W.E.8
Oldeshulte, G.L.9
Richard, B.M.10
Nutt, R.F.11
Ripka, W.C.12
-
16
-
-
0021024677
-
A New Sythesis of Substituted 2(1H)-Pyrazinones
-
Vekemans, J.; Pollers-Wieers, C.; Hoornaert, G. A New Sythesis of Substituted 2(1H)-Pyrazinones. J. Heterocycl. Chem. 1983, 20, 919-923.
-
(1983)
J. Heterocycl. Chem.
, vol.20
, pp. 919-923
-
-
Vekemans, J.1
Pollers-Wieers, C.2
Hoornaert, G.3
-
17
-
-
2542433188
-
A Greatly Improved Procedure for Ruthenium Tetraoxide Catalyzed Oxidations of Organic Compounds
-
Carlsen, P. H. J.; Katsuki, T.; Martin, V. S.; Sharpless, K. B. A Greatly Improved Procedure for Ruthenium Tetraoxide Catalyzed Oxidations of Organic Compounds. J. Org. Chem. 1981, 46, 3936-3938.
-
(1981)
J. Org. Chem.
, vol.46
, pp. 3936-3938
-
-
Carlsen, P.H.J.1
Katsuki, T.2
Martin, V.S.3
Sharpless, K.B.4
-
18
-
-
0026803118
-
Synthesis of α-Aminonitriles by Self-catalyzed, Stoichiometric Reaction of Primary Amines, Aldehydes, and Trimethylsilyl Cyanide
-
Leblanc, J.-P.; Gibson, H. W. Synthesis of α-Aminonitriles by Self-catalyzed, Stoichiometric Reaction of Primary Amines, Aldehydes, and Trimethylsilyl Cyanide, Tetrahedron Lett. 1992, 33, 6295-6298.
-
(1992)
Tetrahedron Lett.
, vol.33
, pp. 6295-6298
-
-
Leblanc, J.-P.1
Gibson, H.W.2
-
20
-
-
0025614358
-
Rat Model of Arterial Thrombosis Induced by Ferric Chloride
-
Kurz, K. D.; Main, B. W.; Sandusky, G. E. Rat Model of Arterial Thrombosis Induced by Ferric Chloride. Thromb. Res. 1990, 60, 269-280. Lewis, S. D.; Ng, A. S.; Lyle, E. A.; Mellott, M. J.; Appleby, S. D.; Brady, S. F.; Stauffer, K. J.; Sisko, J. T.; Mao, S.-S.; Veber, D. F.; Nutt, R. F.; Lynch, J. J., Jr.; Cook, J. J.; Gardell, S. J.; Shafer, J. A. Inhibition of Thrombin by Peptides Containing Lysyl-α-Keto Carbonyl Derivatives. Thromb. Haemost. 1995, 74, 1107-1112.
-
(1990)
Thromb. Res.
, vol.60
, pp. 269-280
-
-
Kurz, K.D.1
Main, B.W.2
Sandusky, G.E.3
-
21
-
-
0028824368
-
Inhibition of Thrombin by Peptides Containing Lysyl-α-Keto Carbonyl Derivatives
-
Kurz, K. D.; Main, B. W.; Sandusky, G. E. Rat Model of Arterial Thrombosis Induced by Ferric Chloride. Thromb. Res. 1990, 60, 269-280. Lewis, S. D.; Ng, A. S.; Lyle, E. A.; Mellott, M. J.; Appleby, S. D.; Brady, S. F.; Stauffer, K. J.; Sisko, J. T.; Mao, S.-S.; Veber, D. F.; Nutt, R. F.; Lynch, J. J., Jr.; Cook, J. J.; Gardell, S. J.; Shafer, J. A. Inhibition of Thrombin by Peptides Containing Lysyl-α-Keto Carbonyl Derivatives. Thromb. Haemost. 1995, 74, 1107-1112.
-
(1995)
Thromb. Haemost.
, vol.74
, pp. 1107-1112
-
-
Lewis, S.D.1
Ng, A.S.2
Lyle, E.A.3
Mellott, M.J.4
Appleby, S.D.5
Brady, S.F.6
Stauffer, K.J.7
Sisko, J.T.8
Mao, S.-S.9
Veber, D.F.10
Nutt, R.F.11
Lynch Jr., J.J.12
Cook, J.J.13
Gardell, S.J.14
Shafer, J.A.15
|