-
1
-
-
60249101860
-
Emergence of new oral antithrombotics: A critical appraisal of their clinical potential
-
Lassen, M. R.; Laux, V. Emergence of new oral antithrombotics: a critical appraisal of their clinical potential Vasc. Health Risk Manage. 2008, 4 (6) 1373-1386
-
(2008)
Vasc. Health Risk Manage.
, vol.4
, Issue.6
, pp. 1373-1386
-
-
Lassen, M.R.1
Laux, V.2
-
2
-
-
78650792758
-
Factor Xa and thrombin as targets for new oral anticoagulants
-
Weitz, J. I. Factor Xa and thrombin as targets for new oral anticoagulants Thromb. Res. 2011, 127 (2) S5-S12
-
(2011)
Thromb. Res.
, vol.127
, Issue.2
-
-
Weitz, J.I.1
-
3
-
-
79955665055
-
Oral, direct thrombin and factor Xa inhibitors: The replacement for warfarin, leeches, and pig intestines
-
Straub, A.; Roehrig, S.; Hillisch, A. Oral, direct thrombin and factor Xa inhibitors: the replacement for warfarin, leeches, and pig intestines Angew. Chem., Int. Ed. 2011, 50, 4574-4590
-
(2011)
Angew. Chem., Int. Ed.
, vol.50
, pp. 4574-4590
-
-
Straub, A.1
Roehrig, S.2
Hillisch, A.3
-
4
-
-
0037171819
-
Structure-based design of novel potent nonpeptide thrombin inhibitors
-
Hauel, N. H.; Nar, H.; Priepke, H.; Ries, U.; Stassen, J. M.; Wienen, W. Structure-based design of novel potent nonpeptide thrombin inhibitors J. Med. Chem. 2002, 45, 1757-1766
-
(2002)
J. Med. Chem.
, vol.45
, pp. 1757-1766
-
-
Hauel, N.H.1
Nar, H.2
Priepke, H.3
Ries, U.4
Stassen, J.M.5
Wienen, W.6
-
5
-
-
34548335207
-
Drug evaluation: Dabigatran etexilate, a thrombin inhibitor for the prevention of venous thromboembolism and stroke
-
Ieko, M. Drug evaluation: dabigatran etexilate, a thrombin inhibitor for the prevention of venous thromboembolism and stroke Curr. Opin. Invest. Drugs 2007, 8 (9) 758-768
-
(2007)
Curr. Opin. Invest. Drugs
, vol.8
, Issue.9
, pp. 758-768
-
-
Ieko, M.1
-
6
-
-
77953168824
-
Dabigatran etexilate - A novel, reversible, oral direct thrombin inhibitor: Interpretation of coagulation assays and reversal of anticoagulant activity
-
Van Ryn, J.; Stangier, J.; Haertter, S.; Liesenfeld, K. H.; Wienen, W.; Feuring, M. Dabigatran etexilate-a novel, reversible, oral direct thrombin inhibitor: interpretation of coagulation assays and reversal of anticoagulant activity Thromb. Haemostasis 2010, 103, 1116-1127
-
(2010)
Thromb. Haemostasis
, vol.103
, pp. 1116-1127
-
-
Van Ryn, J.1
Stangier, J.2
Haertter, S.3
Liesenfeld, K.H.4
Wienen, W.5
Feuring, M.6
-
7
-
-
79954456496
-
Dabigatran etexilate: A new oral thrombin inhibitor
-
Hankey, G. J.; Eikelboom, J. W. Dabigatran etexilate: a new oral thrombin inhibitor Circulation 2011, 123, 1436-1450
-
(2011)
Circulation
, vol.123
, pp. 1436-1450
-
-
Hankey, G.J.1
Eikelboom, J.W.2
-
8
-
-
78650827771
-
The discovery and development of rivaroxaban, an oral, direct factor Xa inhibitor
-
Perzborn, E.; Roehring, S.; Straub, A.; Kubitza, D.; Misselwitz, F. The discovery and development of rivaroxaban, an oral, direct factor Xa inhibitor Nat. Rev. Drug Discovery 2011, 10, 61-75
-
(2011)
Nat. Rev. Drug Discovery
, vol.10
, pp. 61-75
-
-
Perzborn, E.1
Roehring, S.2
Straub, A.3
Kubitza, D.4
Misselwitz, F.5
-
9
-
-
77949483011
-
Entering the era of non-basic P1 site groups: Discovery of Xarelto (rivaroxaban)
-
Straub, A.; Roehrig, S.; Hillisch, A. Entering the era of non-basic P1 site groups: discovery of Xarelto (rivaroxaban) Curr. Top. Med. Chem. 2010, 10, 257-269
-
(2010)
Curr. Top. Med. Chem.
, vol.10
, pp. 257-269
-
-
Straub, A.1
Roehrig, S.2
Hillisch, A.3
-
10
-
-
79952836414
-
The discovery and development of rivaroxaban
-
Misselwitz, F.; Berkowitz, S. D.; Perzborn, E. The discovery and development of rivaroxaban Ann. N.Y. Acad. Sci. 2011, 1222, 64-75
-
(2011)
Ann. N.Y. Acad. Sci.
, vol.1222
, pp. 64-75
-
-
Misselwitz, F.1
Berkowitz, S.D.2
Perzborn, E.3
-
11
-
-
49849099533
-
DU-176b, a potent and orally active factor Xa inhibitor: In vitro and in vivo pharmacological profiles
-
Furugohri, T.; Isobe, K.; Honda, Y.; Kamisato-Matsumoto, C.; Sugiyama, N.; Nagahara, T.; Morishima, Y.; Shibano, T. DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles J. Thromb. Haemostasis 2008, 6, 1542-1549
-
(2008)
J. Thromb. Haemostasis
, vol.6
, pp. 1542-1549
-
-
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
-
12
-
-
35848929515
-
Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)- 4,5,6,7-tetrahydro-1 H -pyrazolo[3,4- c ]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa
-
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.; Lam, P. Y. S. Discovery of 1-(4-methoxyphenyl)-7- oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1 H -pyrazolo[3,4- c ]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa J. Med. Chem. 2007, 50, 5339-5356
-
(2007)
J. Med. Chem.
, vol.50
, pp. 5339-5356
-
-
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
-
13
-
-
42149172523
-
Apixaban, an oral, direct and highly selective factor Xa inhibitor: In vitro, antithrombotic and antihemostatic studies
-
Wong, P. C.; Crain, X. B.; Xin, B.; Wexler, R. R.; Lam, P. Y. S.; Pinto, D. J.; Luettgen, J. M.; Knabb, R. M. Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies J. Thromb. Haemostasis 2008, 6, 820-829
-
(2008)
J. Thromb. Haemostasis
, vol.6
, pp. 820-829
-
-
Wong, P.C.1
Crain, X.B.2
Xin, B.3
Wexler, R.R.4
Lam, P.Y.S.5
Pinto, D.J.6
Luettgen, J.M.7
Knabb, R.M.8
-
14
-
-
0035016364
-
SR123781A, a synthetic heparin mimetic
-
Herbert, J.-M.; Herault, J.-P.; Bernat, A.; Savi, P.; Schaeffer, P.; Driguez, P.-A.; Duchaussoy, P.; Petitou, M. SR123781A, a synthetic heparin mimetic Thromb. Haemostasis 2001, 85, 852-860
-
(2001)
Thromb. Haemostasis
, vol.85
, pp. 852-860
-
-
Herbert, J.-M.1
Herault, J.-P.2
Bernat, A.3
Savi, P.4
Schaeffer, P.5
Driguez, P.-A.6
Duchaussoy, P.7
Petitou, M.8
-
15
-
-
0032538777
-
First synthetic carbohydrates with the full anticoagulant properties of heparin
-
Petitou, M.; Duchaussoy, P.; Driguez, P.-A.; Jaurand, G.; Hérault, J.-P.; Lormeau, J.-C.; van Boeckel, C. A. A.; Herbert, J.-M. First synthetic carbohydrates with the full anticoagulant properties of heparin Angew. Chem., Int. Ed. 1998, 37 (21) 3009-3014
-
(1998)
Angew. Chem., Int. Ed.
, vol.37
, Issue.21
, pp. 3009-3014
-
-
Petitou, M.1
Duchaussoy, P.2
Driguez, P.-A.3
Jaurand, G.4
Hérault, J.-P.5
Lormeau, J.-C.6
Van Boeckel, C.A.A.7
Herbert, J.-M.8
-
16
-
-
0344938369
-
Synthesis of thrombin-inhibiting heparin mimetics without side effects
-
Petitou, M.; Hérault, J.-P.; Bernat, A.; Driguez, P.-A.; Duchaussoy, P.; Lormeau, J.-C.; Herbert, J.-M. Synthesis of thrombin-inhibiting heparin mimetics without side effects Nature 1999, 398, 417-422
-
(1999)
Nature
, vol.398
, pp. 417-422
-
-
Petitou, M.1
Hérault, J.-P.2
Bernat, A.3
Driguez, P.-A.4
Duchaussoy, P.5
Lormeau, J.-C.6
Herbert, J.-M.7
-
17
-
-
0033583519
-
New synthetic heparin mimetics able to inhibit thrombin and factor Xa
-
Petitou, M.; Duchaussoy, P.; Driguez, P.-A.; Hérault, J.-P.; Lormeau, J.-C.; Herbert, J.-M. New synthetic heparin mimetics able to inhibit thrombin and factor Xa Bioorg. Med. Chem. Lett. 1999, 9 (8) 1155-1160
-
(1999)
Bioorg. Med. Chem. Lett.
, vol.9
, Issue.8
, pp. 1155-1160
-
-
Petitou, M.1
Duchaussoy, P.2
Driguez, P.-A.3
Hérault, J.-P.4
Lormeau, J.-C.5
Herbert, J.-M.6
-
18
-
-
4344590703
-
Structure of the antithrombin-thrombin-heparin ternary complex reveals the antithrombotic mechanism of heparin
-
Li, W.; Johnson, D. J. D.; Esmon, C. T.; Huntington, J. A. Structure of the antithrombin-thrombin-heparin ternary complex reveals the antithrombotic mechanism of heparin Nat. Struct. Mol. Biol. 2004, 11, 857-862
-
(2004)
Nat. Struct. Mol. Biol.
, vol.11
, pp. 857-862
-
-
Li, W.1
Johnson, D.J.D.2
Esmon, C.T.3
Huntington, J.A.4
-
19
-
-
19744372264
-
Synthetic heparin derivatives as new anticoagulant drugs
-
De Kort, M.; Buijsmain, R. C.; Van Boeckel, A. A. Synthetic heparin derivatives as new anticoagulant drugs Drug Discovery Today 2005, 10, 769-779
-
(2005)
Drug Discovery Today
, vol.10
, pp. 769-779
-
-
De Kort, M.1
Buijsmain, R.C.2
Van Boeckel, A.A.3
-
20
-
-
70449598272
-
The long way to a new pentasaccharide-based neutralisable anticoagulant with an unprecedented pharmacological profile
-
Petitou, M.; Nancy-Porteboi, V.; Dubreucq, G.; Motte, V.; Meuleman, D.; De Kort, M.; Van Boeckel, C. A. A.; Vogel, G. M. T.; Wisse, J. A. J. The long way to a new pentasaccharide-based neutralisable anticoagulant with an unprecedented pharmacological profile Thromb. Haemostasis 2009, 102, 804-810
-
(2009)
Thromb. Haemostasis
, vol.102
, pp. 804-810
-
-
Petitou, M.1
Nancy-Porteboi, V.2
Dubreucq, G.3
Motte, V.4
Meuleman, D.5
De Kort, M.6
Van Boeckel, C.A.A.7
Vogel, G.M.T.8
Wisse, J.A.J.9
-
21
-
-
0035151738
-
Structural basis for inhibition promiscuity of dual specific thrombin and factor Xa blood coagulation inhibitors
-
Nar, H.; Bauer, M.; Schmid, A.; Stassen, J. M.; Wienen, W.; Priepke, H. W.; Kauffmann, I. K.; Ries, U. J.; Hauel, N. H. Structural basis for inhibition promiscuity of dual specific thrombin and factor Xa blood coagulation inhibitors Structure 2001, 9, 29-37
-
(2001)
Structure
, vol.9
, pp. 29-37
-
-
Nar, H.1
Bauer, M.2
Schmid, A.3
Stassen, J.M.4
Wienen, W.5
Priepke, H.W.6
Kauffmann, I.K.7
Ries, U.J.8
Hauel, N.H.9
-
22
-
-
0038004032
-
Heterocyclic thrombin inhibitors. Part 2: Quinoxalinone derivatives as novel, potent antithrombotic agents
-
Ries, U. J.; Priepke, H. W.; Hauel, N. H.; Handschuh, S.; Mihm, G.; Stassen, J. M.; Wienen, W.; Nar, H. Heterocyclic thrombin inhibitors. Part 2: Quinoxalinone derivatives as novel, potent antithrombotic agents Bioorg. Med. Chem. Lett. 2003, 13, 2297-2302
-
(2003)
Bioorg. Med. Chem. Lett.
, vol.13
, pp. 2297-2302
-
-
Ries, U.J.1
Priepke, H.W.2
Hauel, N.H.3
Handschuh, S.4
Mihm, G.5
Stassen, J.M.6
Wienen, W.7
Nar, H.8
-
23
-
-
33745246311
-
Pharmacokinetics and pharmacodynamics of BIBT 986, a novel small molecule dual inhibitor of thrombin and factor Xa
-
Graefe-Mody, E. U.; Schühly, U.; Rathgen, K.; Stähle, H.; Leitner, J. M.; Jilma, B. Pharmacokinetics and pharmacodynamics of BIBT 986, a novel small molecule dual inhibitor of thrombin and factor Xa J. Thromb. Haemostasis 2006, 4, 1502-1509
-
(2006)
J. Thromb. Haemostasis
, vol.4
, pp. 1502-1509
-
-
Graefe-Mody, E.U.1
Schühly, U.2
Rathgen, K.3
Stähle, H.4
Leitner, J.M.5
Jilma, B.6
-
24
-
-
24344470615
-
Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization
-
Deng, J. Z.; McMasters, D. R.; Rabbat, P. M.; Williams, P. D.; Coburn, C. A.; Yan, Y.; Kuo, L. C.; Lewis, S. D.; Lucas, B. J.; Krueger, J. A.; Strulovici, B.; Vacca, J. P.; Lyle, T. A.; Burgey, C. S. Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization Bioorg. Med. Chem. Lett. 2005, 15, 4411-4416
-
(2005)
Bioorg. Med. Chem. Lett.
, vol.15
, pp. 4411-4416
-
-
Deng, J.Z.1
McMasters, D.R.2
Rabbat, P.M.3
Williams, P.D.4
Coburn, C.A.5
Yan, Y.6
Kuo, L.C.7
Lewis, S.D.8
Lucas, B.J.9
Krueger, J.A.10
Strulovici, B.11
Vacca, J.P.12
Lyle, T.A.13
Burgey, C.S.14
-
25
-
-
34249303110
-
From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3
-
Dönnecke, D.; Schweinitz, A.; Stürzebecher, A.; Steinmetzer, P.; Schuster, M.; Stürzebecher, U.; Nicklisch, S.; Stürzebecher, J.; Steinmetzer, T. From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3 Bioorg. Med. Chem. Lett. 2007, 17, 3322-3329
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 3322-3329
-
-
Dönnecke, D.1
Schweinitz, A.2
Stürzebecher, A.3
Steinmetzer, P.4
Schuster, M.5
Stürzebecher, U.6
Nicklisch, S.7
Stürzebecher, J.8
Steinmetzer, T.9
-
26
-
-
34247333018
-
Selective and dual action orally active inhibitors of thrombin and factor Xa
-
Young, R. J.; Brown, D.; Burns-Kurtis, C. L.; Chan, C.; Convery, M. A.; Hubbard, J. A.; Kelly, H. A.; Pateman, A. J.; Patikis, A.; Senger, S.; Shah, G. P.; Toomey, J. R.; Watson, N. S.; Zhou, P. Selective and dual action orally active inhibitors of thrombin and factor Xa Bioorg. Med. Chem. Lett. 2007, 17, 2927-2930
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 2927-2930
-
-
Young, R.J.1
Brown, D.2
Burns-Kurtis, C.L.3
Chan, C.4
Convery, M.A.5
Hubbard, J.A.6
Kelly, H.A.7
Pateman, A.J.8
Patikis, A.9
Senger, S.10
Shah, G.P.11
Toomey, J.R.12
Watson, N.S.13
Zhou, P.14
-
27
-
-
33747665628
-
Exploration of potential prodrugs of RWJ-445167, an oxyguanidine based dual inhibitor of thrombin and factor Xa
-
Maryanoff, B. E.; McComsey, D. F.; Costanzo, M. J.; Yabut, S. C.; Lu, T.; Player, M. R.; Giardino, E. C.; Damiano, B. P. Exploration of potential prodrugs of RWJ-445167, an oxyguanidine based dual inhibitor of thrombin and factor Xa Chem. Biol. Drug Des. 2006, 68, 29-36
-
(2006)
Chem. Biol. Drug Des.
, vol.68
, pp. 29-36
-
-
Maryanoff, B.E.1
McComsey, D.F.2
Costanzo, M.J.3
Yabut, S.C.4
Lu, T.5
Player, M.R.6
Giardino, E.C.7
Damiano, B.P.8
-
28
-
-
76449108473
-
Cooperative antithrombotic effect from the simultaneous inhibition of thrombin and factor Xa
-
Giardino, E. C.; Haertlein, B. J.; De Garavilla, L.; Costanzo, M. J.; Damiano, B. P.; Andrade-Gordon, P.; Maryanoff, B. E. Cooperative antithrombotic effect from the simultaneous inhibition of thrombin and factor Xa Blood Coagulation Fibrinolysis 2010, 21, 128-134
-
(2010)
Blood Coagulation Fibrinolysis
, vol.21
, pp. 128-134
-
-
Giardino, E.C.1
Haertlein, B.J.2
De Garavilla, L.3
Costanzo, M.J.4
Damiano, B.P.5
Andrade-Gordon, P.6
Maryanoff, B.E.7
-
29
-
-
12144289000
-
SSR182289A, a selective and potent orally active thrombin inhibitor
-
Altenburger, J.-M.; Lassalle, G. Y.; Matrougui, M.; Galtier, D.; Jetha, J.-C.; Bocskei, Z.; Berry, C. N.; Lunven, C.; Lorrain, J.; Herault, J.-P.; Schaeffer, P.; O'Connor, S. E.; Herbert, J.-M. SSR182289A, a selective and potent orally active thrombin inhibitor Bioorg. Med. Chem. 2004, 12, 1713-1730
-
(2004)
Bioorg. Med. Chem.
, vol.12
, pp. 1713-1730
-
-
Altenburger, J.-M.1
Lassalle, G.Y.2
Matrougui, M.3
Galtier, D.4
Jetha, J.-C.5
Bocskei, Z.6
Berry, C.N.7
Lunven, C.8
Lorrain, J.9
Herault, J.-P.10
Schaeffer, P.11
O'Connor, S.E.12
Herbert, J.-M.13
-
30
-
-
0036896159
-
SSR182289A, a novel, orally active thrombin inhibitor: In vitro profile and ex vivo anticoagulant activity
-
Berry, C. N.; Lassalle, G.; Lunven, C.; Altenburger, J.-M.; Guilbert, F.; Lalé, A.; Hérault, J.-P.; Lecoffre, C.; Pfersdorff, C.; Herbert, J.-M.; O'Connor, S. E. SSR182289A, a novel, orally active thrombin inhibitor: in vitro profile and ex vivo anticoagulant activity J. Pharmacol. Exp. Ther. 2002, 303, 1189-1198
-
(2002)
J. Pharmacol. Exp. Ther.
, vol.303
, pp. 1189-1198
-
-
Berry, C.N.1
Lassalle, G.2
Lunven, C.3
Altenburger, J.-M.4
Guilbert, F.5
Lalé, A.6
Hérault, J.-P.7
Lecoffre, C.8
Pfersdorff, C.9
Herbert, J.-M.10
O'Connor, S.E.11
-
31
-
-
0037307985
-
Antithrombotic properties of SSR182289A, a new, orally active thrombin inhibitor
-
Lorrain, J.; Millet, L.; Lechaire, I.; Lochot, S.; Ferrari, P.; Visconte, C.; Sainte-Marie, M.; Lunven, C.; Berry, C. N.; Schaeffer, P.; Herbert, J.-M.; O'Connor, S. E. Antithrombotic properties of SSR182289A, a new, orally active thrombin inhibitor J. Pharmacol. Exp. Ther. 2002, 304, 567-574
-
(2002)
J. Pharmacol. Exp. Ther.
, vol.304
, pp. 567-574
-
-
Lorrain, J.1
Millet, L.2
Lechaire, I.3
Lochot, S.4
Ferrari, P.5
Visconte, C.6
Sainte-Marie, M.7
Lunven, C.8
Berry, C.N.9
Schaeffer, P.10
Herbert, J.-M.11
O'Connor, S.E.12
-
33
-
-
0037468471
-
Molecular structures of human factor Xa complexed with ketopiperazine inhibitors: Preference for a neutral group in the S1 pocket
-
Maignan, S.; Guilloteau, J.-P.; Choi-Sledeski, Y. M.; Becker, M. R.; Ewing, W. R.; Pauls, H. W.; Spada, A. P.; Mikol, V. Molecular structures of human factor Xa complexed with ketopiperazine inhibitors: preference for a neutral group in the S1 pocket J. Med. Chem. 2003, 46, 685-690
-
(2003)
J. Med. Chem.
, vol.46
, pp. 685-690
-
-
Maignan, S.1
Guilloteau, J.-P.2
Choi-Sledeski, Y.M.3
Becker, M.R.4
Ewing, W.R.5
Pauls, H.W.6
Spada, A.P.7
Mikol, V.8
-
34
-
-
0037468474
-
Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand
-
Choi-Sledeski, Y. M.; Kearney, R.; Poli, G.; Pauls, H.; Gardner, C.; Gong, Y.; Becker, M.; Davis, R.; Spada, A.; Liang, G.; Chu, V.; Brown, K.; Collussi, D.; Leadley, R., Jr.; Rebello, S.; Moxey, P.; Morgan, S.; Bentley, R.; Kasiewski, C.; Maignan, S.; Guilloteau, J.-P.; Mikol, V. Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand J. Med. Chem. 2003, 46, 681-684
-
(2003)
J. Med. Chem.
, vol.46
, pp. 681-684
-
-
Choi-Sledeski, Y.M.1
Kearney, R.2
Poli, G.3
Pauls, H.4
Gardner, C.5
Gong, Y.6
Becker, M.7
Davis, R.8
Spada, A.9
Liang, G.10
Chu, V.11
Brown, K.12
Collussi, D.13
Leadley Jr., R.14
Rebello, S.15
Moxey, P.16
Morgan, S.17
Bentley, R.18
Kasiewski, C.19
Maignan, S.20
Guilloteau, J.-P.21
Mikol, V.22
more..
-
35
-
-
70349786321
-
Evidence for C-Cl/C-Br···π Interactions as an Important Contribution to Protein-Ligand Binding Affinity
-
Matter, H.; Nazaré, M.; Güssregen, S.; Will, D. W.; Schreuder, H.; Bauer, A.; Urmann, M.; Ritter, K.; Wagner, M.; Wehner, V. Evidence for C-Cl/C-Br···π Interactions as an Important Contribution to Protein-Ligand Binding Affinity Angew. Chem., Int. Ed. 2009, 48, 2911-2916
-
(2009)
Angew. Chem., Int. Ed.
, vol.48
, pp. 2911-2916
-
-
Matter, H.1
Nazaré, M.2
Güssregen, S.3
Will, D.W.4
Schreuder, H.5
Bauer, A.6
Urmann, M.7
Ritter, K.8
Wagner, M.9
Wehner, V.10
-
36
-
-
24944536065
-
Discovery of the novel antithrombotic agent 5-chloro -N- ({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): An oral, direct factor Xa inhibitor
-
Roehrig, S.; Straub, A.; Pohlmann, J.; Lampe, T.; Pernerstorfer, S.; Schlemmer, K.-H.; Reinemer, P.; Perzborn, E. Discovery of the novel antithrombotic agent 5-chloro -N- ({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl) phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): an oral, direct factor Xa inhibitor J. Med. Chem. 2005, 48, 5900-5908
-
(2005)
J. Med. Chem.
, vol.48
, pp. 5900-5908
-
-
Roehrig, S.1
Straub, A.2
Pohlmann, J.3
Lampe, T.4
Pernerstorfer, S.5
Schlemmer, K.-H.6
Reinemer, P.7
Perzborn, E.8
-
37
-
-
0141645562
-
Highly functionalized organomagnesium reagents prepared through halogen-metal exchange
-
Knochel, P.; Dohle, W.; Gommermann, N.; Kneisel, F. F.; Kopp, F.; Korn, T.; Sapountzis, I.; Vu, V. A. Highly functionalized organomagnesium reagents prepared through halogen-metal exchange Angew. Chem., Int. Ed. 2003, 42, 4302-4320
-
(2003)
Angew. Chem., Int. Ed.
, vol.42
, pp. 4302-4320
-
-
Knochel, P.1
Dohle, W.2
Gommermann, N.3
Kneisel, F.F.4
Kopp, F.5
Korn, T.6
Sapountzis, I.7
Vu, V.A.8
-
38
-
-
85022543214
-
Asymmetric syntheses via heterocyclic intermediates; XVII1. Enantioselective synthesis of (R)-α-methyl- S -benzylcysteine methyl ester and (R)-α-methyl- S - T -butylcysteine methyl ester using l -valine as chiral auxiliary reagent
-
Groth, U.; Schöllkopf, U. Asymmetric syntheses via heterocyclic intermediates; XVII1. Enantioselective synthesis of (R)-α-methyl- S -benzylcysteine methyl ester and (R)-α-methyl- S-t -butylcysteine methyl ester using l -valine as chiral auxiliary reagent Synthesis 1983, 1, 37-38
-
(1983)
Synthesis
, vol.1
, pp. 37-38
-
-
Groth, U.1
Schöllkopf, U.2
-
39
-
-
33644973993
-
Inhibitors of blood coagulation factors Xa and IIa synergize to reduce thrombus weight and thrombin generation in vivo and in vitro
-
Gould, W. R.; McClanahan, T. B.; Welch, K. M.; Baxi, S. M.; Saiya-Cork, K.; Chi, L.; Johnson, T. R.; Leadley, R. J. Inhibitors of blood coagulation factors Xa and IIa synergize to reduce thrombus weight and thrombin generation in vivo and in vitro J. Thromb. Haemostasis 2006, 4, 834-841
-
(2006)
J. Thromb. Haemostasis
, vol.4
, pp. 834-841
-
-
Gould, W.R.1
McClanahan, T.B.2
Welch, K.M.3
Baxi, S.M.4
Saiya-Cork, K.5
Chi, L.6
Johnson, T.R.7
Leadley, R.J.8
-
40
-
-
76449108473
-
Cooperative antithrombotic effect from the simultaneous inhibition of thrombin and factor Xa
-
Giardino, E. C.; Haertlein, B. J.; de Garavilla, L.; Costanzo, M. J.; Damiano, B. P.; Andrade-Gordon, P.; Maryanoff, B. E. Cooperative antithrombotic effect from the simultaneous inhibition of thrombin and factor Xa Blood Coagulation Fibrinolysis 2010, 21, 128-134
-
(2010)
Blood Coagulation Fibrinolysis
, vol.21
, pp. 128-134
-
-
Giardino, E.C.1
Haertlein, B.J.2
De Garavilla, L.3
Costanzo, M.J.4
Damiano, B.P.5
Andrade-Gordon, P.6
Maryanoff, B.E.7
-
41
-
-
84890447817
-
-
WO2009103440.
-
Follmann, M.; Wehner, V.; Meneyrol, J.; Altenburger, J.-M.; Petit, F.; Lassalle, G.; Herault, J. P. Preparation of Chlorothiophene-amides as Inhibitors of Coagulation Factors Xa and Thrombin. WO2009103440, 2009.
-
(2009)
Preparation of Chlorothiophene-amides As Inhibitors of Coagulation Factors Xa and Thrombin
-
-
Follmann, M.1
Wehner, V.2
Meneyrol, J.3
Altenburger, J.-M.4
Petit, F.5
Lassalle, G.6
Herault, J.P.7
-
42
-
-
84890447817
-
-
WO2009103439.
-
Follmann, M.; Wehner, V.; Altenburger, J.-M.; Lassalle, G.; Herault, J.-P.; Preparation of Chlorothiophene-isoxazoles as Inhibitors of Coagulation Factors Xa and Thrombin. WO2009103439, 2009.
-
(2009)
Preparation of Chlorothiophene-isoxazoles As Inhibitors of Coagulation Factors Xa and Thrombin
-
-
Follmann, M.1
Wehner, V.2
Altenburger, J.-M.3
Lassalle, G.4
Herault, J.-P.5
-
43
-
-
0001158361
-
Organotin-mediated selective desulfurization: Tri- n -butyltin hydride reduction of unsymmetric sulfides
-
Gutierrez, C. G.; Leo, R.; Summerhays, L. R. Organotin-mediated selective desulfurization: tri- n -butyltin hydride reduction of unsymmetric sulfides J. Org. Chem. 1984, 49 (26) 5206-5213
-
(1984)
J. Org. Chem.
, vol.49
, Issue.26
, pp. 5206-5213
-
-
Gutierrez, C.G.1
Leo, R.2
Summerhays, L.R.3
-
44
-
-
22244460783
-
Probing the subpockets of factor Xa reveals two binding modes for inhibitors based on a 2-carboxyindole scaffold: A study combining structure-activity relationship and X-ray crystallography
-
Nazaré, M.; Will, D. W.; Matter, H.; Schreuder, H.; Ritter, K.; Urmann, M.; Essrich, M.; Bauer, A.; Wagner, M.; Czech, J.; Lorenz, M.; Laux, V.; Wehner, V. Probing the subpockets of factor Xa reveals two binding modes for inhibitors based on a 2-carboxyindole scaffold: a study combining structure-activity relationship and X-ray crystallography J. Med. Chem. 2005, 48, 4511-4525
-
(2005)
J. Med. Chem.
, vol.48
, pp. 4511-4525
-
-
Nazaré, M.1
Will, D.W.2
Matter, H.3
Schreuder, H.4
Ritter, K.5
Urmann, M.6
Essrich, M.7
Bauer, A.8
Wagner, M.9
Czech, J.10
Lorenz, M.11
Laux, V.12
Wehner, V.13
-
45
-
-
3142682251
-
Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents
-
Nazaré, M.; Essrich, M.; Will, D. H.; Matter, H.; Ritter, K.; Urmann, M.; Bauer, A.; Schreuder, H.; Dudda, A.; Czech, J.; Lorenz, M.; Laux, V.; Wehner, V. Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents Bioorg. Med. Chem. Lett. 2004, 14, 4191-4195
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 4191-4195
-
-
Nazaré, M.1
Essrich, M.2
Will, D.H.3
Matter, H.4
Ritter, K.5
Urmann, M.6
Bauer, A.7
Schreuder, H.8
Dudda, A.9
Czech, J.10
Lorenz, M.11
Laux, V.12
Wehner, V.13
-
46
-
-
2142705744
-
A facile one-pot synthesis of alkyl aryl sulfides from aryl bromides
-
Ham, J.; Yang, I.; Kang, H. A facile one-pot synthesis of alkyl aryl sulfides from aryl bromides J. Org. Chem. 2004, 69, 3236-3239
-
(2004)
J. Org. Chem.
, vol.69
, pp. 3236-3239
-
-
Ham, J.1
Yang, I.2
Kang, H.3
-
47
-
-
0015861774
-
Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction
-
Cheng, Y.; Prusoff, W. H. Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction Biochem. Pharmacol. 1973, 22, 3099-3108
-
(1973)
Biochem. Pharmacol.
, vol.22
, pp. 3099-3108
-
-
Cheng, Y.1
Prusoff, W.H.2
-
48
-
-
0003518480
-
-
John Wiley & Sons: New York - 125
-
Segal, I. H. Enzyme Kinetics; John Wiley & Sons: New York, 1975; pp 100-125.
-
(1975)
Enzyme Kinetics
, pp. 100
-
-
Segal, I.H.1
-
49
-
-
0029085314
-
Thrombin generation in plasma: Its assessment via the endogenous thrombin potential
-
Hemker, H. C.; Beguin, S. Thrombin generation in plasma: its assessment via the endogenous thrombin potential Thromb. Haemostasis 1995, 74, 134-138
-
(1995)
Thromb. Haemostasis
, vol.74
, pp. 134-138
-
-
Hemker, H.C.1
Beguin, S.2
-
50
-
-
0034537312
-
Monitoring hypocoagulant conditions in rat plasma: Factors determining the endogenous thrombin potential of tissue factor-activated plasma
-
Nieuwenhuys, C. M.; Feijge, M. A.; Beguin, S.; Heemskerk, J. W. Monitoring hypocoagulant conditions in rat plasma: factors determining the endogenous thrombin potential of tissue factor-activated plasma Thromb. Haemostasis 2000, 84, 1045-1051
-
(2000)
Thromb. Haemostasis
, vol.84
, pp. 1045-1051
-
-
Nieuwenhuys, C.M.1
Feijge, M.A.2
Beguin, S.3
Heemskerk, J.W.4
-
51
-
-
0037142372
-
Design and quantitative structure-activity relationship of 3-amidinobenzyl-1 H -indole-2-carboxamides as potent, nonchiral, and selective inhibitors of blood coagulation factor Xa
-
Matter, H.; Defossa, E.; Heinelt, U.; Blohm, P.-M.; Schneider, D.; Mueller, A.; Herok, S.; Schreuder, H.; Liesum, A.; Brachvogel, V.; Loenze, P.; Walser, A.; Al-Obeidi, F.; Wildgoose, P. Design and quantitative structure-activity relationship of 3-amidinobenzyl-1 H -indole-2-carboxamides as potent, nonchiral, and selective inhibitors of blood coagulation factor Xa J. Med. Chem. 2002, 45, 2749-2769
-
(2002)
J. Med. Chem.
, vol.45
, pp. 2749-2769
-
-
Matter, H.1
Defossa, E.2
Heinelt, U.3
Blohm, P.-M.4
Schneider, D.5
Mueller, A.6
Herok, S.7
Schreuder, H.8
Liesum, A.9
Brachvogel, V.10
Loenze, P.11
Walser, A.12
Al-Obeidi, F.13
Wildgoose, P.14
-
53
-
-
0031059866
-
Processing of X-ray Diffraction Data Collected in Oscillation Mode
-
Carter, C.W. Jr. Sweet, R. M. Methods in Enzymology, Vol. Academic Press: New York - 326
-
Otwinowski, Z.; Minor, W. Processing of X-ray Diffraction Data Collected in Oscillation Mode. In Macromolecular Crystallography. Part A; Carter, C.W., Jr.; Sweet, R. M., Eds.; Methods in Enzymology, Vol. 276; Academic Press: New York, 1997; pp 307-326.
-
(1997)
Macromolecular Crystallography. Part A
, vol.276
, pp. 307
-
-
Otwinowski, Z.1
Minor, W.2
-
54
-
-
13244281317
-
Coot: Model-building tools for molecular graphics
-
Emsley, P.; Cowtan, K. Coot: model-building tools for molecular graphics Acta Crystallogr. 2004, D60, 2126-2132
-
(2004)
Acta Crystallogr.
, vol.60
, pp. 2126-2132
-
-
Emsley, P.1
Cowtan, K.2
-
55
-
-
84858642798
-
-
version 2.11.2; Global Phasing Ltd. Cambridge, U.K.
-
Bricogne, G.; Blanc, E.; Brandl, M.; Flensburg, C.; Keller, P.; Paciorek, W.; Roversi, P.; Sharff, A.; Smart, O. S.; Vonrhein, C.; Womack, T. O. BUSTER, version 2.11.2; Global Phasing Ltd.: Cambridge, U.K., 2011.
-
(2011)
BUSTER
-
-
Bricogne, G.1
Blanc, E.2
Brandl, M.3
Flensburg, C.4
Keller, P.5
Paciorek, W.6
Roversi, P.7
Sharff, A.8
Smart, O.S.9
Vonrhein, C.10
Womack, T.O.11
-
56
-
-
85046526624
-
Evaluation of single-crystal X-ray diffraction data from a position sensitive detector
-
Kabsch, W. Evaluation of single-crystal X-ray diffraction data from a position sensitive detector J. Appl. Crystallogr. 1988, 21, 916-924
-
(1988)
J. Appl. Crystallogr.
, vol.21
, pp. 916-924
-
-
Kabsch, W.1
-
57
-
-
0028103275
-
The CCP4 suite: Programs for protein crystallography
-
Collaborative Computational Project, Number 4. - 763
-
Collaborative Computational Project, Number 4. The CCP4 suite: programs for protein crystallography Acta Crystallogr. 1994, D50, 760-763
-
(1994)
Acta Crystallogr.
, vol.50
, pp. 760
-
-
-
58
-
-
3543012707
-
Crystallography & NMR System (CNS), a new software suite for macromolecular structure determination
-
Brunger, A. T.; Adams, P. D.; Clore, G. M.; Gros, P.; Grosse-Kunstleve, R. W.; Jiang, J.-S.; Kuszewski, J.; Nilges, N.; Pannu, N. S.; Read, R. J.; Rice, L. M.; Simonson, T.; Warren, G. L. Crystallography & NMR System (CNS), a new software suite for macromolecular structure determination Acta Crystallogr. 1998, D54, 905-921
-
(1998)
Acta Crystallogr.
, vol.54
, pp. 905-921
-
-
Brunger, A.T.1
Adams, P.D.2
Clore, G.M.3
Gros, P.4
Grosse-Kunstleve, R.W.5
Jiang, J.-S.6
Kuszewski, J.7
Nilges, N.8
Pannu, N.S.9
Read, R.J.10
Rice, L.M.11
Simonson, T.12
Warren, G.L.13
-
59
-
-
7544226311
-
PRODRG - A tool for high-throughput crystallography of protein-ligand complexes
-
Schüttelkopf, A. W.; van Aalten, D. M. F. PRODRG-a tool for high-throughput crystallography of protein-ligand complexes Acta Crystallogr. 2004, D60, 1355-1363
-
(2004)
Acta Crystallogr.
, vol.60
, pp. 1355-1363
-
-
Schüttelkopf, A.W.1
Van Aalten, D.M.F.2
-
60
-
-
0032212015
-
Incorporation of prior phase information strengthen maximum-likelihood structure refinement
-
Pannu, N. J.; Murshudov, G. N.; Dodson, E. J.; Read, R. J. Incorporation of prior phase information strengthen maximum-likelihood structure refinement Acta Crystallogr. 1998, D54, 1285-1294
-
(1998)
Acta Crystallogr.
, vol.54
, pp. 1285-1294
-
-
Pannu, N.J.1
Murshudov, G.N.2
Dodson, E.J.3
Read, R.J.4
|