-
1
-
-
0010359154
-
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors
-
Dallas, TX, March 29-April 2, Abstract 202
-
This work was partially presented at the 215th ACS National Meeting: Quan, M. L. Design and Synthesis of Isoxazoline Derivatives as Factor Xa Inhibitors. 215th ACS National Meeting, Dallas, TX, March 29-April 2, 1998, Abstract 202.
-
(1998)
215th ACS National Meeting
-
-
Quan, M.L.1
-
2
-
-
0026337077
-
The coagulation cascade: Initiation, maintenance and regulation
-
Davre, E. W.; Fujikawa, K.; Kisiel, W. The coagulation cascade: initiation, maintenance and regulation. Biochemistry 1991, 30, 10363-10370.
-
(1991)
Biochemistry
, vol.30
, pp. 10363-10370
-
-
Davre, E.W.1
Fujikawa, K.2
Kisiel, W.3
-
3
-
-
0018729826
-
Optimization of conditions for the catalytic effect of the factor IXa-factor VIII complex: Probable role of the complex in the amplication of blood coagulation
-
Elodi, S.; Varadi, K. Optimization of conditions for the catalytic effect of the factor IXa-factor VIII complex: probable role of the complex in the amplication of blood coagulation. Thromb. Res. 1979, 15, 617-629.
-
(1979)
Thromb. Res.
, vol.15
, pp. 617-629
-
-
Elodi, S.1
Varadi, K.2
-
4
-
-
0030858427
-
Antithrombotic strategies targeting thrombin activities, thrombin receptors and thrombin generation
-
Harker, L. A.; Hanson, S. R.; Kelly, A. B. Antithrombotic Strategies Targeting Thrombin Activities, Thrombin Receptors and Thrombin Generation. Thromb. Haemostasis 1997, 78, 736-741.
-
(1997)
Thromb. Haemostasis
, vol.78
, pp. 736-741
-
-
Harker, L.A.1
Hanson, S.R.2
Kelly, A.B.3
-
5
-
-
0013481920
-
Antithrombotics/serine proteases
-
Bristol, J. A., Ed.; Academic Press: New York
-
Ripka, W. C.; Vlasuk, G. P. Antithrombotics/Serine Proteases. In Annual Reports in Medicinal Chemistry; Bristol, J. A., Ed.; Academic Press: New York, 1997, Vol. 32, pp 71-89.
-
(1997)
Annual Reports in Medicinal Chemistry
, vol.32
, pp. 71-89
-
-
Ripka, W.C.1
Vlasuk, G.P.2
-
6
-
-
0018973964
-
Strategies for anticoagulation with synthetic protease inhibitors. Xa inhibitors versus thrombin inhibitors
-
Tidwell, R. R.; Webster, W. P.; Shaver, S. R.; Geratz, J. D. Strategies for Anticoagulation with Synthetic Protease Inhibitors. Xa Inhibitors Versus Thrombin Inhibitors. Thromb. Res. 1980, 19, 339-349.
-
(1980)
Thromb. Res.
, vol.19
, pp. 339-349
-
-
Tidwell, R.R.1
Webster, W.P.2
Shaver, S.R.3
Geratz, J.D.4
-
7
-
-
0017059735
-
Synthetic inhibitors of serine proteinases XIV. Inhibition of factor Xa by derivatives of benzamidine
-
Stürzebecher, J.; Markwardt, F.; Walsmann, P. Synthetic Inhibitors of Serine Proteinases XIV. Inhibition of Factor Xa by Derivatives of Benzamidine. Thromb. Res. 1976, 9, 637-646.
-
(1976)
Thromb. Res.
, vol.9
, pp. 637-646
-
-
Stürzebecher, J.1
Markwardt, F.2
Walsmann, P.3
-
8
-
-
0018872335
-
Synthetic inhibitors of serine proteinases XXIII. Inhibition of factor Xa by diamidines
-
Stürzebecher, J.; Markwardt, F.; Walsmann, P. Synthetic Inhibitors of Serine Proteinases XXIII. Inhibition of Factor Xa by Diamidines. Thromb. Res. 1980, 17, 545-548.
-
(1980)
Thromb. Res.
, vol.17
, pp. 545-548
-
-
Stürzebecher, J.1
Markwardt, F.2
Walsmann, P.3
-
9
-
-
0028265990
-
Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors
-
Nagahara, T.; Yukoyama, Y.; Inamura, K.; Katakura, S.; Komoriya, S.; Yamaguchi, H.; Hara, T.; Iwamoto, M. Dibasic (amidinoaryl)propanoic Acid Derivatives as Novel Blood Coagulation Factor Xa Inhibitors. J. Med. Chem. 1994, 37, 1200-1207.
-
(1994)
J. Med. Chem.
, vol.37
, pp. 1200-1207
-
-
Nagahara, T.1
Yukoyama, Y.2
Inamura, K.3
Katakura, S.4
Komoriya, S.5
Yamaguchi, H.6
Hara, T.7
Iwamoto, M.8
-
10
-
-
0029038740
-
Design, synthesis and biological activities of orally active coagulation factor Xa inhibitors
-
Nagahara, T.; Yukoyama, Y.; Inamura, K.; Katakura, S.; Komoriya, S.; Yamaguchi, H.; Hara, T.; Iwamoto, M. Design, Synthesis and Biological Activities of Orally Active Coagulation Factor Xa Inhibitors. Eur. J. Med. Chem. 1995, 30, 139s.
-
(1995)
Eur. J. Med. Chem.
, vol.30
-
-
Nagahara, T.1
Yukoyama, Y.2
Inamura, K.3
Katakura, S.4
Komoriya, S.5
Yamaguchi, H.6
Hara, T.7
Iwamoto, M.8
-
11
-
-
0031588348
-
YM-60828, a novel factor Xa inhibitor: Separation of its antithrombotic effects from its prolongation of bleeding time
-
Sato, K.; Kawasaki, T.; Taniuchi, Y.; Hisamichi, N.; Koshio, H.; Matsumoto, Y. YM-60828, a Novel Factor Xa Inhibitor: Separation of its Antithrombotic Effects from its Prolongation of Bleeding Time. Eur. J. Pharmacol. 1997, 339, 141-146.
-
(1997)
Eur. J. Pharmacol.
, vol.339
, pp. 141-146
-
-
Sato, K.1
Kawasaki, T.2
Taniuchi, Y.3
Hisamichi, N.4
Koshio, H.5
Matsumoto, Y.6
-
12
-
-
0031888018
-
Biochemical and pharmacological characterization of YM-60828, a newly synthesized and orally active inhibitor of human factor Xa
-
Taniuchi, Y.; Sakai, Y.; Hisamichi, N.; Kayama, M.; Mano, Y.; Sato, K.; Hirayama, F.; Koshio, H.; Matsumoto, Y.; Kawasaki, T. Biochemical and Pharmacological Characterization of YM-60828, a Newly Synthesized and Orally Active Inhibitor of Human Factor Xa. Thromb. Haemostasis 1998, 79, 543-548.
-
(1998)
Thromb. Haemostasis
, vol.79
, pp. 543-548
-
-
Taniuchi, Y.1
Sakai, Y.2
Hisamichi, N.3
Kayama, M.4
Mano, Y.5
Sato, K.6
Hirayama, F.7
Koshio, H.8
Matsumoto, Y.9
Kawasaki, T.10
-
13
-
-
0031964032
-
Antithrombotic effects of YM-60828, a newly synthesized factor Xa inhibitor, in rat thrombosis model and its effects on bleeding time
-
Sato, K.; Kawasaki, T.; Hisamichi, N.; Taniuchi, Y.; Hirayama, F.; Koshio, H.; Matsumoto, Y. Antithrombotic Effects of YM-60828, a Newly Synthesized Factor Xa Inhibitor, in Rat Thrombosis Model and its Effects on Bleeding Time. Br. J. Pharmacol. 1998, 123, 92-96.
-
(1998)
Br. J. Pharmacol.
, vol.123
, pp. 92-96
-
-
Sato, K.1
Kawasaki, T.2
Hisamichi, N.3
Taniuchi, Y.4
Hirayama, F.5
Koshio, H.6
Matsumoto, Y.7
-
14
-
-
15144344269
-
Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors
-
Maduskuie, T. P., Jr.; McNamara, K. J.; Ru, Y.; Knabb, R. M.; Stouten, P. F. W. Rational Design and Synthesis of Novel, Potent Bis-Phenylamidine Carboxylate Factor Xa Inhibitors. J. Med Chem. 1998, 41, 53-62.
-
(1998)
J. Med Chem.
, vol.41
, pp. 53-62
-
-
Maduskuie T.P., Jr.1
McNamara, K.J.2
Ru, Y.3
Knabb, R.M.4
Stouten, P.F.W.5
-
15
-
-
15444348427
-
Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa
-
At the time this work was carried out, there were no published reports on monobasic FXa inhibitors. Subsequently, the following manuscripts have been published: (a) Klein, S. I.; Czekaj, M.; Gardner, C. J.; Guertin, K. R.; 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. Identification and Initial Structure-Activity Relationships of a Novel Class of Nonpeptide Inhibitors of Blood Coagulation Factor Xa. J. Med. Chem. 1998, 41, 437-450.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 437-450
-
-
Klein, S.I.1
Czekaj, M.2
Gardner, C.J.3
Guertin, K.R.4
Cheney, D.L.5
Spada, A.P.6
Bolton, S.A.7
Brown, K.8
Colussi, D.9
Heran, C.L.10
Morgan, S.R.11
Leadley, R.J.12
Dunwiddie, C.T.13
Perrone, M.H.14
Chu, V.15
-
16
-
-
0032505156
-
Discovery of N-[2-[5-[amino(imino)methyl]-2-hydro-1-methyl-1H-imidazol-2-ylphenoxy]pyridin-4- yl]-N-methylglycine (ZK-807834): A potent, selective, and orally active inhibitor of the blood coagulation enyme factor Xa
-
(b) Phillips, G. B.; Buckman, B. O.; Davey, D. D.; Eagen, K. A.; Guilford, W. J.; Hinchman, J.; Ho, E.; Koovakkar, A. L.; Light, D. R.; Mohan, R.; Ng, H. P.; Post, J. M.; Shaw, K. J.; Smith, D.; Subramanyam, B.; Sullivan, M. E.; Trinh, L.; Verona, R.; Walters, J.; White, K.; Whitlow, M.; Wu, S.; Xu, W.; Morrissey, M. M. Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin- 4-yl]-N-methylglycine (ZK-807834): A Potent, Selective, and Orally Active Inhibitor of the Blood Coagulation Enyme Factor Xa. J. Med. Chem. 1998, 41, 3557-3562.
-
(1998)
J. Med. Chem.
, vol.41
, pp. 3557-3562
-
-
Phillips, G.B.1
Buckman, B.O.2
Davey, D.D.3
Eagen, K.A.4
Guilford, W.J.5
Hinchman, J.6
Ho, E.7
Koovakkar, A.L.8
Light, D.R.9
Mohan, R.10
Ng, H.P.11
Post, J.M.12
Shaw, K.J.13
Smith, D.14
Subramanyam, B.15
Sullivan, M.E.16
Trinh, L.17
Verona, R.18
Walters, J.19
White, K.20
Whitlow, M.21
Wu, S.22
Xu, W.23
Morrissey, M.M.24
more..
-
17
-
-
0030783421
-
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors
-
Quan, M. L.; Pruitt, J. R.; Ellis, C. D.; Liauw, A. Y.; Galemmo, R. A., Jr.; Stouten, P. F. W.; Wityak, J.; Knabb, R. M.; Thoolen, M. J.; Wong, P. C.; Wexler, R. R. Design and Synthesis of Isoxazoline Derivatives as Factor Xa Inhibitors. Bioorg. Med. Chem. Lett. 1997, 7, 2813-2818.
-
(1997)
Bioorg. Med. Chem. Lett.
, vol.7
, pp. 2813-2818
-
-
Quan, M.L.1
Pruitt, J.R.2
Ellis, C.D.3
Liauw, A.Y.4
Galemmo R.A., Jr.5
Stouten, P.F.W.6
Wityak, J.7
Knabb, R.M.8
Thoolen, M.J.9
Wong, P.C.10
Wexler, R.R.11
-
18
-
-
0033615010
-
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1
-
Quan, M. L.; Liauw, A. Y.; Ellis, C. D.; Pruitt, J. R.; Bostrom, L. L.; Carini, D. J.; Hung, P. P.; Moody, K.; Knabb, R. M.; Thoolen, M. J.; Wong, P. C.; Wexler, R. R. Design and Synthesis of Isoxazoline Derivatives as Factor Xa Inhibitors. 1. J. Med. Chem. 1999, 42, 2752-2759.
-
(1999)
J. Med. Chem.
, vol.42
, pp. 2752-2759
-
-
Quan, M.L.1
Liauw, A.Y.2
Ellis, C.D.3
Pruitt, J.R.4
Bostrom, L.L.5
Carini, D.J.6
Hung, P.P.7
Moody, K.8
Knabb, R.M.9
Thoolen, M.J.10
Wong, P.C.11
Wexler, R.R.12
-
20
-
-
0025369168
-
New preparation of highly functionalized aromatic and heteroaromatic zinc and copper organometallics
-
Majid, T. N.; Knoechel, P. A New Preparation of Highly Functionalized Aromatic and Heteroaromatic Zinc and Copper Organometallics. Tetrahedron Lett. 1990, 31, 4413-4416.
-
(1990)
Tetrahedron Lett.
, vol.31
, pp. 4413-4416
-
-
Majid, T.N.1
Knoechel, P.A.2
-
21
-
-
33845280673
-
Synthesis and reactivity toward acyl chlorides and enones of the new highly functionalized copper reagents RCu(CN)ZnI
-
Knoechel, P.; Yeh, M. C. P.; Berk, S. C.; Telbert, J. Synthesis and Reactivity Toward Acyl Chlorides and Enones of the New highly Functionalized Copper Reagents RCu(CN)ZnI. J. Org. Chem. 1988, 53, 2390-2393.
-
(1988)
J. Org. Chem.
, vol.53
, pp. 2390-2393
-
-
Knoechel, P.1
Yeh, M.C.P.2
Berk, S.C.3
Telbert, J.4
-
22
-
-
0028930160
-
Kinetic and crystallographic studies of thrombin with Ac-(D)Phe-Pro-boroArg-OH and its lysine, amidine, homolysine and ornithine analogues
-
Weber, P. C.; Lee, S.; Lewandowski, F. A.; Schadt, M. C.; Chang, C.; Kettner, C. A. Kinetic and Crystallographic Studies of Thrombin with Ac-(D)Phe-Pro-boroArg-OH and its Lysine, Amidine, Homolysine and Ornithine Analogues. Biochemistry 1995, 34, 3750-3757.
-
(1995)
Biochemistry
, vol.34
, pp. 3750-3757
-
-
Weber, P.C.1
Lee, S.2
Lewandowski, F.A.3
Schadt, M.C.4
Chang, C.5
Kettner, C.A.6
-
23
-
-
0027304964
-
Structure of human Des(1-45) factor Xa at 2.2 Å resolution
-
Padmanabhan, K.; Padmanabhan, K. P.; Tulinsky, A.; Park, C. H.; Bode, W.; Huber, R.; Blankenship, D. T.; Cardin, A. D.; Kiesel, W. Structure of Human Des(1-45) Factor Xa at 2.2 Å Resolution. J. Mol. Biol. 1993, 232, 947-966.
-
(1993)
J. Mol. Biol.
, vol.232
, pp. 947-966
-
-
Padmanabhan, K.1
Padmanabhan, K.P.2
Tulinsky, A.3
Park, C.H.4
Bode, W.5
Huber, R.6
Blankenship, D.T.7
Cardin, A.D.8
Kiesel, W.9
-
24
-
-
0345029328
-
-
note
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The model was generated by minimizing the conformation of 79 (SM084) in the active site of FXa using Discover with the CFF95 force field (MSI, San Diego, CA) until the rms force was smaller than 0.001 kcal/mol Å. The minimizations were carried out keeping the protein rigid and the inhibitor completely flexible.
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-
-
-
25
-
-
0026592320
-
In vivo characterizations of a synthetic thrombin inhibitor
-
Knabb, R. M.; Kettner, C. A.; Timmermans, P. B. M. W. M.; Reilly, T. M. In Vivo Characterizations of a Synthetic Thrombin Inhibitor. Thromb. Haemostasis 1992, 67, 56-59.
-
(1992)
Thromb. Haemostasis
, vol.67
, pp. 56-59
-
-
Knabb, R.M.1
Kettner, C.A.2
Timmermans, P.B.M.W.M.3
Reilly, T.M.4
-
26
-
-
0025094310
-
The selective inhibition of thrombin by peptides of boroarginine
-
Kettner, C. A.; Mersinger, L. J.; Knabb, R. M. The Selective Inhibition of Thrombin by Peptides of Boroarginine. J. Biol. Chem. 1990, 265, 18289-18297.
-
(1990)
J. Biol. Chem.
, vol.265
, pp. 18289-18297
-
-
Kettner, C.A.1
Mersinger, L.J.2
Knabb, R.M.3
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