Non-Amidine-Containing 1,2-Dibenzamidobenzene Inhibitors of Human Factor Xa with Potent Anticoagulant and Antithrombotic Activity-Reference-Cited by-同舟云学术

Non-Amidine-Containing 1,2-Dibenzamidobenzene Inhibitors of Human Factor Xa with Potent Anticoagulant and Antithrombotic Activity

Published:2000-05-12 Issue:11 Volume:43 Page:2087-2092
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Masters John J.¹,Franciskovich Jeffry B.¹,Tinsley Jennifer M.¹,Campbell Charles¹,Campbell Jack B.¹,Craft Trelia J.¹,Froelich Larry L.¹,Gifford-Moore Donetta S.¹,Hay Lynne A.¹,Herron David K.¹,Klimkowski Valentine J.¹,Kurz Kenneth D.¹,Metz James T.¹,Ratz Andrew M.¹,Shuman Robert T.¹,Smith Gerald F.¹,Smith Tommy¹,Towner Richard D.¹,Wiley Michael R.¹,Wilson Alex¹,Yee Ying K.¹

Affiliation:

1. Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/jm990625b

Reference15 articles.

1. The earliest reports of efficacy in vivo were with protein-based agents. (a) Vlasuk, G. P.; Fujita, T.; Dunwiddie, C. T.; Nutt, E. M.; Smith, D. E.; Shebuski, T. J. Comparison of the In Vivo Anticoagulant Properties of Standard Heparin and the Highly Selective Factor Xa Inhibitors Antistasin and Tick Anticoagulant Peptide (TAP) in a Rabbit Model of Venous Thrombosis.Thromb. Haemostasis1993,70(1), 212−216. (b) Schaffer, L. W.; Davidson, J. T.; Vlasuk, G. P.; Dunwiddie, C. T.; Siegl, P. K. S. Selective Factor Xa Inhibition by Recombinant Antistasin Prevents Vascular Graft Thrombosis in Baboons. Arteroscl. Thromb.1992,12, 879−885. Reports of efficacy in vivo with small molecule inhibitors of fXa have more recently been disclosed. (c) Bostwick, J. S.; Bentley, R.; Morgan, S.; Brown, K.; Chu, V.; Ewing, W. R.; Spada, A. P.; Pauls, H.; Perrone, M. H.; Dunwiddie, C. T.; Leadley, R. J., Jr. RPR120844, a Novel, Specific Inhibitor of Coagulation Factor Xa inhibits Venous Thrombosis in the Rabbit.Thromb. Haemostasis1999,81(1), 157−160. (d) Kawasaki, T.; Sato, K.; Sakai, Y.; Hirayama, F.; Koshio, H.; Taniuchi, Y.; Matsumoto, Y. Comparative Studies of an Orally-Active Factor Xa inhibitor, YM-60828, with other 2091 Antithrombotic Agents in a Rat Model of Arterial Thrombosis.Thromb. Haemostasis1998,79(2), 410−416. (e) Wong, A. G.; Ku, P.; Lin, P. H.; Zhu, B. Y.; Marlowe, C. K.; Scarborough, R. M.; Hollenbach, S. J.; Sinha, U. Inhibition of Rabbit Deep Vein Thrombosis by Specific Inhibitors of Coagulation Factor Xa. Presented at XVIth Congress of the International Society on Thrombosis and Haemostasis, Florence, Italy, June 6−12, 1997, Abstract PS-1197. (f) Herault, J. P.; Bernat, A.; Pflieger, A. M.; Lormeau, J. C.; Herbert, J. M. Comparative Effects of Two Direct and Indirect Factor Xa Inhibitors on Free and Clot-Bound Prothrombinase.J. Pharmacol. Exp. Ther.1997,283(1), 16−22. (g) Kim, D.; Kambayashi, J.; Shibuya, T.; Sakon, M.; Kawasaki, T. In Vivo Evaluation of DX-9065a, a Synthetic Factor Xa Inhibitor, in experimental Vein Graft.J. Atheroscler.Thromb.1996,2(2), 110−116.

2. 1,2-Dibenzamidobenzene Inhibitors of Human Factor Xa

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