Antithrombotic agents

Details Antithrombotic agents Antithrombotic agents

1995-09-01

1998-01-13

Huff, Sheela

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

540593, 540594, 540595, 540362, 544323, 546199, 546246, 546 22, 548128, 548131, 548190, 548112, 548214, 548233, 548535, 548566, 548453, 5483265, 560 34, 560 35, 560168, 560169, 562126, 562439, 562560, 562 15, 564123, 564 15, 558170, C07F 906, C07F 908, C07D21126, C07D21134, C07D22316, C07D20508, C07D23902, A61K 3800

Patent

active

057079668

ABSTRACT:
This invention relates to thrombin inhibiting compounds having the Formula I

REFERENCES:
patent: 4316889 (1982-02-01), Bajusz et al.
patent: 4346078 (1982-08-01), Bajusz et al.
patent: 4399065 (1983-08-01), Bajusz et al.
patent: 4478745 (1984-10-01), Bajusz et al.
patent: 4703036 (1987-10-01), Bajusz et al.
patent: 5053392 (1991-10-01), Klein et al.
patent: 5153176 (1992-10-01), Abe et al.
patent: 5202416 (1993-04-01), Steuber et al.
patent: 5204323 (1993-04-01), Findlay et al.
patent: 5250660 (1993-10-01), Shuman et al.
patent: 5252566 (1993-10-01), Shuman
patent: 5380713 (1995-01-01), Balasubramanian et al.
patent: 5416093 (1995-05-01), Shuman
patent: 5430023 (1995-07-01), Gesellchen et al.
patent: 5436229 (1995-07-01), Ruterbories et al.
patent: 5439888 (1995-08-01), Shuman et al.
patent: 5484772 (1996-01-01), Sall et al.
patent: 5488037 (1996-01-01), Sall et al.
patent: 5510369 (1996-04-01), Lumma et al.
patent: 5561146 (1996-10-01), Kim et al.
patent: 5578574 (1996-11-01), Shuman et al.
Misra, Raj N., et al., Bioorg. & Med. Chem. Letters, 4, 2165-2170, (1994).
Bajusz, S., et al., J. Med. Chem., 1990, 33, 1729-1735.
Fareed, J., et al., Annals N.Y. Academy of Sciences, 1981, 765-784.
Shuman R. T., et al., In Peptides (Proceedings of the Twelfth American Peptide Symposium, Jun. 16-21, 1991); ESCOM: Leiden: 1992; pp. 799-800 and 801-802.
Wilson, et al., American Heart Association, Nov. 11-14, 1991, Anaheim Convention Center, Anaheim, CA, Abstract.
Bajusz, et al. Int. J. Peptide Res., 12, 1978, 217-221.
Gesellchen, et al., Tenth American Peptide Symposium, May 23-28, 1987, St. Louis, MO, Abstract and posters.
Claeson, et al., Proceedings of the Twelfth American Peptide symposium, Jun. 16-21, 1991, Cambridge, MA, pp. 824-825.
Smith, G. F., Shuman, R. T. Gesellchen, P.D., Craft, T.J., Gifford, P., Kurz, K.D., Jackson, C.V., Sandusky, G.E., and P.D. Williams, A New Family of Thrombin Inhibitors with Improved Specificity and Therapeutic Index. (Submitted to the American Heart Association, Oct., 1991, Circulation Oct., 1991, vol. 84, II-579, 1991), Abstract.
Jackson, V., Wilson, H., Frank, J., Crowe, V., Craft, T., and G. Smith. The Thrombin Inhibitor, Methyl-D-Phe-Pro-Arginal--An Effective Adjunct to Coronary Artery Thrombolysis in the Anesthetized Dog. FASEB J. 5(4)A520
Crowe, V., Frank, J., Wilson, H., Coffman, B., Smith, G., and V. Jackson. Anticoagulant and Antithrombotic Efficacy of the Novel Thrombin Inhibitor Methyl-D-Phg-Pro-Arginal in a Canine Model of Coronary Thrombosis. FASEB CK!.
Wilson, H., Frank J., Crowe, V., Coffman, B., Smith. G., Shuman, R., and V. Jackson, Anticoagulant and Antithrombotic Efficacy of the Novel Thrombin Inhibitor, Methyl-D-Phg-Pro-Arginal, in a Canine Model of Coronary Thrombosis (Arteriosclerosis and Thrombosis, 11(5), Oct., 1991) p. 1586a. Abstract.
Jackson, V., Wilson, H., Frank, J., Crowe, V., Coffman, B., Shuman, R., and G. Smith. The Novel Thrombin Inhibitor Methyl-D-Phg-Pro-Arginal: An Effective Conjunctive Agent to Coronary Artery Thrombolysis in the Anesthetized Dog. (Arteriosclerosis and Thrombosis, 11(5), Oct., 1991) p. 1586a, Abstract.
Shuman, R.T., Rothenberger, R.B., Campbell, C.S., Smith, G.F., Jackson, C.V., Kur, K.D., and P.D. Gesellchen. A Series of Highly Active Serine Proteinae Inhibitors. American Peptide Symposium, Jun. 1991, Abstract.
Jackson, C.V., Frank, J.D., Crowe, V.G., Craft, T.J., and G.F. Smith. Assessment of the Anticoagulant and Antithrombotic Efficacy of the Thrombin Inhibitor, BOC-Phe-Pro-Arginal, in a Canine Model of Coronary Thrombosis. Arteriosclerosis, 10 922A (1990).
Jackson, C.V., Frank, J.D., Crowe, V.G., Craft, T.J., and G.F. Smith. The Thrombin Inhibitor, BOC-D-Phe-Pro-Arginal. An Effective Adjunct to Coronary Artery Thrombolysis in the Anesthetized Dog. Arteriosclerosis, 10 923a (1990).
Shackelford. K.A., Tanzer, R.L., Shuman, R., Gesellchen, P.D., Grindey, G.B., Sundboom, J.L., Smith, G.F., and R.L., Merriman. Inhibition of Spontaneous Metastasis by Boc-D-Phe-Pro-Arginal. American Association for Cancer Research, San Francisco, 1989. Proc. Am. Assn. Cancer Res., 30 86, 1989.
Neubauer, B.L., Clemens, J.A., Gesellchen, P.D., Hirsch, K.S., Hoover, D.M., Merriman. R.L., and G.F. Smith. Endocrine Characterization and Sensitivity of the PAIII Prostatic Adenocarcinoma in Male Lobund-Wistar (LW) Rats to Anti-Fibrin Agents. American Association for Cancer Research. New Orleans, May 1988, Proc. Am. Assn. Cancer Res., 29 240 (1988).
Neubauer, B.L., Best, K.L., Gesellchen, P.D., Goode, R.L., Merriman, R.L., Tanzer, L.R., Shaar, C.J., Shuman, R., Sundboom, Pro-Arginal on the Metastasis of the PAIII Prostatic Adenocarcinoma in Male Lobund Wistar (LW) Rats. American Urological Association. Boston, May 1988, J. Urol., 139 175A (1988).
Gesellchen, P.D., Smith, G.F., et al., Anticoagulant, Antithrombotic, and Antimetastatic Effects of a Serine Proteinase Inhibitor. 10th American Peptide Symposium, Washington University, St. Louis, MO (1987), Abstract.
Smith, G.F., Sundboom, J.L., Best, K., Gesellchen, P.D., Merriman, R.L., Shuman, R., and Neubauer, B.L. Heparin, Boc-D-Phe-Pro-Arginal, and Warfarin (Fibrin Antagonists) Inhibit Metastasis in an In Vivo Model. American Chemical Society National Meeting. Abstract BIOL 70 Biochemistry (1987).
K.D. Kurz, T. Smith, R.A. Moore, and B.W. Main. Comparison of Thrombin Inhibitors in Rat Models to Thrombosis and Thrombolysis. FASEB Journal, vol. 5 (No. 4), 1991, Abstract #886.
Tomori, et al., Chromatographia, vol. 19, 437-442 (1984).
Dayhoff, Atlas of Protein Sequence and Structure, 5, pp. 85-89 (1972).
Shuman, et al., J. Med. Chem., 36(3), 314-319 (1993).
Jackson, et al., J. Cardiovasc. Pharmacol., 21(4), 587-594 (1993).
Cheng, et al., Tetrahedron Lett., 32 (49), 7333-7336 (1991).
Bagdy, et al., Thrombosis and Haemostasis, 68(2), 125-129 (1992).
Thrombosis and Haemostasis, 65, 1289, Nos. 2150-2151 and 2152 (1991).
Bagdy, et al., Thrombosis and Haemostasis, 67(3), 325-330 (1992).
Bagdy, et al., Thrombosis and Haemostasis, 67(3): 357-365 (1992).
Balasubramanian, et al., J. Med. Chem., 36, 300-303 (1993).
Shuman, et al., Oral Activity of Tripeptide Aldehyde Thrombin Inhibitors, Thirteenth American Peptide Symposium, Jun. 2025, 1993, Abstract.
Kurz et al., Antithrombotic Efficacy in the Rat After Intravenous and Oral Administration of a Direct Inhibitor of Thrombin FASEB, Mar. 28-Apr. 1, 1993.
Iwanowicz, et al., Bioorg. Med. Chem. Lett., 2(12), 1607-1612 (1992).
Barabas, et al., Blood Coagul. Fibrin., 4, 243-248 (1993).
Jackson, et al., Conjunctive Therapy with the Thrombin Inhibitor, LY 294468, and Aspirin Produced Enhanced Antireocclusive Activity When Used in a Canine Model of Streptokinase-Induced Coronary Thrombolysis, The Pharmacologist, 35(3), 207 (1993), Abstract #407.
Pozagay, et al., Study of the Specifity of Thrombin with Tripeptidyl-p-Nitroanilide Substrates, Eur. J. Biochem., 115, 491-495 (1981).
Smith, et al., Synthesis and Pharmacological Activity of Angiotensin Converting Enzyme Inhibitors: N-(Mercaptoacyl)-4-substituted-(S)-prolines, J. Med. Chem., 31, 875-885 (1988).
Jackson, et al., The Journal of Pharmacology and Experimental Therapy, 261(2), 546-552 (1992).
Stueber, et al., Proc. of the 13th American Peptide Symposium, Jun. 20-25, 1993.
Sturzebecher, et al., XIVth Congress of the International Society on Thrombosis and Hemostasis, Jul. 4-9, 1993.
Simoons et al., Circulation, 90, I-231, Abstr. 1241 (1994).
Iwanowicz, Edwin J., et al., J. Med. Chem., 37, 2122-2124, (1994).

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