Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1995-03-02
1996-11-26
Scheiner, Toni R.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
514 19, 530331, 540476, 544372, 544111, 544141, 544 585, 548146, 548215, 548240, 548214, 548468, A61K 3800, C07K 500, C07K 700, C07K 1700
Patent
active
055785743
ABSTRACT:
This invention relates to L-arginine aldehyde derivatives, having the formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
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 et al.
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.
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, et al., Proceedings of the Twelfth American Peptide Symposium, Jun. 16-21, 1991, pp. 799-802.
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.
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 (1991).
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 J. 5(4)A520 (1991).
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.
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. (Arteriosclerosos and Thrombosis, 11(5), Oct., 1991) p. 1586a.
Shuman, R. T., Rothenberger, R. B., Campbell, C. S., Smith, G. F., Jackson, C. V., Kurz, K. D., and P. D. Gesellchen. Prevention of Reocclusion by a Thrombin Inhibitor. (American Peptide Symposium, Jun., 1991, pp. 799-800).
Shuman, R. T., Rothenberger, R. B., Campbell, C. S., Smith, G. F., Jackson, C. V., Kurz, K. D., and P. D. Gesellchen. A Series of Highly Active Serine Proteinase Inhibitors.(American Peptide Symposium, Jun. 1991, pp. 801-802).
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 of 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 of 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. 20-25, 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 Specificity of Thrombin with Tripeptidyl-p-Nitroanilide Substrates, Eur. J. Biochem., 115, 491-495 (1981).
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.
St urzebecher, 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).
Kurz Kenneth D.
Rothenberger Robert B.
Sall Daniel J.
Shuman Robert T.
Smith Gerald F.
Boone David E.
Demeter John C.
Eli Lilly and Company
Huff Sheela J.
Jackson Thomas E.
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