Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-05-19
1996-10-08
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514414, 514422, 514423, 514822, 514826, A61K 31445, A61K 3140
Patent
active
055631568
ABSTRACT:
This invention relates to novel polyfluorinated alkyl derivatives of certain tripeptides, to the methods for their preparation, the intermediates therefore, to their use in inhibiting thrombin and lung tryptase and in their end-use application as anti-coagulants useful in treating thrombophlebitis and coronary thrombosis and in the treatment of asthma.
REFERENCES:
patent: 4061625 (1977-12-01), AfEkenstam et al.
patent: 4216142 (1980-08-01), Ali
patent: 4217269 (1980-08-01), Cole
patent: 4221706 (1980-09-01), Ali et al.
patent: 4247454 (1981-01-01), AfEkenstam et al.
patent: 4275153 (1981-06-01), Gargiulo et al.
patent: 4318904 (1982-03-01), Shaw et al.
patent: 4450105 (1984-05-01), Nagasawa et al.
patent: 4607047 (1986-08-01), Debay
patent: 4643991 (1987-03-01), Digenis
patent: 4720484 (1988-01-01), Vincent et al.
patent: 4762821 (1988-08-01), Nestor
patent: 4816560 (1989-03-01), Verdini
patent: 4816562 (1989-03-01), Nagasawa et al.
patent: 4826814 (1989-05-01), Sawayama et al.
patent: 4880780 (1989-11-01), Trainor et al.
patent: 4929602 (1990-05-01), Harker et al.
patent: 4980349 (1990-12-01), Roger et al.
patent: 5053392 (1991-10-01), Klein et al.
Kolb, M., et al, "Preparation of Fluorinated Ketone Analogues of Phenylalanine, Lysine, and p-(Guanidino)phenylalanine" Liebigs Ann. chem. pp. 1-6, (1990).
Peet N. P., et al, "Synthesis of Peptidyl Fluoromethyl Ketones and peptidyl .alpha.-Keto Esters as Inhibitors of Procine Pancreatic Elastase, Human Neutrophil Elastase, and Rat human Neutrophil Cathepsin G" J. Med. Chem. 33, pp. 394-407, (1990).
Neises, B., et al "Thrombin Inhibition by the Tripeptide Trifluoromehtyl Ketone D-Phe-Pro-Arg-CF.sub.3 Journal of the International Society on Thrombosis and Haemostatis", Abstracts p. 1290 (1990).
Chem Absts, vol. 110, p. 709, 1989, No. 76058; Angliker, "Synthesis and properties of peptidyl derivatives of arginylfluoromethames" Biochemical Journal, vol. 256, No. 2, pp. 481-486 (1988).
Gelb et al., "Fluoro Ketone inhibitors of Hydrolytic Enzymes," Biochemistry, vol. 24, No. 8, pp. 1813-1817, 1985.
Sham et al., "Highly potent and specific inhibitors of human renin", FEBS Letters, vol. 220, No. 2, pp. 299-301, 1987.
Chem Absts, vol. 107, 1987, No. 40336Y, p. 758.
Shuman et al., Proceedings of the 12th American Peptide Symposium, pp. 801-802, (1991).
Kolb et al, Tetrahedron Letters, vol. 27, No. 37, pp. 4437-4440, (1986).
Kolb et al, Tetrahedron Letters, vol. 27, No. 14, pp. 1579-1582, (1986).
Broersma, Jr. Robert J.
Ganzhorn Axel
Neises Bernhard
Tarnus C eline
Boudreaux William R.
Jordan Kimberly
Merrell Pharmaceuticals Inc.
LandOfFree
Thrombin inhibitors does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Thrombin inhibitors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Thrombin inhibitors will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-57597