Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1997-02-06
1999-07-13
Fonda, Kathleen K.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
536 53, 536 54, 536 551, A61K 31715
Patent
active
059226900
ABSTRACT:
A method of inhibiting thrombin generation and of inhibiting complement activation by using a dermatan sulfate having at least 2 sulfate groups per disaccharide obtained by chemical sulfation of native dermatan sulfate. The resulting dermatan sulfate having an average molecular weight from about 5000 to 35000 Daltons is characterized by (i) a high content of L-iduronic->4,6-di-O-sulfated N-acetyl-D-galactosamine residues, and (ii) a specific heparin cofactor II-mediated anti-thrombin activity, depending on average molecular weight, between about 25 to 125 U/mg.
REFERENCES:
patent: 3207664 (1965-09-01), Nomine et al.
patent: 3634123 (1972-01-01), Eriksson et al.
patent: 4440926 (1984-04-01), Mardiguian
patent: 4727063 (1988-02-01), Naggi et al.
patent: 4745106 (1988-05-01), Griffin et al.
patent: 5013724 (1991-05-01), Petitou et al.
patent: 5547994 (1996-08-01), Mascellini et al.
Fernandez et al, "Catalysis of Thrombin Inhibition Provides an Inde for Esimating the Antithrombotic Potential of Glycosaminoglycans in Rabbis," Thromb. Haemostas., (1987), pp. 286-293.
Fernandez et al, "The Hemorrhagic and Antithrombotic Effects of Dermatan Sulfate," Brit. J. Haematol., 64 (1986), pp. 309-317.
Linhardt et al, "Dermatan Sulfate as Potential Therapeutic Agent," Gen. Pharmar., 26, No. 3 (1995), pp. 443-451.
Ofosu et al, "Heparan Sulfate and Dermatan Sulfate Inhibit the Generation of Thrombin Activity in Plasma by Complementary Pathways," Blood, 64, No. 3 (Sep. 1984), pp. 742-747.
Okwusidi et al, "In Vivo Catalysis of Thrombin Inhibition by Antithrombin III or Heparin Co-Factor II and Antithrombotic Effect: Differential Effects of Unfractionated Heparin and Dermatan Sulfate," Thromb. Haeorrh. Disorders, 1, (1990), pp. 77-80.
Ryan et al, "Antithrombotic Properties of Dermatan Sulfate (MF701) in Haemodialysis for Chronic Renal Failure," Thromb. Haemostas., 68 (1992), pp. 563-569.
Tollefsen et al, "The Interaction of Glycosaminoglycans with Heparin Cofactor II: Structure and Activity of a High-Affinity Dermatan Sulfate Hexasaccharide," Plenum Press, (1992), pp. 167-176.
Van Ryn-McKenna, "Dermatan Sulfate: A New Concept in Antithrombotic Therapy," Diss. Abstr. Int., B 53, (1993), p. 5662.
Volpi et al, "Physico-Chemical Properties and the Structure of Dermatan Sulfate Fractions Purified from Plasma after Oral Administration in Healthy Human Volunteers," Thromb. Haemostas., 75 (1996), pp. 491-496.
Whinna et al, "Interaction of Heparin Cofactor II with Biglycan and Decorin," J. Biol. Chem., 268, (Feb. 1993), pp. 3920-3924.
Agnelli, "New Antithrombins and Nonheparin Glycosaminoglycans in Clinical Development," Vessels , 1 (1995), pp. 9-16.
Bergonzini et al, "Pharmacokineics of Native and Low Molecular Weight Dermatans: Preliminary Studies in Rats and Primates," Seminars in Thrombosis and Hemostasis, Sup 2, (1991), pp. 235-239.
Cifonelli et al, "," Unknown Journal, 233 (1958), pp. 541-545.
Brister et al, "Is Heparin the Ideal Anticoagulant for Cardiopulmonary Bypass? Dermatan Sulphate May Be an Alternate Choice,," Thromb. Haemostas., 71 (1994), pp. 468-473.
Dietrich et al, "The influence of Preoperative Anticoagulation on Heparin Response During Cardiopulmnary Bypass," J. Thorac. Cardiovasc. Surg., 102 (1991), pp. 505-514.
Dunstone et al, "Ion-Exchange Reactions Between Acid Mucopolysaccharides and Various Cations," Biochem.J., 85, No. 3 (1962), pp. 336-351.
Edens et al, "Heparin and Derivatized Heparin Inhibit Zymosan and Cobra Venom Factor Activation of Complement in Serum," Immunopharmoacol., 27 (1994), pp. 145-153.
Edens et al, "Heparin Is Not Just An Anticoagulant Anymore: Six and One-Half Decades of Studies on the Ability of Heparin to Regulate Complement Activity," Complement Profiles, (1993), pp. 96-120.
Fareed et al, "Molecular and Functional Heterogeneity in Dermatan Sulfate Preparations," Seminars in Thrombosis and Hemostasis, 17, supp 2 (1991), pp. 174-180.
Ferrari et al, "Preliminary Chemical, Biochemical, and Pharmacological Characterization of a Low Molecular Weight Dermatan Sulphate," Carbohydrate Res., 255, No. 3 (1994), pp. 125-132.
Hemker et al, "Mode of Action of Heparin and Related Drugs," Seminars In Thrombosis and Hemostasis, 17, supp 1 (1991), pp. 29-34.
Hogg et al, "Fibrin Monomer Protects Thrombin from Inactivation by Heparinantithrombin III: Implications for Heparin Therapy," Proc. Natl. Acad. Sci., 86 (May 1989), pp. 3619-3638.
Ireland et al, "Heparin as an Anticoagulant During Extracorporal Circulation," Heparin, (1989), pp. 549-574.
Kawai et al, "Chondroitin Polysulfate of Squid Cartilage," Biochem, 60 (1966), pp. 317-321.
Kiss, ".beta.-Eliminative Degradation of Carbohydrates Containing Uronic Acid Residues," Adv. Carbohydr. Chem. Biochem., 29 (1974), pp. 229-303.
Levy et al, "Chemical and Pharmacologica Studies on N-Resulfated Heparin," Proc. Soc. Exp. Biol. Med.., 109 (1962), pp. 901-905.
Linhardt et al, "Low Molecular Weight Dermatan Sulfate as an Antithrombotic Agent," Biochem. Pharm., 47, No. 7 (1994), pp. 1241-1252.
Linhardt et al, "Analysis of Glycosaminoglycans with Polysaccharide Lyases," Current Protocols in Molecular Biology, (1995), pp. 2:17.13.17-17.13.32.
Maaroufi et al, "Influence of the Oversulfation Method and the Degree of Sulfation on the Anticoagulant Properties of Dermatan Sulfate Derivatives," Thromb. Res., 59, (1990), pp. 749-758.
Maimone et al, "Structure of a Dermatan Sulfate Hexasaccharide that Binds to Heparin Cofactor II with High Affinity," J. Biol. Chem., 265, (Oct. 1990), pp. 1863-1871.
Mascellani et al, "Quantitation of Dermatan Sulfate Active Site for Heparin Cofactor II by .sup.1 H Nuclear Magnetic Resonance Spectroscopy," Anal. Biochem.., 223 (1994), pp. 135-141.
Mascellani et al, "Relative Influence of Different Disulphate Disaccharide Clusters on the HCII-Mediated Inhibition of Thrombin by Dermatan Sulfates of Different Origins," Thromb. Res., 74, (1994), pp. 605-615.
Matthiasson et al, "The Haemorrhagic Effect of Low Molecular Weight Heparins, Dermatan Sulphate and Hirudin," Haemostasis, 25 (1995), pp. 203-211.
Ogamo et al, "Reactivity Toward Chemical Sulfation of Hydroxyl Groups of Heparin," Carboh. Res., 193, (1989), pp. 165-172.
Seikagaku Kogyo Co., Products for Life Science, (1989).
Tollefsen et al, Heparin Cofactor II. Purification and Properties of a Heparin-Dependent Inhibitor of Thrombin in Human Plasma, J. Biol. Chem., 257, (Mar. 1982), pp. 2162-2169.
Thomas et al, "Relative Efficacy of Heparin and Related Glycosaminoglycans as Antithrombotic Drugs," Ann. N.Y. Acad. Sci., 556 (1989), pp. 313-322.
Uchiyama et al, "Changes in the Structure and Biological Property of N.fwdarw.O Sulfate Transferred N-Reulfated Heparin" J. Biol. Chem., 4, (Apr. 1991), pp. 6756-6760.
Volpi et al, "Dermatan Sulfate from Beef Mucosa: Structure, Physicochemical and Biological Properties of Fractions Prepared by Chemical Depolymerization and Anion-Exchange Chromatography," Carbohydrate Res., 255, (1994), pp. 133-144.
Weiler et al, "Heparin and Modified Heparin Inhibit Complement Activation In Vivo," J. Immunol., 148, (May 1992), pp. 3210-3215.
Murata et al. Renal Physiol. 1978, 1(1), 48-55.
Mascellani et al. Thrombosis Research Oct. 1996, 84(1), 21-32.
Pavao et al. J. Biol. Chem. Dec. 1995, 270(52), 31027-31036.
Ofosu et al. Biochem. J. Dec. 1987, 248, 889-896.
Linhardt et al. Biochemical Pharmacology Sep. 1991, 42(8), 1609-1619.
Nagasawa et al, "Chemical Sulfation of Preparations of Chrondroitin 4- and 6-Sulfate, and Dermatan Sulfate Preparation of Chondroitin Sulfate E-Like Materails From Chondroitin," Carbohydrate Research, 158, No. 1 (Dec. 1986), pp. 183-190, Amsterdam, Netherlands.
Brister Stephanie J.
Buchanan Michael R.
Linhardt Robert J.
Van Gorp Cornelius L.
Fonda Kathleen K.
Guttag Eric W.
Smith Mark F.
LandOfFree
Dermatan disulfate, an inhibitor of thrombin generation and acti does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Dermatan disulfate, an inhibitor of thrombin generation and acti, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Dermatan disulfate, an inhibitor of thrombin generation and acti will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2275808