Method of synthesis of 2-O-desulfated Heparin and use thereof fo

Details Method of synthesis of 2-O-desulfated Heparin and use thereof fo Method of synthesis of 2-O-desulfated Heparin and use thereof fo

1994-02-03

1997-09-16

Lilling, Herbert J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

536 21, A61K 31425

Patent

active

056681186

ABSTRACT:
A method and medicament for the inhibition of neutrophil elastase and cathepsin G in mammals comprising administering a treatment effective amount of 2-O-desulfated heparin to a mammal in need thereof. The medicament preferably is administered by aerosolization or by intravenous (IV) injection. Preferably, the 2-O-desulfated heparin medicament includes a physiologically acceptable carrier which may be selected from the group consisting of physiologically buffered saline, normal saline, and distilled water. Additionally provided is a method of synthesizing 2-O-desulfated heparin.

REFERENCES:
patent: 4816446 (1989-03-01), Feller et al.
patent: 5296471 (1994-03-01), Holme et al.
L. Levy et al., "Chemical and Pharmacological Studies on N-Sulfated Heparin", Proc. Soc. Exp. Biol. and Med., 109:901-905 (1962).
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F. Redini et al., "Inhibition of Leukocyte Elastase by Heparin and its Derivatives", Biochem. J., 252:515-519 (1988).
M. Jaseija et al., "Novel Regio-and Stereoselective Modifications of Heparin in Alkaline Solution. Nuclear Magnetic Resonance Spectroscopic Evidence", Can. J. Chem., 67:1449-1456 (1989).
E. Sache et al., "Partially N-Desulfated Heparin as a Non-Anticoagulant Heparin: Some Physico-Chemical and Biological Properties", Thromb. Res. 55:247-258 (1989).
N. V. Rao et al., "Sulfated Polysaccharides Prevent Human Leukocute Elastase-Induced Acute Lung Injury and Emphysema in Hamsters", Am. Rev. Respir. Dis., 142:407-412 (1990).
T. Irimura et al., "Chemically Modified Heparins as Inhibitors of Heparan Sulfate Specific Endo-.beta.-glucuronidase (Heparanase) of Metastatic Melanoma Cells": Biochemistry, 25:5322-5328 (1986).
Nagasawa et al., "Hydrophobic-Interaction Chromatography of Glycosaminoglycuronans", Carb. Res. 111:273-281 (1983).

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