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

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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536 21, A61K 31725, C08B 3710

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active

057079749

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.

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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 Leukocyte 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 Metastiatic Melanoma Cells", Biochemistry, 25:5322-5328 (1986).
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