Covalently attached complex of alpha-1-proteinase inhibitor with a water soluble polymer
AssigneeMiles Laboratories, Inc.
InventorGautam Mitra
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Abstract
There is disclosed a process for producing a covalently attached alpha-1-proteinase inhibitor - water soluble polymer complex useful for pulmonary emphysema therapy, a covalently attached alpha-1-proteinase inhibitor - water soluble polymer complex produced by the process, a composition thereof in a pharmaceutically acceptable carrier, and a method for treating pulmonary emphysema by administering to a human patient a therapeutically effective amount of the complex or preparation.
Claims45
A process for producing a covalently attached complex of alpha-1-proteinase inhibitor with a water soluble polymer having hydroxy groups pendant to the polymer backbone, which hydroxy groups and amino groups pendant to alpha-1-proteinase inhibitor are chemically reactive with a polyfunctional coupling compound, comprising the steps of:
- (a) contacting the water soluble polymer having hydroxy groups pendant to the polymer backbone, which hydroxy groups are chemically reactive with a polyfunctional coupling compound, with a polyfunctional coupling compound having functional groups which are reactive with said hydroxy groups in a chemical activation reaction to obtain an activated intermediate which is reactive with amino groups pendant to the protein, alpha-1-proteinase inhibitor;
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- (b) contacting the activated intermediate from step (a) with alpha-1-proteinase inhibitor in a chemical coupling reaction to effect covalent attachment and to thereby obtain a covalently attached complex of alpha-1-proteinase inhibitor with the water soluble polymer.
Dependencies are inferred from the claim text.