Method for the preparation of conjugates of adenine-9-...

C - Chemistry – Metallurgy – 07 – H

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167/114, 530/15.

C07H 19/20 (2006.01) A61K 38/38 (2006.01) A61K 47/48 (2006.01)

Patent

CA 1252719

ABSTRACT OF THE DISCLOSURE For the preparation of conjugates of adenine-9-beta-D- arabinofuranoside 5'-monophosphate (ara-AMP) with lactosaminated human albumin (L-HSA) aqueous solutions of the two components to be conjugated are brought into contact in the presence of 1- ethyl-3-(dimethylaminopropyl)-carbodiimide, by adjusting the pH in the range from slightly acidic to alkaline and by carrying out the conjugate separation. The resulting conjugate, wherein the molar ratio, as determined through spectrophotometric route, between ara-AMP and L-HSA does vary between 5 and 20, remains soluble after lyophilization even at room temperature and shows biological activity at least equivalent to that of the conjugate as prepared according to the known art.

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