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|Title:||Process for the preparation of desulfatohirudins|
|Abstract:||The present invention relates to desulfatohirudins, to the preparation thereof, to pharmaceutical compositions containing these compounds, and to the use thereof. The desulfatohirudins of this invention correspond to hirudin in biological activity and are therefore particularly useful for inhibiting blood clotting.|
|Inventor(s):||Fritz; Hans (Hohenbrunn, DE), Dodt; Johannes (Munich, DE), Seemuller; Ursula (Munich, DE), Fink; Ernst (Westerstede-Giesselhorst, DE)|
|Assignee:||Ciba-Geigy Corporation (Ardsley, NY) Plantorgan Werk Heinrich G.E. Christensen KG (Bad Zwischenahn, DE)|
|Filing Date:||Nov 21, 1984|
|Claims:||1. A process for the preparation of a desulfatohirudin, or a salt thereof comprising hydrolytically removing from hirudin a sulfuric acid monoester group from the phenolic hydroxyl group of the tyrosine residue at position 63 of hirudin, said desulfatohirudin being of the formula ##STR3## or of the formula ##STR4## wherein the -Cys- residues are linked in pairs by disulfide bridges in the same manner as in hirudin, or a salt thereof. |
2. A process according to claim 1, wherein hirudin is subjected to the hydrolytic cleavage with an arylsulfatase, and any of the desulfatohirudins of formula I or II is separated.
3. A process according to claim 1, wherein the hydrolytic removal is carried out under the conditions of acid catalysis.