Deep knowledge on
small-molecule drugs and
the 110,000 global patents
Anticipate generic drug launch
Manage your formulary budget
Find generic entry opportunities
Proactively manage your pharmacy inventory
Drug patents …
… from Kazakhstan to Kalamazoo
Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|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.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.