US4654302A
Expired / Lapsed
US
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Process for the preparation of desulfatohirudins
Assignee: UCP Gen Pharma AG
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Filing: 1984-11-21
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Granted: 1987-03-31
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Expires: 2004-11-21
Abstract
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.
Inventors
- 👤 Hans Fritz
- 👤 Johannes Dodt
- 👤 Ursula Seemuller
- 👤 Ernst Fink
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 16:15
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/81; C07K14/815; A; A61; A61P; A61P7/00; A61P7/02; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/26
Claims Analysis
Total Claims: 4
Claim 1
Independent Claim
70 words
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.
Claim 2
Dependent Claim
70 words
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.
Claim 3
Dependent Claim
29 words
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.
Claim 4
Dependent Claim
19 words
A process according to claim 1, wherein the hydrolytic removal is carried out under the conditions of acid catalysis.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-03-30 | 1990-09-29 | 1991-03-31 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-03-30 | 1994-09-29 | 1995-03-31 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-03-30 | 1998-09-29 | 1999-03-31 | $7700.00 | Window Closed / Lapsed |