Patent US4767742A successfully refreshed from Google Patents.
US4767742A
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US
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Hirudin-PA and its derivatives, process for manufacturing these and the use of these substances
Assignee: UCP Gen Pharma AG
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Filing: 1985-12-12
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Granted: 1988-08-30
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Expires: 2005-12-12
Abstract
Abstract The present invention relates to a new content substance found in leeches (Hirudo medicinalis), the derivatives of this abbreviated at the N-terminus and the C-terminus, and the desulfated derivatives therefrom as well as a process for the production of these compounds, and their use. These compounds possess thrombin-inhibiting properties and can be used to inhibit clotting in human and animals, for blood conservation, or as reagents for the analytical determination of thrombin.
Inventors
- 👤 Johannes Dodt
- 👤 Ursula Seemuller
- 👤 Hans Fritz
- 👤 Ernst Fink
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 21:00
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/81; C07K14/815; A; A61; A61P; A61P43/00; A61P7/00; A61P7/02; A61K; A61K38/00
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
91 words
A hirudin-PA compound of the formula I: ##STR6## in which the above letters represent proteinogenic amino acids corresponding to the IUPAC nomenclature, said amino acids being peptidically bonded, and in which Y * is tyrosin, tyrosin-O-sulfate, or derivatives thereof, shortened by up to 2 amino acids at the N-terminus, and the amino acid chain at the C-terminus is shortened by the sequence ##STR7## or, if Y * is tyrosin, the amino acid chain is shortened by the sequence D E or E at the C-terminus, or a pharmaceutically useful salt thereof.
Claim 2
Dependent Claim
91 words
A hirudin-PA compound of the formula I: ##STR6## in which the above letters represent proteinogenic amino acids corresponding to the IUPAC nomenclature, said amino acids being peptidically bonded, and in which Y * is tyrosin, tyrosin-O-sulfate, or derivatives thereof, shortened by up to 2 amino acids at the N-terminus, and the amino acid chain at the C-terminus is shortened by the sequence ##STR7## or, if Y * is tyrosin, the amino acid chain is shortened by the sequence D E or E at the C-terminus, or a pharmaceutically useful salt thereof.
Claim 3
Dependent Claim
27 words
Hirudin-PA derivatives as in claim 1 of the general formula I, wherein the amino acid chain is abbreviated at the N-terminus by the sequence I or IT.
Claim 4
Dependent Claim
18 words
The hirudin-PA compound as in claim 1, wherein Y * is tyrosin-O-sulfate or a pharmaceutically useful salt thereof.
Claim 5
Dependent Claim
19 words
A desulfato hirudin-PA compound as in claim 1, wherein Y * is tyrosin or a pharmaceutically useful salt thereof.
Claim 6
Dependent Claim
23 words
A desulfato hirudin-PA compound as in claim 1 having the formula: ##STR8## wherein Y * is tyrosin is a pharmaceutically useful salt thereof.
Claim 7
Dependent Claim
23 words
A desulfato hirudin-PA compound as in claim 1 having the formula: ##STR9## wherein Y * is tyrosin or a pharmaceutically useful salt thereof.
Claim 8
Dependent Claim
25 words
The hirudin-PA compound of claim 1, which comprises 66 amino acids having a molecular weight of 7087 and a specific antithrombin activity of 680-720 IU/mg.
Claim 9
Dependent Claim
27 words
A method for inhibiting blood clotting in humans or animals, which comprises administering a therapeutically effective amount of the hirudin-PA compound of claim 1 to a subject.
Claim 10
Dependent Claim
30 words
The method according to claim 8, which comprises administering about 0.005 to about 0.1 mg/kg by body weight of said compound to the subject by intravenous, intramuscular or subcutaneous injection.
Claim 11
Dependent Claim
21 words
A composition comprising an effective thrombin inhibiting amount of the hirudin-PA compound of claim 1 and a pharmaceutically acceptable carrier therefor.
Claim 12
Dependent Claim
9 words
A topical preparation comprising the composition of claim 10.
References Cited (Backward Citations)
EP0142860A2
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-08-30 | 1992-02-29 | 1992-08-30 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-08-30 | 1996-02-29 | 1996-08-30 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-08-30 | 2000-02-29 | 2000-08-30 | $7700.00 | Window Closed / Lapsed |