US5312736A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Anticoagulant analogues of the tissue factor extrinsic pathway inhibitor (EPI) with reduced affinity for heparin
Assignee: Novo Nordisk AS
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Filing: 1990-08-17
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Granted: 1994-05-17
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Expires: 2010-08-17
Abstract
Abstract Novel extrinsic pathway inhibitors (EPI) are provided wherein one or more of the amino acid residues of native EPI have been deleted. A preferred group of the novel EPI analogues have no or a low heparin binding capacity. The novel EPI analogues can be used for the treatment of patients having coagulation disorders or cancer.
Inventors
- 👤 Jesper S. Rasmussen
- 👤 Ole J. Nordfang
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 00:43
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/81; C07K14/8107; C07K14/811; C07K14/8114; A; A61; A61P; A61P35/00; A61P7/00; A61P7/02; A61K; A61K38/00
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
75 words
An analogue of extrinsic pathway inhibitor (EPI) which analogue is a derivative of the full-length EPI sequence depicted in SEQ ID NO: 1, and which analogue retains the anticoagulant activity of native EPI as well as anti-FXa activity, comprises the three Kunitz protease inhibitor domains present in EPI, but has a heparin binding capacity less than 50% of the heparin binding capacity of native EPI when each is contacted with immobilized heparin under physiological conditions.
Claim 2
Dependent Claim
75 words
An analogue of extrinsic pathway inhibitor (EPI) which analogue is a derivative of the full-length EPI sequence depicted in SEQ ID NO: 1, and which analogue retains the anticoagulant activity of native EPI as well as anti-FXa activity, comprises the three Kunitz protease inhibitor domains present in EPI, but has a heparin binding capacity less than 50% of the heparin binding capacity of native EPI when each is contacted with immobilized heparin under physiological conditions.
Claim 3
Dependent Claim
24 words
EPI analogue according to claim 1 comprising the amino acid sequence from Asp1 to Thr161 (SEQ ID NO: 7) of the native EPI molecule.
Claim 4
Dependent Claim
24 words
EPI analogue according to claim 1 comprising the amino acid sequence from Glu15 to Thr161 (SEQ ID NO: 5) of the native EPI molecule.
Claim 5
Dependent Claim
17 words
EPI analogue according to claim 1 and further having a Ser as the N-terminal amino acid residue.
Claim 6
Dependent Claim
9 words
DNA-sequence encoding an EPI analogue according to claim 1.
Claim 7
Dependent Claim
9 words
Expression vector containing a DNA-sequence according to claim 5.
Claim 8
Dependent Claim
14 words
Transformed or transfected microorganism or cell line comprising a vector according to claim 6.
Claim 9
Dependent Claim
32 words
A method for preparation of an EPI analogue wherein a microorganism or cell line according to claim 7 is cultured in a suitable culture medium and said EPI analogue is isolated therefrom.
Claim 10
Dependent Claim
17 words
A therapeutic preparation comprising an EPI analogue according to claim 1 and a suitable adjuvant or carrier.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1997-05-16 | 1997-11-15 | 1998-05-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2001-05-16 | 2001-11-15 | 2002-05-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2005-05-16 | 2005-11-15 | 2006-05-17 | $7700.00 | Window Closed / Lapsed |