US4495285A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Plasminogen activator derivatives
Assignee: Nippon Chemiphar Co Ltd
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Filing: 1982-10-27
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Granted: 1985-01-22
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Expires: 2002-10-27
Abstract
Abstract A derivative of a human-originated non-immunogenic plasminogen activator is disclosed which comprises at least one polyalkylene glycol attached with at least one coupling agent to amino acid side chains of said plasminogen activator, said polyalkylene glycol having a molecular weight of 200-20,000 and optionally containing one or more alkyl and/or alkanoyl groups as substituents. Also disclosed are a process for producing such derivative and a thrombolytic agent containing such derivative.
Inventors
- 👤 Kimihiro Shimizu
- 👤 Tsuguji Nakahara
- 👤 Taketoshi Kinoshita
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 03:59
CPC Classifications
C; C12; C12Y; C12Y304/00; C12Y304/21; C12Y304/21073; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/59; A61K47/60; A61P; A61P7/00; A61P7/02; C12N; C12N9/00; C12N9/14; C12N9/48; C12N9/50; C12N9/64; C12N9/6421; C12N9/6424; C12N9/6456; C12N9/6462; C12N9/96; A61K38/00
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
61 words
A derivative of a human-originated non-immunogenic plasminogen activator, comprising at least one polyalkylene glycol chemically bonded with at least one coupling agent to amino acid side chains of said plasminogen activator, wherein said polyalkylene glycol has a molecular weight in the range of 200-20,000 and is unsubstituted or is substituted with one or more alkyl or one or more alkanoyl groups.
Claim 2
Dependent Claim
61 words
A derivative of a human-originated non-immunogenic plasminogen activator, comprising at least one polyalkylene glycol chemically bonded with at least one coupling agent to amino acid side chains of said plasminogen activator, wherein said polyalkylene glycol has a molecular weight in the range of 200-20,000 and is unsubstituted or is substituted with one or more alkyl or one or more alkanoyl groups.
Claim 3
Dependent Claim
13 words
The derivative as claimed in claim 1, wherein said plasminogen activator is urokinase.
Claim 4
Dependent Claim
61 words
The derivative as claimed in claim 1, wherein said polyalkylene glycol is selected from the group consisting of an unsubstituted polyethylene glycol, a polyethylene glycol substituted with one or more alkyl or one or more alkanoyl groups, an unsubstituted polypropylene glycol, or a polypropylene glycol substituted with one or more alkyl or one or more alkanoyl groups, or a mixture thereof.
Claim 5
Dependent Claim
19 words
The derivative as claimed in claims 1 or 3, wherein said polyalkylene glycol is a polyethylene glycol monoalkyl ether.
Claim 6
Dependent Claim
17 words
The derivative as claimed in claims 1 or 3, wherein said polyalkylene glycol is a polypropylene glycol.
Claim 7
Dependent Claim
20 words
The derivative as claimed in claim 1, wherein said polyalkylene glycol has a molecular weight in the range of 500-10,000.
Claim 8
Dependent Claim
15 words
The derivative as claimed in claim 1, wherein said coupling agent is a cyanuric halide.
Claim 9
Dependent Claim
16 words
Monomethyl ether polyethylene glycol-4,6-dichloro-1,3,5-triazine-modified urokinase, whose polyethylene glycol moiety has an average molecular weight of 5,000.
Claim 10
Dependent Claim
16 words
Monomethyl ether polyethylene glycol-4,6-dichloro-1,3,5-triazine-modified urokinase, whose polyethylene glycol moiety has an average molecular weight of 5,000.
Claim 11
Dependent Claim
14 words
Polypropylene glycol-4-chloro-6-hydroxy-1,3,5-triazine-modified urokinase, whose polypropylene glycol moiety has an average molecular weight of 4,000.
Claim 12
Dependent Claim
14 words
Polypropylene glycol-4-chloro-6-hydroxy-1,3,5-triazine-modified urokinase, whose polypropylene glycol moiety has an average molecular weight of 4,000.
Claim 13
Dependent Claim
64 words
A process for preparing a derivative of a human-originated non-immunogenic plasminogen activator, which comprises reacting a coupled product of at least one polyalkylene glycol and at least one coupling agent with a plasminogen activator, wherein said polyalkylene glycol has a molecular weight in the range of 200-20,000 and is unsubstituted or is substituted with one or more alkyl or one or more alkanoyl groups.
Claim 14
Dependent Claim
64 words
A process for preparing a derivative of a human-originated non-immunogenic plasminogen activator, which comprises reacting a coupled product of at least one polyalkylene glycol and at least one coupling agent with a plasminogen activator, wherein said polyalkylene glycol has a molecular weight in the range of 200-20,000 and is unsubstituted or is substituted with one or more alkyl or one or more alkanoyl groups.
Claim 15
Dependent Claim
13 words
The process as claimed in claim 10, wherein said plasminogen activator is urokinase.
Claim 16
Dependent Claim
30 words
The process as claimed in claim 10, wherein said coupled product and said plasminogen activator are reacted under such conditions that the latter activator does not lose its physiological activity.
Claim 17
Dependent Claim
17 words
A thrombolytic agent comprising a derivative of a human-originated non-immunogenic plasminogen activator as claimed in claim 1.
Claim 18
Dependent Claim
51 words
The process as claimed in claim 12, wherein said conditions comprise reacting said coupled product and said plasminogen activator at a temperature in the range of 0° C. to room temperature at a pH in the range of 2 to 10, whereby said plasminogen activator does not lose its physiological activity.
Claim 19
Dependent Claim
64 words
A derivative of a human-originated non-immunogenic plasminogen activator, produced by a process which comprises reacting a coupled product of at least one polyalkylene glycol and at least one coupling agent with a plasminogen activator, wherein said polyalkylene glycol has a molecular weight in the range of 200-20,000 and is unsubstituted or is substituted with one or more alkyl or one or more alkanoyl groups.
Claim 20
Dependent Claim
64 words
A derivative of a human-originated non-immunogenic plasminogen activator, produced by a process which comprises reacting a coupled product of at least one polyalkylene glycol and at least one coupling agent with a plasminogen activator, wherein said polyalkylene glycol has a molecular weight in the range of 200-20,000 and is unsubstituted or is substituted with one or more alkyl or one or more alkanoyl groups.
Claim 21
Dependent Claim
29 words
The derivative as claimed in claim 15, wherein said coupled product and said plasminogen activator are reacted under conditions that the latter activator does not lose its physiological activity.
Claim 22
Dependent Claim
13 words
The derivative as claimed in claim 15, wherein said plasminogen activator is urokinase.
References Cited (Backward Citations)
US4179337A
Cited
US4349630A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-01-22 | 1988-07-23 | 1989-01-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-01-22 | 1992-07-23 | 1993-01-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-01-22 | 1996-07-23 | 1997-01-22 | $7700.00 | Window Closed / Lapsed |