US4609546A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Long-acting composition
Assignee: Japan Chemical Research Co Ltd
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Filing: 1983-06-23
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Granted: 1986-09-02
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Expires: 2003-06-23
Abstract
Abstract A composition wherein a physiologically active polypeptide or a glycoprotein of human origin, for instance, urokinase, kallikrein or leukocyte interferon, is coupled to a polyoxyethylene-polyoxypropylene copolymer. The composition is effective in the human body for a prolonged period of time.
Inventors
- 👤 Hajime Hiratani
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 12:00
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/59; A61K47/60; A61K38/00; A61K38/16; A61K38/17; A61K38/19; A61K38/21; A61K38/212; A61K38/43; A61K38/46; A61K38/48; A61K38/482; A61K38/4853; A61K38/49; C; C07; C07K; C07K17/00; C07K17/02; C07K17/06; C12; C12N; C12N11/00; C12N11/02; C12N11/08; C12N11/089; C12Y; C12Y304/00; C12Y304/21; C12Y304/21031; Y; Y10; Y10S; Y10S530/00; Y10S530/81; Y10S530/812; Y10S530/815
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
53 words
A long-acting composition which comprises a physiologically active polypeptide or glycoprotein of human origin coupled to a polyoxyethylene-polyoxypropylene copolymer having a molecular weight between about 1,000 and about 10,000 by means of a coupling agent capable of linking the terminal hydroxyl group of said copolymer with the amino group of said active substance.
Claim 2
Dependent Claim
53 words
A long-acting composition which comprises a physiologically active polypeptide or glycoprotein of human origin coupled to a polyoxyethylene-polyoxypropylene copolymer having a molecular weight between about 1,000 and about 10,000 by means of a coupling agent capable of linking the terminal hydroxyl group of said copolymer with the amino group of said active substance.
Claim 3
Dependent Claim
59 words
A composition according to claim 1 wherein the physiologically active polypeptide or glycoprotein of human origin is human menopausal gonadotropin, human growth hormone, epidermal growth factor, nerve growth factor, colony formation stimulating factor, urokinase, plasminogen (PLG), kallikrein, interferon α, interferonβ, interferonγ, interleukin 1, interleukin 2. urinary trypsin inhibitor, urinary thiol protease inhibitor, placental arylsulfatase, urinary lysozyme or urinary asparaginase.
Claim 4
Dependent Claim
37 words
A composition according to claim 1 wherein the copolymer has a molecular weight of between about 1,000 and about 10,000 having at both ends thereof hydroxyl groups which may be substituted by an alkyl or acyl group.
Claim 5
Dependent Claim
18 words
A composition according to claim 1 wherein the copolymer has a polyoxyethylene- polyoxypropylene ratio from 4:16 to 256:54.
Claim 6
Dependent Claim
36 words
A composition according to claim 1 wherein the copolymer is a monomethylation product of a polyoxyethylene-polyoxypropylene copolymer having an ethylene oxide: propylene oxide: ethylene oxide ratio of 46:16:46 and having an average molecular weight of 5,000.
Claim 7
Dependent Claim
29 words
A composition according to claim 1 wherein the copolymer is an ethyoxy-polyoxyethylene-polyoxypropylene glycol having an average molecular weight of 3,400 and an ethylene oxide:proplyene oxide:ethylene oxide ratio of 15:30:19.
Claim 8
Dependent Claim
36 words
A composition according to claim 1 wherein the coupling agent contains at least one functional group capable of reacting with a hydroxyl group and at least one functional group capable of reacting with an amino group.
Claim 9
Dependent Claim
17 words
A composition according to claim 1 wherein the coupling agent is 2,4,6-trichloro-s-triazine, dibromosuccinic anhydride or maleic anhydride.
Claim 10
Dependent Claim
67 words
A long-acting composition which comprises a physiologically active polypeptide or glycoprotein of human origin selected from the group of human epidermal growth factor, urokinase, kallikrein and leukocyte interferon, coupled to a polyoxyethylene-polyoxypropylene copolymer having a molecular weight between about 1,000 and about 10,000, by means of a coupling agent capable of linking the terminal hydroxyl group of said copolymer with the amino group of said active substance.
Claim 11
Dependent Claim
67 words
A long-acting composition which comprises a physiologically active polypeptide or glycoprotein of human origin selected from the group of human epidermal growth factor, urokinase, kallikrein and leukocyte interferon, coupled to a polyoxyethylene-polyoxypropylene copolymer having a molecular weight between about 1,000 and about 10,000, by means of a coupling agent capable of linking the terminal hydroxyl group of said copolymer with the amino group of said active substance.
Claim 12
Dependent Claim
37 words
A pharmaceutical composition useful for prolonging the effect of a physiologically active polypeptide or glycoprotein of human origin, comprised of a pharmaceutically effective prolonging amount of the long-acting composition of claim 1 and a pharmaceutically acceptable carrier.
Claim 13
Dependent Claim
37 words
A pharmaceutical composition useful for prolonging the effect of a physiologically active polypeptide or glycoprotein of human origin, comprised of a pharmaceutically effective prolonging amount of the long-acting composition of claim 2 and a pharmaceutically acceptable carrier.
Claim 14
Dependent Claim
37 words
A pharmaceutical composition useful for prolonging the effect of a physiologically active polypeptide or glycoprotein of human origin, comprised of a pharmaceutically effective prolonging amount of the long-acting composition of claim 9 and a pharmaceutically acceptable carrier.
Claim 15
Dependent Claim
39 words
A method for prolonging the effect of a physiologically active substance in the human body which comprises administering to said human body a pharmaceutically effective amount of the pharmaceutical composition of claim 10 which contains said physiologically active substance.
Claim 16
Dependent Claim
39 words
A method for prolonging the effect of a physiologically active substance in the human body which comprises administering to said human body a pharmaceutically effective amount of the pharmaceutical composition of claim 11 which contains said physiologically active substance.
Claim 17
Dependent Claim
39 words
A method for prolonging the effect of a physiologically active substance in the human body which comprises administering to said human body a pharmaceutically effective amount of the pharmaceutical composition of claim 12 which contains said physiologically active substance.
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) | 1989-09-01 | 1990-03-03 | 1990-09-02 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-09-01 | 1994-03-03 | 1994-09-02 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-09-01 | 1998-03-03 | 1998-09-02 | $7700.00 | Window Closed / Lapsed |