US4986980A
Expired / Lapsed
US
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Water-soluble, carrier-bound paramagnetic metal containing diagnostic agents
Assignee: GE Healthcare AS
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Filing: 1985-11-01
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Granted: 1991-01-22
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Expires: 2005-11-01
Abstract
Abstract There is disclosed a diagnostic agent containing a non-radioactive paramagnetic metal species which agent comprises a physiologically tolerable, water-soluble, hydroxyl group-containing macromolecular product to which is chemically bound said metal species, said product consisting essentially of at least one polymeric or polymerized carbohydrate or polymerized sugar alcohol or derivative thereof.
Inventors
- 👤 Trond Jacobsen
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 23:20
CPC Classifications
A; A61; A61K; A61K49/00; A61K49/06; A61K49/08; A61K49/085; A61K49/10; A61K49/12; A61K49/126; C; C08; C08B; C08B37/00; C08B37/0006; C08B37/0009; C08B37/0021; Y; Y10; Y10S; Y10S436/00; Y10S436/806; Y10T; Y10T436/00; Y10T436/24
Claims Analysis
Total Claims: 37
Claim 1
Independent Claim
75 words
A diagnostic agent comprising a water-soluble macromolecular complex of a non-radioactive paramagnetic metal ion, wherein said agent comprises a physiologically tolerable, water-soluble, hydroxyl group-containing macromolecular product of weight average molecular weight (M w ) of at least 30,000 to which is bound in a coordination complex at least one said non-radioactive paramagnetic metal ion, said macromolecular product comprising at least one material selected from the group consisting of polysaccharides, polymerized sugar alcohols and derivatives thereof.
Claim 2
Dependent Claim
75 words
A diagnostic agent comprising a water-soluble macromolecular complex of a non-radioactive paramagnetic metal ion, wherein said agent comprises a physiologically tolerable, water-soluble, hydroxyl group-containing macromolecular product of weight average molecular weight (M w ) of at least 30,000 to which is bound in a coordination complex at least one said non-radioactive paramagnetic metal ion, said macromolecular product comprising at least one material selected from the group consisting of polysaccharides, polymerized sugar alcohols and derivatives thereof.
Claim 3
Dependent Claim
19 words
A diagnostic agent according to claim 1 wherein said macromolecular product is a material degradable in the animal body.
Claim 4
Dependent Claim
17 words
A diagnostic agent according to claim 1 wherein said macromolecular product is a material degradable by hydrolases.
Claim 5
Dependent Claim
27 words
A diagnostic agent according to claim 1 wherein said non-radioactive paramagnetic metal is selected from the group of elements having atomic numbers 21-29, 42, 44 and 57-70.
Claim 6
Dependent Claim
30 words
A diagnostic agent according to claim 4 wherein said non-radioactive paramagnetic metal is selected from the group consisting of gadolinium, erbium, europium, dysprosium, holmium, manganese, iron, nickel, chromium and copper.
Claim 7
Dependent Claim
26 words
A diagnostic agent according to claim 1 wherein said non-radioactive paramagnetic metal ion is bound to said macromolecular product in the form of a chelate complex.
Claim 8
Dependent Claim
16 words
A diagnostic agent according to claim 1 further comprising at least one pharmaceutical carrier or excipient.
Claim 9
Dependent Claim
20 words
A diagnostic agent according to claim 7 in solution form further comprising a viscosity enhancing agent and/or an osmolality regulator.
Claim 10
Dependent Claim
45 words
A diagnostic agent according to claim 1 wherein the molecular weight of said macromolecular product is sufficient to prevent rapid excretion of said paramagnetic metal ion from the blood into the urine, the weight average molecular weight of said macromolecular product being at least 40000.
Claim 11
Dependent Claim
45 words
A diagnostic agent according to claim 1 wherein the molecular weight of said macromolecular product is sufficient to prevent rapid excretion of said paramagnetic metal ion from the blood into the urine, the weight average molecular weight of said macromolecular product being at least 50000.
Claim 12
Dependent Claim
21 words
A diagnostic agent according to claim 1 wherein the weight average molecular weight of said macromolecular product is lower than 200000.
Claim 13
Dependent Claim
15 words
A diagnostic agent according to claim 1 wherein said macromolecular product comprises a polysaccharide material.
Claim 14
Dependent Claim
21 words
A diagnostic agent according to claim 1 wherein said macromolecular product comprises a material selected from dextrans, starches and derivatives thereof.
Claim 15
Dependent Claim
13 words
A diagnostic agent according to claim 5 wherein said paramagnetic metal is gadolinium.
Claim 16
Dependent Claim
38 words
A diagnostic agent according to claim 6 wherein said paramagnetic metal ion is bound in a chelate complex wherein one of the metal coordinating atoms is a nitrogen atom, one other being a nitrogen, oxygen or sulphur atom.
Claim 17
Dependent Claim
39 words
A diagnostic agent according to claim 6 wherein said paramagnetic metal ion is bound in a chelate complex by a chelate forming group which is itself bound to the basic molecule of the macromolecular product by a bridging group.
Claim 18
Dependent Claim
32 words
A diagnostic agent according to claim 6 wherein said paramagnetic metal ion is bound in a chelate complex by a chelate forming group which is a aminopolycarboxylic acid or a derivative thereof.
Claim 19
Dependent Claim
20 words
A diagnostic agent according to claim 16 wherein said chelate forming group is a aminopolycarboxylic acid or a derivative thereof.
Claim 20
Dependent Claim
64 words
A diagnostic agent comprising a water-soluble, macromolecular complex of a non-radioactive paramagnetic metal ion, wherein said agent comprises a physiologically tolerable, water-soluble, hydroxyl group-containing, macromolecular product to which is bound at least one said non-radioactive paramagnetic metal ion, said paramagnetic metal ion being complexed by diethylenetriamine-pentaacetic acid coupled to dextran of weight average molecular weight of about 40000 and said paramagnetic metal being gadolinium.
Claim 21
Dependent Claim
64 words
A diagnostic agent comprising a water-soluble, macromolecular complex of a non-radioactive paramagnetic metal ion, wherein said agent comprises a physiologically tolerable, water-soluble, hydroxyl group-containing, macromolecular product to which is bound at least one said non-radioactive paramagnetic metal ion, said paramagnetic metal ion being complexed by diethylenetriamine-pentaacetic acid coupled to dextran of weight average molecular weight of about 40000 and said paramagnetic metal being gadolinium.
Claim 22
Dependent Claim
65 words
A diagnostic agent comprising a water-soluble, macromolecular complex of a non-radioactive paramagnetic metal ion, wherein said agent comprises a physiologically tolerable, water-soluble, hydroxyl group-containing, macromolecular product to which is bound at least one said non-radioactive paramagnetic metal ion, said paramagnetic metal ion being complexed by triethylene tetraaminehexaacetic acid coupled to dextran of weight average molecular weight of about 40000 and said paramagnetic metal being gadolinium.
Claim 23
Dependent Claim
65 words
A diagnostic agent comprising a water-soluble, macromolecular complex of a non-radioactive paramagnetic metal ion, wherein said agent comprises a physiologically tolerable, water-soluble, hydroxyl group-containing, macromolecular product to which is bound at least one said non-radioactive paramagnetic metal ion, said paramagnetic metal ion being complexed by triethylene tetraaminehexaacetic acid coupled to dextran of weight average molecular weight of about 40000 and said paramagnetic metal being gadolinium.
Claim 24
Dependent Claim
64 words
A diagnostic agent comprising a water-soluble, macromolecular complex of a non-radioactive paramagnetic metal ion, wherein said agent comprises a physiologically tolerable, water-soluble, hydroxyl group-containing, macromolecular product to which is bound at least one said non-radioactive paramagnetic metal ion, said paramagnetic metal ion being complexed by diethylenetriamine-pentaacetic acid coupled to dextran of weight average molecular weight of about 70000 and said paramagnetic metal being gadolinium.
Claim 25
Dependent Claim
64 words
A diagnostic agent comprising a water-soluble, macromolecular complex of a non-radioactive paramagnetic metal ion, wherein said agent comprises a physiologically tolerable, water-soluble, hydroxyl group-containing, macromolecular product to which is bound at least one said non-radioactive paramagnetic metal ion, said paramagnetic metal ion being complexed by diethylenetriamine-pentaacetic acid coupled to dextran of weight average molecular weight of about 70000 and said paramagnetic metal being gadolinium.
Claim 26
Dependent Claim
69 words
A diagnostic agent comprising a water-soluble, macromolecular complex of a non-radioactive paramagnetic metal ion, wherein said agent comprises a physiologically tolerable, water-soluble, hydroxyl group-containing, macromolecular product to which is bound at least one said non-radioactive paramagnetic metal ion, said paramagnetic metal ion being complexed by 1,4,7,10-tetraazacyclododecane-N,N',N", N"'-tetraacetic acid coupled by a glycine residue to dextran of weight average molecular weight of about 40000 and said paramagnetic metal being gadolinium.
Claim 27
Dependent Claim
69 words
A diagnostic agent comprising a water-soluble, macromolecular complex of a non-radioactive paramagnetic metal ion, wherein said agent comprises a physiologically tolerable, water-soluble, hydroxyl group-containing, macromolecular product to which is bound at least one said non-radioactive paramagnetic metal ion, said paramagnetic metal ion being complexed by 1,4,7,10-tetraazacyclododecane-N,N',N", N"'-tetraacetic acid coupled by a glycine residue to dextran of weight average molecular weight of about 40000 and said paramagnetic metal being gadolinium.
Claim 28
Dependent Claim
49 words
A diagnostic agent according to claim 1 whereof the said paramagnetic metal ion has a specific relaxation rate, T 1 , enhancement of at least 0.01s -1 /mM of said paramagnetic metal ion measured at 10 MHz in a 1:2.13 by volume glycerol and water mixture at 37° C.
Claim 29
Dependent Claim
20 words
A diagnostic agent according to claim 6 wherein said chelate complex is uncharged on dissolution in a neutral aqueous medium.
Claim 30
Dependent Claim
23 words
A diagnostic agent according to claim 24, comprising Cu(II) bound in a chelate complex by the residue of S-acetylmercaptosuccinic acid coupled to thioldextran.
Claim 31
Dependent Claim
24 words
A diagnostic agent according to claim 24 comprising Gd(III) bound in a chelate complex by the residue of ethylenediaminetetraacetic acid coupled by hydroxypropyl starch.
Claim 32
Dependent Claim
41 words
A diagnostic agent according to claim 1 wherein said macromolecular product comprises at least one material selected from the group consisting of starches, alpha-amylase degradable polysaccharides and alpha-amylase degradable derivatives thereof having an average degree of substitution of less than 0.6.
Claim 33
Independent Claim
119 words
A method of imaging a human or non-human animal body, which method comprises administering to a human or non-human animal body or to a selected region thereof a diagnostically effective amount of a diagnostic agent comprising a water-soluble macromolecular complex of a non-radioactive paramagnetic metal ion and generating an NMR or ultrasound image of said body or said region, wherein said agent comprises a physiologically tolerable, water-soluble, hydroxyl group-containing macromolecular product of weight average molecular weight (M w ) of at least 30,000 to which is bound in a coordination at least one said non-radioactive paramagnetic metal ion, said macromolecular product comprising at least one material selected from the group consisting of polysaccharides, polymerized sugar alcohols and derivatives thereof.
Claim 34
Independent Claim
119 words
A method of imaging a human or non-human animal body, which method comprises administering to a human or non-human animal body or to a selected region thereof a diagnostically effective amount of a diagnostic agent comprising a water-soluble macromolecular complex of a non-radioactive paramagnetic metal ion and generating an NMR or ultrasound image of said body or said region, wherein said agent comprises a physiologically tolerable, water-soluble, hydroxyl group-containing macromolecular product of weight average molecular weight (M w ) of at least 30,000 to which is bound in a coordination at least one said non-radioactive paramagnetic metal ion, said macromolecular product comprising at least one material selected from the group consisting of polysaccharides, polymerized sugar alcohols and derivatives thereof.
Claim 35
Dependent Claim
22 words
A method of imaging according to claim 28 wherein the weight average molecular weight of said macromolecular product is at least 40,000.
Claim 36
Dependent Claim
14 words
A method of imaging according to claim 28 wherein said paramagnetic metal is gadolinium.
Claim 37
Dependent Claim
14 words
A method of imaging according to claim 29 wherein said paramagnetic metal is gadolinium.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1994-01-21 | 1994-07-23 | 1995-01-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-01-21 | 1998-07-23 | 1999-01-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-01-21 | 2002-07-23 | 2003-01-22 | $7700.00 | Window Closed / Lapsed |