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Hybrid magnetic resonance contrast agents

Assignee: ImaRx Therapeutics Inc
•
Filing: 1994-02-28
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Granted: 1995-04-18
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Expires: 2014-02-28
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Abstract

Abstract Novel MRI contrast agents that comprise one or more metal-ion chelates in juxtaposition with one or more free-radical nitroxide compounds in a polymeric or oligomeric molecule. Both the chelate units and the free radical units may, independently, be inside the main chain of the polymer or in a side chain of the linkage portion of the polymer. The number of combined units of chelates and free radicals in the polymer or oligomer is at least two.

Inventors

  • 👤 Evan C. Unger
  • 👤 Guanli Wu

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-10 02:06
CPC Classifications
G; G01; G01R; G01R33/00; G01R33/20; G01R33/44; G01R33/48; G01R33/54; G01R33/56; G01R33/5601; A; A61; A61B; A61B90/00; A61B90/39; A61K; A61K49/00; A61K49/06; A61K49/08; A61K49/10; A61K49/101; A61K49/103; A61K49/12; A61K49/122; A61K49/126; A61K49/128; A61K49/20; A61K51/00; A61K51/02; A61K51/04; A61K51/06; C; C08; C08G; C08G63/00; C08G63/68; C08G69/00; C08G69/40; C08G69/48; C08G79/00; A61B2090/3954; A61K2123/00

Claims Analysis

Total Claims: 88
Claim 1
Independent Claim 65 words
A hybrid, copolymeric magnetic-resonance-imaging contrast agent comprising: at least one chelating unit monomer; at least one free radical monomer linked to said at least one chelating unit monomer; and at least one paramagnetic ion combined with at least one of said at least one chelating unit monomer; wherein said chelating unit monomer is a polynitrilo chelating agent and said free radical monomer is a nitroxide.
Claim 2
Dependent Claim 65 words
A hybrid, copolymeric magnetic-resonance-imaging contrast agent comprising: at least one chelating unit monomer; at least one free radical monomer linked to said at least one chelating unit monomer; and at least one paramagnetic ion combined with at least one of said at least one chelating unit monomer; wherein said chelating unit monomer is a polynitrilo chelating agent and said free radical monomer is a nitroxide.
Claim 3
Dependent Claim 173 words
The contrast agent of claim 1, having the following structure: ##STR36## wherein Ch is a polynitrilo chelating unit monomer, L is a linker monomer, FR is a nitroxide free radical monomer, and M is a paramagnetic ion; wherein q=1 to 10,000; wherein, within each of the q polymeric groups ##STR37## independently, p=0 to 10,000 and p'=0 to 10,000; wherein, within each of the p oligomeric groups ##STR38## independently, n=0 to 10,000 and j=0 to 10,000; for each group of paramagnetic ions ##STR39## chelated by each of the n chelating unit monomers --Ch-- in the p oligomeric groups, independently, k=0 to 2; and for each group of free radical monomers ##STR40## linked to each of the j linker monomers --L-- in the p oligomeric groups, independently, m=0 to 2; and wherein, within each of the p' oligomeric groups ##STR41## independently, n=0 to 10,000 and m=0 to 10,000; and for each group of paramagnetic ions ##STR42## chelated by each of the n chelating unit monomers --Ch-- in the p' oligomeric groups, independently, k=0 to 2.
Claim 4
Dependent Claim 51 words
The contrast agent of claim 1, wherein each polynitrilo chelating agent comprises at least one COOH, COOR 1 , or COZ group; each R 1 being, independently, a C1-C20 substituted or unsubstituted, saturated or unsaturated, alkyl or cycloalkyl group or an anhydride; and each Z being, independently, Cl, Br, or I.
Claim 5
Dependent Claim 42 words
The contrast agent of claim 3, wherein at least one of said C1-C20 alkyl or cycloalkyl group is substituted with at least one moiety selected from the group of OH, NH 2 , SH, COOH, and PO 4 , or mixtures thereof.
Claim 6
Dependent Claim 18 words
The contrast agent of claim 3, wherein each R 1 is, independently, a polyhydroxy-substituted alkyl or cycloalkyl group.
Claim 7
Dependent Claim 30 words
The contrast agent of claim 5, wherein said polyhydroxy-substituted alkyl or cycloalkyl group is selected from the group consisting of sugar alcohols, monosaccharides, polysaccharides, and synthetic polymers, or mixtures thereof.
Claim 8
Dependent Claim 57 words
The contrast agent of claim 1, wherein each polynitrilo chelating unit monomer consists, independently, of a chelating agent selected from the group consisting of ethylenediamine tetraacetic acid; diethylenetriamine pentaacetic acid; 1,5-di-methoxyethylene-iminocarbonyl-methylene-1,3,5-tricarboxymethylene-1,3,5,-triazapentane; 1,5-di-α,-dihydroxypropeneimino-carbonyl-methylene-1,3,5-tricarboxymethylene-1,3,5-triazapentane; 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid; 1,4,7,10-tetraazacyclododecane-N,N',N"-triacetic acid; 3,6,9-triaza-12-oxa-3,6,9-tricarboxymethylene-10-carboxy-13-phenyl-tridecanoic acid; hydroxybenzyl-ethylenediamine diacetic acid; N,N'-bis(pyridoxyl-5-phosphate)ethylenediamine-N,N'-diacetic acid; 1,4,7-triazacyclononane-N,N',N"-triacetic acid; 1-oxa-4,7,10-triazacyclododecane-triacetic acid; 1,4,8,11-tetraazacyclotetradecane-N,N',N",N'"-tetraacetic acid; triethylenetetraamine hexaacetic acid; 1,2-diaminocyclohexane-N,N,N',N'-tetraacetic acid; and anhydrides thereof.
Claim 9
Dependent Claim 25 words
The contrast agent of claim 1, wherein each free radical monomer is selected from the group consisting of heterocyclic nitroxide monomers and non-heterocyclic nitroxide monomers.
Claim 10
Dependent Claim 104 words
The contrast agent of claim 8, wherein said heterocyclic nitroxide monomers have the following general structure: ##STR43## wherein a five member ring is pyrrolidine, oxazolidine, imidazolidine, or thiazolidine; a six member ring is piperidine; and each of Ra, Rb, Rc and Rd is, independently, a C1-C20 alkyl or cycloalkyl group, said alkyl or cycloalkyl group being interrupted or terminated with OH, SH, NH 2 , NHR 1 , COOH, COOR 1 , NCS, COCHCH 2 , or COZ, each R 1 being, independently, a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group or an anhydride, and each Z being, independently, Cl, Br, or I.
Claim 11
Dependent Claim 22 words
The contrast agent of claim 8, wherein said non-heterocyclic nitroxide monomers are selected from the group consisting of diphenylnitroxide and di-tert-butyl nitroxide.
Claim 12
Dependent Claim 81 words
The contrast agent of claim 1, wherein each nitroxide free radical monomer is selected from the group consisting of 2,2,6,6-tetramethylpiperidine-1-oxyl; 2,2,4,4-tetramethyl-pyrrolidine-1-oxyl; 2,2,4,4-tetramethyl-imidazolidine-3-oxyl; 2,2,4,4-tetramethyl-1,3-thiazolidine-3-oxyl; 2,2,4,4-tetramethyl-1,3-oxazolidine-3-oxyl; 2,2,6,6-tetramethylpyrimidine-1-oxyl; diphenyl-nitroxide; and di-tert-butylnitroxide; and wherein each nitroxide may have one or more OH, SH, NH 2 , NHR 1 , COOH, COOR 1 , NCS, COCHCH 2 , or COZ, each R 1 being, independently, a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group or an anhydride, and each Z being, independently, Cl, Br, or I.
Claim 13
Dependent Claim 36 words
The contrast agent of claim 1, wherein each nitroxide free radical monomer is a monofunctionalized compound selected from the group consisting of 1-oxyl-2,2,6,6-tetramethyl-4-piperidinyl acrylate; 4-(iodomethylenecarbonylimino)-2,2,6,6-tetramethyl-piperdinyl-1-oxy; 4-(bromomethylenecarbonylimino)-2,2,6,6-tetramethyl-piperidinyl-1-oxy; 3-carboxy-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 3-chlorocarbonyl-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 3-aminomethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 3-hydroxymethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 3-hydroxy-2,2,5,5-tetramethylpyrrolidine-1-oxyl; 3-chloroformyl-2,2,5,5-tetramethylpyrrolidine-1-oxyl; 4-amino-2,2,6,6-tetramethylpiperidine-1-oxyl; 4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl; and 3-thiocabamoylmethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxy.
Claim 14
Dependent Claim 36 words
The contrast agent of claim 1, wherein each nitroxide free radical monomer is a difunctionalized compound selected from the group consisting of cis-1-oxyl-2,2,5,5-tetramethylpyrrolidine; trans-1-oxyl-2,2,5,5-tetramethylpyrrolidine; 3-amino-4-aminomethylene-2,2,5,5-tetramethylpyrrolidine; cis-2,5-dimethyl-2(aminomethyl)-5-(2-carboxyethyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2-(hydroxymethyl)-5-(methoxycarbonylmethyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2-(hydroxymethyl)-5-(2-hydroxyhexyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2,5-bis(3-hydroxypropyl)-pyrrolidinyl-1-oxy; trans-2,5-dimethyl-2,5-bis(3-hydroxypropyl)-pyrrolidinyl-1-oxy; trans-2,5-dimethyl-2,5-bis(2-carboxyethyl)-pyrrolidinyl-1-oxy; cis-2,5-dimethyl-2,5-bis(2-hydroxy-5-methylphenyl)-tetrahydroxypyrrol-1-oxy; 3-amino-4-carboxy-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 2,5-di-tertbutyl-3,4-diethyloxycarbonyl-pyrrol-1-oxyl; and 1,4-bis(4-hydroxy-2,2,6,6-tetramethyl-1-oxyl-4-piperidyl)-butane.
Claim 15
Dependent Claim 21 words
The contrast agent of claim 1, wherein each paramagnetic ion is selected from the group consisting of transition and lanthanide elements.
Claim 16
Dependent Claim 31 words
The contrast agent of claim 1, wherein each paramagnetic ion is selected from the group consisting of Gd(III), Mn(II), Cu(II), Cr(III), Fe(II), Fe(III), Co(II), Er(II), Ni(II), Eu(III), Dy(III), Yb(III), and Ho(III).
Claim 17
Dependent Claim 21 words
The contrast agent of claim 1, wherein each paramagnetic ion is selected from the group consisting of Gd(III), Mn(II) and Fe(III).
Claim 18
Dependent Claim 127 words
The contrast agent of claim 2, wherein each linker monomer has the following general structure: X.sub.1 [(CHR.sub.2).sub.m --CHR.sub.2 --Y].sub.n --G.sub.q --(CHR.sub.2).sub.m' --CHR.sub.2 --X.sub.2 wherein each R 2 is, independently, a C1-C20 substituted or unsubstituted, saturated or unsaturated, alkyl or cycloalkyl group; X 1 and X 2 are, independently, OH, NH 2 , NHR 1 , COOH, COOR 1 , SH, Z or NCS; Y is O, NH, NR 1 , S or CO; each R 1 is, independently, a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group or an anhydride; each Z is, independently, Cl, Br, or I; G is a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group, a saccharide, a peptide or a polysulfide; and m, m', n, and q are, independently, 0 to 10,000.
Claim 19
Dependent Claim 43 words
The contrast agent of claim 17, wherein each linker monomer is, independently, a polyamino linker monomer selected from the group consisting of 1,2-diaminoethane, 13-diaminopropane, 1,4-diaminobutane, 1,5-diamino-3-(2-aminoethyl)-pentane, N,N'-dimethyl-1,2-diaminoethane, N,N'-dimethyl-1,3-diaminopropane, 2-hydroxy-1,3-diaminopropane, 2-amino-1,3-diaminopropane, 2,3-diamino-1,4-butanediol, 1,4-diamino-2,3-butane diol, 1,4-diaminocyclohexane, 1,4-phenylenediamine, 1,1,1-tris(aminomethyl)ethane, 2,2',2"-tris-aminoethylamine, tris(aminomethylene)methane, diethylenetriamine, triethylenetetraamine, 1,3,5-triaminocyclohexane, and 1,3,5-triaminobenzene.
Claim 20
Dependent Claim 36 words
The contrast agent of claim 17, wherein each linker monomer is a polyhydroxy linker monomer selected from the group consisting of 2,2-dimethyl-1,3-propanediol, tris-(2-hydroxyethyl)amine, 1,1,1-tris-(hyroxymethylene)ethane, glycerine, erythritol, sugar alcohols, polyethyleneglycol, w-amino-polyethyleneglycol, N-substituted-w-aminopolyethyleneglycol, w-thiol-polyethyleneglycol, polysulfide-blocked polyethyleneglycol, and polyethylene-imine.
Claim 21
Dependent Claim 21 words
The contrast agent of claim 17, wherein each linker monomer is selected from the group consisting of ethylenedioxydiethylamine, N,N'-bis-dihydroxypropylethylenedioxydiethylamine, and ethylenedioxydiethylmercaptane.
Claim 22
Dependent Claim 52 words
The contrast agent of claim 2, wherein each polynitrilo chelating unit monomer comprises at least one COOH, COOR 1 , or COZ group; each R 1 being, independently, a C1-C20 substituted or unsubstituted, saturated or unsaturated, alkyl or cycloalkyl group or an anhydride; and each Z being, independently, Cl, Br, or I.
Claim 23
Dependent Claim 42 words
The contrast agent of claim 21, wherein at least one of said C1-C20 alkyl or cycloalkyl group is substituted with at least one moiety selected from the group of OH, NH 2 , SH, COOH, and PO 4 , or mixtures thereof.
Claim 24
Dependent Claim 18 words
The contrast agent of claim 21, wherein each R 1 is, independently, a polyhydroxy-substituted alkyl or cycloalkyl group.
Claim 25
Dependent Claim 27 words
The contrast agent of claim 23, wherein said polyhydroxy-substituted alkyl or cycloalkyl group is selected from the group consisting of sugar alcohols, monosaccharides, polysaccharides, and synthetic polymers.
Claim 26
Dependent Claim 57 words
The contrast agent of claim 2, wherein each polynitrilo chelating unit monomer consists, independently, of a chelating agent selected from the group consisting of ethylenediamine tetraacetic acid; diethylenetriamine pentaacetic acid; 1,5-di-methoxyethylene-iminocarbonyl-methylene-1,3,5-tricarboxymethylene-1,3,5,-triazapentane; 1,5-di-α,-dihydroxypropeneimino-carbonyl-methylene-1,3,5-tricarboxymethylene-1,3,5-triazapentane; 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid; 1,4,7,10-tetraazacyclododecane-N,N',N"-triacetic acid; 3,6,9-triaza-12-oxa-3,6,9-tricarboxymethylene-10-carboxy-13-phenyl-tridecanoic acid; hydroxybenzyl-ethylenediamine diacetic acid; N,N'-bis(pyridoxyl-5-phosphate)ethylenediamine-N,N'-diacetic acid; 1,4,7-triazacyclononane-N,N',N"-triacetic acid; 1-oxa-4,7,10-triazacyclododecane-triacetic acid; 1,4,8,11-tetraazacyclotetradecane-N,N',N",N'"-tetraacetic acid; triethylenetetraamine hexaacetic acid; 1,2-diaminocyclohexane-N,N,N',N'-tetraacetic acid; and anhydrides thereof.
Claim 27
Dependent Claim 26 words
The contrast agent of claim 2, wherein each free radical monomer, independently, is selected from the group consisting of heterocyclic nitroxide monomers and non-heterocyclic nitroxide monomers.
Claim 28
Dependent Claim 104 words
The contrast agent of claim 26, wherein said heterocyclic nitroxide monomers have the following general structure: ##STR44## wherein a five member ring is pyrrolidine, oxazolidine, imidazolidine, or thiazolidine; a six member ring is piperidine; and each of Ra, Rb, Rc and Rd is, independently, a C1-C20 alkyl or cycloalkyl group, said alkyl or cycloalkyl group being interrupted or terminated with OH, SH, NH 2 , NHR 1 , COOH, COOR 1 , NCS, COCHCH 2 , or COZ, each R 1 being, independently, a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group or an anhydride, and each Z being, independently, Cl, Br, or I.
Claim 29
Dependent Claim 22 words
The contrast agent of claim 26, wherein said non-heterocyclic nitroxide monomers are selected from the group consisting of diphenylnitroxide and di-tert-butyl nitroxide.
Claim 30
Dependent Claim 82 words
The contrast agent of claim 2, wherein each nitroxide free radical monomer is, independently, selected from the group consisting of 2,2,6,6-tetramethylpiperidine-1-oxyl; 2,2,4,4-tetramethyl-pyrrolidine-1-oxyl; 2,2,4,4-tetramethylimidazolidine-3-oxyl; 2,2,4,4-tetramethyl-1,3-thiazolidine-3-oxyl; 2,2,4,4-tetramethyl-1,3-oxazolidine-3-oxyl; 2,2,6,6-tetramethylpyrimidine-1-oxyl; diphenyl-nitroxide; and di-tertbutylnitroxide; and wherein each nitroxide may have one or more OH, SH, NH 2 , NHR 1 , COOH, COOR 1 , NCS, COCHCH 2 , or COZ, each R 1 being, independently, a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group or an anhydride, and each Z being, independently, Cl, Br, or I.
Claim 31
Dependent Claim 37 words
The contrast agent of claim 2, wherein each nitroxide free radical monomer is, independently, a monofunctionalized compound selected from the group consisting of 1-oxyl-2,2,6,6-tetramethyl-4-piperidinyl acrylate; 4-(iodomethylenecarbonylimino)-2,2,6,6-tetramethyl-piperdinyl-1-oxy; 4-(bromomethylenecarbonylimino)-2,2,6,6-tetramethyl-piperidinyl-1-oxy; 3-carboxy-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 3-chlorocarbonyl-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 3-aminomethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 3-hydroxymethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxyl; 3-hydroxy-2,2,5,5-tetramethylpyrrolidine-1-oxyl; 3-chloroformyl-2,2,5,5-tetramethylpyrrolidine-1-oxyl; 4-amino-2,2,6,6-tetramethylpiperidine-1-oxyl; 4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl; and 3-thiocabamoylmethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxy.
Claim 32
Dependent Claim 37 words
The contrast agent of claim 2, wherein each nitroxide free radical monomer is, independently, a difunctionalized compound selected from the group consisting of cis-1-oxyl-2,2,5,5-tetramethylpyrrolidine; trans-1-oxyl-2,2,5,5-tetramethylpyrrolidine; 3-amino-4-aminomethylene-2,2,5,5-tetramethylpyrrolidine; cis-2,5-dimethyl-2(aminomethyl)-5-(2-carboxyethyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2-(hydroxymethyl)-5-(methoxycarbonylmethyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2-(hydroxymethyl)-5-(2-hydroxyhexyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2,5-bis(3-hydroxypropyl)-pyrrolidinyl-1-oxy; trans-2,5-dimethyl-2,5-bis(3-hydroxypropyl)-pyrrolidinyl-1-oxy; trans-2,5-dimethyl-2,5-bis(2-carboxyethyl)-pyrrolidinyl-1-oxy; cis-2,5-dimethyl-2,5-bis(2-hydroxy-5-methylphenyl)-tetrahydroxypyrrol-1-oxy; 3-amino-4-carboxy-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 2,5-di-tert-butyl-3,4-diethyloxycarbonyl-pyrrol-1-oxyl; and 1,4-bis(4-hydroxy-2,2,6,6-tetramethyl-1-oxyl-4-piperidyl)-butane.
Claim 33
Dependent Claim 21 words
The contrast agent of claim 2, wherein each paramagnetic ion is selected from the group consisting of transition and lanthanide elements.
Claim 34
Dependent Claim 31 words
The contrast agent of claim 2, wherein each paramagnetic ion is selected from the group consisting of Gd(III), Mn(II), Cu(II), Cr(III), Fe(II), Fe(III), Co(II), Er(II), Ni(II), Eu(III), Dy(III), Yb(III), and Ho(III).
Claim 35
Dependent Claim 21 words
The contrast agent of claim 2, wherein each paramagnetic ion is selected from the group consisting of Gd(III), Mn(II) and Fe(III).
Claim 36
Dependent Claim 166 words
The contrast agent of claim 1, having the following structure: ##STR45## wherein Ch is a polynitrilo chelating unit monomer, L is a linker monomer, FR is a nitroxide free radical monomer, and M is a paramagnetic ion; wherein, independently, p=1 to 10,000 and p'=1 to 10,000; wherein, within each of the p oligomeric groups ##STR46## independently, n=0 to 10,000 and j=0 to 10,000; for each group of paramagnetic ions ##STR47## chelated by each of the n chelating unit monomers --Ch-- in each of the p oligomeric groups, independently, k=0 to 2; and for each group of free radical monomers ##STR48## linked to each of the j linker monomers --L-- in each of the oligomeric groups, independently, m=0 to 2; and wherein, within each of the p' oligomeric groups ##STR49## independently, n=0 to 10,000 and m=0 to 10,000; and for each group of paramagnetic ions ##STR50## chelated by each of the n chelating unit monomers --Ch-- in each of the p' oligomeric groups, independently, k=0 to 2.
Claim 37
Dependent Claim 127 words
The contrast agent of claim 35, wherein each linker monomer has the following general structure: X.sub.1 [(CHR.sub.2).sub.m --CHR.sub.2 --Y].sub.n --G.sub.q --(CHR.sub.2).sub.m' --CHR.sub.2 --X.sub.2 wherein each R 2 is, independently, a C1-C20 substituted or unsubstituted, saturated or unsaturated, alkyl or cycloalkyl group; X 1 and X 2 are, independently, OH, NH 2 , NHR 1 , COOH, COOR 1 , SH, Z or NCS; Y is O, NH, NR 1 , S or CO; each R 1 is, independently, a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group or an anhydride; each Z is, independently, Cl, Br, or I; G is a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group, a saccharide, a peptide or a polysulfide; and m, m', n, and q are, independently, 0 to 10,000.
Claim 38
Dependent Claim 43 words
The contrast agent of claim 36, wherein each linker monomer is, independently, a polyamino linker monomer selected from the group consisting of 1,2-diaminoethane, 13-diaminopropane, 1,4-diaminobutane, 1,5-diamino-3-(2-aminoethyl)-pentane, N,N'-dimethyl-1,2-diaminoethane, N,N'-dimethyl-1,3-diaminopropane, 2-hydroxy-1,3-diaminopropane, 2-amino-1,3-diaminopropane, 2,3-diamino-1,4-butanediol, 1,4-diamino-2,3-butane diol, 1,4-diaminocyclohexane, 1,4-phenylenediamine, 1,1,1-tris-(aminomethyl)ethane, 2,2',2"-tris-aminoethylamine, tris-(aminomethylene)methane, diethylenetriamine, triethylenetetraamine, 1,3,5-triaminocyclohexane, and 1,3,5-triaminobenzene.
Claim 39
Dependent Claim 36 words
The contrast agent of claim 36, wherein each linker monomer is a polyhydroxy linker monomer selected from the group consisting of 2,2-dimethyl-1,3-propanediol, tris-(2-hydroxyethyl)amine, 1,1,1-tris-(hyroxymethylene)ethane, glycerine, erythritol, sugar alcohols, polyethyleneglycol, w-amino-polyethyleneglycol, N-substituted-w-aminopolyethyleneglycol, w-thiol-polyethyleneglycol, polysulfide-blocked polyethyleneglycol, and polyethylene-imine.
Claim 40
Dependent Claim 21 words
The contrast agent of claim 36, wherein each linker monomer is selected from the group consisting of ethylenedioxydiethylamine, N,N'-bis-dihydroxypropylethylenedioxydiethylamine, and ethylenedioxydiethylmercaptane.
Claim 41
Dependent Claim 52 words
The contrast agent of claim 35, wherein each polynitrilo chelating unit monomer comprises at least one COOH, COOR 1 , or COZ group; each R 1 being independently, a C1-C20 substituted or unsubstituted, saturated or unsaturated, alkyl or cycloalkyl group or an anhydride; and each Z being, independently, Cl, Br, or I.
Claim 42
Dependent Claim 42 words
The contrast agent of claim 40, wherein at least one of said C1-C20 alkyl or cycloalkyl group is substituted with at least one moiety selected from the group of OH, NH 2 , SH, COOH, and PO 4 , or mixtures thereof.
Claim 43
Dependent Claim 18 words
The contrast agent of claim 40, wherein each R 1 is, independently, a polyhydroxy-substituted alkyl or cycloalkyl group.
Claim 44
Dependent Claim 27 words
The contrast agent of claim 42, wherein said polyhydroxy-substituted alkyl or cycloalkyl group is selected from the group consisting of sugar alcohols, monosaccharides, polysaccharides, and synthetic polymers.
Claim 45
Dependent Claim 57 words
The contrast agent of claim 35, wherein each polynitrilo chelating unit monomer consists, independently, of a chelating agent selected from the group consisting of ethylenediamine tetraacetic acid; diethylenetriamine pentaacetic acid; 1,5-di-methoxyethylene-iminocarbonyl-methylene-1,3,5-tricarboxymethylene-1,3,5,-triazapentane; 1,5-di-α,-dihydroxypropeneimino-carbonyl-methylene-1,3,5-tricarboxymethylene-1,3,5-triazapentane; 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid; 1,4,7,10-tetraazacyclododecane-N,N',N"-triacetic acid; 3,6,9-triaza-12-oxa-3,6,9-tricarboxymethylene-10-carboxy-13-phenyl-tridecanoic acid; hydroxybenzyl-ethylenediamine diacetic acid; N,N'-bis(pyridoxyl-5-phosphate)ethylenediamine-N,N'-diacetic acid; 1,4,7-triazacyclononane-N,N',N"-triacetic acid; 1-oxa-4,7,10-triazacyclododecane-triacetic acid; 1,4,8,11-tetraazacyclotetradecane-N,N',N",N'"-tetraacetic acid; triethylenetetraamine hexaacetic acid; 1,2-diaminocyclohexane-N,N,N',N'-tetraacetic acid; and anhydrides thereof.
Claim 46
Dependent Claim 26 words
The contrast agent of claim 35, wherein each free radical monomer, independently, is selected from the group consisting of heterocyclic nitroxide monomers and non-heterocyclic nitroxide monomers.
Claim 47
Dependent Claim 104 words
The contrast agent of claim 45, wherein said heterocyclic nitroxide monomers have the following general structure: ##STR51## wherein a five member ring is pyrrolidine, oxazolidine, imidazolidine, or thiazolidine; a six member ring is piperidine; and each of Ra, Rb, Rc and Rd is, independently, a C1-C20 alkyl or cycloalkyl group, said alkyl or cycloalkyl group being interrupted or terminated with OH, SH, NH 2 , NHR 1 , COOH, COOR 1 , NCS, COCHCH 2 , or COZ, each R 1 being, independently, a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group or an anhydride, and each Z being, independently, Cl, Br, or I.
Claim 48
Dependent Claim 22 words
The contrast agent of claim 45, wherein said non-heterocyclic nitroxide monomers are selected from the group consisting of diphenylnitroxide and di-tert-butyl nitroxide.
Claim 49
Dependent Claim 82 words
The contrast agent of claim 35, wherein each nitroxide free radical monomer is, independently, selected from the group consisting of 2,2,6,6-tetramethylpiperidine-1-oxyl; 2,2,4,4-tetramethyl-pyrrolidine-1-oxyl; 2,2,4,4-tetramethylimidazolidine-3-oxyl; 2,2,4,4-tetramethyl-1,3-thiazolidine-3-oxyl; 2,2,4,4-tetramethyl-1,3-oxazolidine-3-oxyl; 2,2,6,6-tetramethylpyrimidine-1-oxyl; diphenyl-nitroxide; and di-tertbutylnitroxide; and wherein each nitroxide may have one or more OH, SH, NH 2 , NHR 1 , COOH, COOR 1 , NCS, COCHCH 2 , or COZ, each R 1 being, independently, a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group or an anhydride, and each Z being, independently, Cl, Br, or I.
Claim 50
Dependent Claim 37 words
The contrast agent of claim 35, wherein each nitroxide free radical monomer is, independently, a monofunctionalized compound selected from the group consisting of 1-oxyl-2,2,6,6-tetramethyl-4-piperidinyl acrylate; 4-(iodomethylenecarbonylimino)-2,2,6,6-tetramethyl-piperdinyl-1-oxy; 4-(bromomethylenecarbonylimino)-2,2,6,6-tetramethyl-piperidinyl-1-oxy; 3-carboxy-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 3-chlorocarbonyl-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 3-aminomethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 3-hydroxymethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxyl; 3-hydroxy-2,2,5,5-tetramethylpyrrolidine-1-oxyl; 3-chloroformyl-2,2,5,5-tetramethylpyrrolidine-1-oxyl; 4-amino-2,2,6,6-tetramethylpiperidine-1-oxyl; 4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl; and 3-thiocabamoylmethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxy.
Claim 51
Dependent Claim 37 words
The contrast agent of claim 35, wherein each nitroxide free radical monomer is, independently, a difunctionalized compound selected from the group consisting of cis-1-oxyl-2,2,5,5-tetramethylpyrrolidine; trans-1-oxyl-2,2,5,5-tetramethylpyrrolidine; 3-amino-4-aminomethylene-2,2,5,5-tetramethylpyrrolidine; cis-2,5-dimethyl-2(aminomethyl)-5-(2-carboxyethyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2-(hydroxymethyl)-5-(methoxycarbonylmethyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2-(hydroxymethyl)-5-(2-hydroxyhexyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2,5-bis(3-hydroxypropyl)-pyrrolidinyl-1-oxy; trans-2,5-dimethyl-2,5-bis(3-hydroxypropyl)-pyrrolidinyl-1-oxy; trans-2,5-dimethyl-2,5-bis(2-carboxyethyl)-pyrrolidinyl-1-oxy; cis-2,5-dimethyl-2,5-bis(2-hydroxy-5-methylphenyl)-tetrahydroxypyrrol-1-oxy; 3-amino-4-carboxy-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 2,5-di-tert-butyl-3,4-diethyloxycarbonyl-pyrrol-1-oxyl; and 1,4-bis(4-hydroxy-2,2,6,6-tetramethyl-1-oxyl-4-piperidyl)-butane.
Claim 52
Dependent Claim 21 words
The contrast agent of claim 35, wherein each paramagnetic ion is selected from the group consisting of transition and lanthanide elements.
Claim 53
Dependent Claim 31 words
The contrast agent of claim 35, wherein each paramagnetic ion is selected from the group consisting of Gd(III), Mn(II), Cu(II), Cr(III), Fe(II), Fe(III), Co(II), Er(II), Ni(II), Eu(III), Dy(III), Yb(III), and Ho(III).
Claim 54
Dependent Claim 21 words
The contrast agent of claim 35, wherein each paramagnetic ion is selected from the group consisting of Gd(III), Mn(II) and Fe(III).
Claim 55
Dependent Claim 115 words
The contrast agent of claim 1, having the following structure: ##STR52## wherein Ch is a polynitrilo chelating unit monomer, L is a linker monomer, FR is a nitroxide free radical monomer, and M is a paramagnetic ion; wherein p=1 to 10,000; and wherein, within each of the p oligomeric groups ##STR53## independently, n=0 to 10,000 and j=0 to 10,000; for each group of paramagnetic ions ##STR54## chelated by each of the n chelating unit monomers --Ch-- in each of the p oligomeric groups, independently, k=0 to 2; and for each group of free radical monomers ##STR55## linked to each of the j linker monomers --L-- in each of the oligomeric groups, independently, m=0 to 2.
Claim 56
Dependent Claim 127 words
The contrast agent of claim 54, wherein each linker monomer has the following general structure: X.sub.1 [(CHR.sub.2).sub.m --CHR.sub.2 --Y].sub.n --G.sub.q --(CHR.sub.2).sub.m' --CHR.sub.2 --X.sub.2 wherein each R 1 is, independently, a C1-C20 substituted or unsubstituted, saturated or unsaturated, alkyl or cycloalkyl group; X 1 and X 2 are, independently, OH, NH 2 , NHR 1 , COOH, COOR 1 , SH, Z or NCS; Y is O, NH, NR 1 , S or CO; each R 1 is, independently, a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group or an anhydride; each Z is, independently, Cl, Br, or I; G is a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group, a saccharide, a peptide or a polysulfide; and m, m', n, and q are, independently, 0 to 10,000.
Claim 57
Dependent Claim 43 words
The contrast agent of claim 55, wherein each linker monomer is, independently, a polyamino linker monomer selected from the group consisting of 1,2-diaminoethane, 13-diaminopropane, 1,4-diaminobutane, 1,5-diamino-3-(2-aminoethyl)-pentane, N,N'-dimethyl-1,2-diaminoethane, N,N'-dimethyl-1,3-diaminopropane, 2-hydroxy-1,3-diaminopropane, 2-amino-1,3-diaminopropane, 2,3-diamino-1,4-butanediol, 1,4-diamino-2,3-butane diol, 1,4-diaminocyclohexane, 1,4-phenylenediamine, 1,1,1-tris-(aminomethyl)ethane, 2,2',2"-tris-aminoethylamine, tris-(aminomethylene)methane, diethylenetriamine, triethylenetetraamine, 1,3,5-triaminocyclohexane, and 1,3,5-triaminobenzene.
Claim 58
Dependent Claim 36 words
The contrast agent of claim 55, wherein each linker monomer is a polyhydroxy linker monomer selected from the group consisting of 2,2-dimethyl-1,3-propanediol, tris-(2-hydroxyethyl)amine, 1,1,1-tris-(hyroxymethylene)ethane, glycerine, erythritol, sugar alcohols, polyethyleneglycol, w-amino-polyethyleneglycol, N-substituted-w-aminopolyethyleneglycol, w-thiol-polyethyleneglycol, polysulfide-blocked polyethyleneglycol, and polyethylene-imine.
Claim 59
Dependent Claim 21 words
The contrast agent of claim 55, wherein each linker monomer is selected from the group consisting of ethylenedioxydiethylamine, N,N'-bis-dihydroxypropylethylenedioxydiethylamine, and ethylenedioxydiethylmercaptane.
Claim 60
Dependent Claim 52 words
The contrast agent of claim 54, wherein each polynitrilo chelating unit monomer comprises at least one COOH, COOR 1 , or COZ group; each R 1 being, independently, a C1-C20 substituted or unsubstituted, saturated or unsaturated, alkyl or cycloalkyl group or an anhydride; and each Z being, independently, Cl, Br, or I.
Claim 61
Dependent Claim 42 words
The contrast agent of claim 59, wherein at least one of said C1-C20 alkyl or cycloalkyl group is substituted with at least one moiety selected from the group of OH, NH 2 , SH, COOH, and PO 4 , or mixtures thereof.
Claim 62
Dependent Claim 18 words
The contrast agent of claim 59, wherein each R 1 is, independently, a polyhydroxy-substituted alkyl or cycloalkyl group.
Claim 63
Dependent Claim 27 words
The contrast agent of claim 61, wherein said polyhydroxy-substituted alkyl or cycloalkyl group is selected from the group consisting of sugar alcohols, monosaccharides, polysaccharides, and synthetic polymers.
Claim 64
Dependent Claim 57 words
The contrast agent of claim 54, wherein each polynitrilo chelating unit monomer consists, independently, of a chelating agent selected from the group consisting of ethylenediamine tetraacetic acid; diethylenetriamine pentaacetic acid; 1,5-di-methoxyethylene-iminocarbonyl-methylene-1,3,5-tricarboxymethylene-1,3,5,-triazapentane; 1,5-di-α,-dihydroxypropeneimino-carbonyl-methylene-1,3,5-tricarboxymethylene-1,3,5-triazapentane; 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid; 1,4,7,10-tetraazacyclododecane-N,N',N"-triacetic acid; 3,6,9-triaza-12-oxa-3,6,9-tricarboxymethylene-10-carboxy-13-phenyl-tridecanoic acid; hydroxybenzyl-ethylenediamine diacetic acid; N,N'-bis(pyridoxyl-5-phosphate)ethylenediamine-N,N'-diacetic acid; 1,4,7-triazacyclononane-N,N',N"-triacetic acid; 1-oxa-4,7,10-triazacyclododecane-triacetic acid; 1,4,8,11-tetraazacyclotetradecane-N,N',N",N'"-tetraacetic acid; triethylenetetraamine hexaacetic acid; 1,2-diaminocyclohexane-N,N,N',N'-tetraacetic acid; and anhydrides thereof.
Claim 65
Dependent Claim 26 words
The contrast agent of claim 54, wherein each free radical monomer, independently, is selected from the group consisting of heterocyclic nitroxide monomers and non-heterocyclic nitroxide monomers.
Claim 66
Dependent Claim 104 words
The contrast agent of claim 64, wherein said heterocyclic nitroxide monomers have the following general structure: ##STR56## wherein a five member ring is pyrrolidine, oxazolidine, imidazolidine, or thiazolidine; a six member ring is piperidine; and each of Ra, Rb, Rc and Rd is, independently, a C1-C20 alkyl or cycloalkyl group, said alkyl or cycloalkyl group being interrupted or terminated with OH, SH, NH 2 , NHR 1 , COOH, COOR 1 , NCS, COCHCH 2 , or COZ, each R 1 being, independently, a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group or an anhydride, and each Z being, independently, Cl, Br, or I.
Claim 67
Dependent Claim 22 words
The contrast agent of claim 64, wherein said non-heterocyclic nitroxide monomers are selected from the group consisting of diphenylnitroxide and di-tert-butyl nitroxide.
Claim 68
Dependent Claim 82 words
The contrast agent of claim 54, wherein each nitroxide free radical monomer is, independently, selected from the group consisting of 2,2,6,6-tetramethylpiperidine-1-oxyl; 2,2,4,4-tetramethyl-pyrrolidine-1-oxyl; 2,2,4,4-tetramethylimidazolidine-3-oxyl; 2,2,4,4-tetramethyl-1,3-thiazolidine-3-oxyl; 2,2,4,4-tetramethyl-1,3-oxazolidine-3-oxyl; 2,2,6,6-tetramethylpyrimidine-1-oxyl; diphenyl-nitroxide; and di-tertbutylnitroxide; and wherein each nitroxide may have one or more OH, SH, NH 2 , NHR 1 , COOH, COOR 1 , NCS, COCHCH 2 , or COZ, each R 1 being, independently, a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group or an anhydride, and each Z being, independently, Cl, Br, or I.
Claim 69
Dependent Claim 37 words
The contrast agent of claim 54, wherein each nitroxide free radical monomer is, independently, a monofunctionalized compound selected from the group consisting of 1-oxyl-2,2,6,6-tetramethyl-4-piperidinyl acrylate; 4-(iodomethylenecarbonylimino)-2,2,6,6-tetramethyl-piperdinyl-1-oxy; 4-(bromomethylenecarbonylimino)-2,2,6,6-tetramethyl-piperidinyl-1-oxy; 3-carboxy-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 3-chlorocarbonyl-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 3-aminomethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 3-hydroxymethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxyl; 3-hydroxy-2,2,5,5-tetramethylpyrrolidine-1-oxyl; 3-chloroformyl-2,2,5,5-tetramethylpyrrolidine-1-oxyl; 4-amino-2,2,6,6-tetramethylpiperidine-1-oxyl; 4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl; and 3-thiocabamoylmethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxy.
Claim 70
Dependent Claim 37 words
The contrast agent of claim 54, wherein each nitroxide free radical monomer is, independently, a difunctionalized compound selected from the group consisting of cis-1-oxyl-2,2,5,5-tetramethylpyrrolidine; trans-1-oxyl-2,2,5,5-tetramethylpyrrolidine; 3-amino-4-aminomethylene-2,2,5,5-tetramethylpyrrolidine; cis-2,5-dimethyl-2(aminomethyl)-5-(2-carboxyethyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2-(hydroxymethyl)-5-(methoxycarbonylmethyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2-(hydroxymethyl)-5-(2-hydroxyhexyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2,5-bis(3-hydroxypropyl)-pyrrolidinyl-1-oxy; trans-2,5-dimethyl-2,5-bis(3-hydroxypropyl)-pyrrolidinyl-1-oxy; trans-2,5-dimethyl-2,5-bis(2-carboxyethyl)-pyrrolidinyl-1-oxy; cis-2,5-dimethyl-2,5-bis(2-hydroxy-5-methylphenyl)-tetrahydroxypyrrol-1-oxy; 3-amino-4-carboxy-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 2,5-di-tert-butyl-3,4-diethyloxycarbonyl-pyrrol-1-oxyl; and 1,4-bis(4-hydroxy-2,2,6,6-tetramethyl-1-oxyl-4-piperidyl)-butane.
Claim 71
Dependent Claim 21 words
The contrast agent of claim 54, wherein each paramagnetic ion is selected from the group consisting of transition and lanthanide elements.
Claim 72
Dependent Claim 31 words
The contrast agent of claim 54, wherein each paramagnetic ion is selected from the group consisting of Gd(III), Mn(II), Cu(II), Cr(III), Fe(II), Fe(III), Co(II), Er(II), Ni(II), Eu(III), Dy(III), Yb(III), and Ho(III).
Claim 73
Dependent Claim 21 words
The contrast agent of claim 54, wherein each paramagnetic ion is selected from the group consisting of Gd(III), Mn(II) and Fe(III).
Claim 74
Dependent Claim 83 words
The contrast agent of claim 1, having the following structure: ##STR57## wherein Ch is a polynitrilo chelating unit monomer, FR is a nitroxide free radical monomer, and M is a paramagnetic ion; wherein p'=1 to 10,000; and wherein, within each of the p' oligomeric groups ##STR58## independently, n=0 to 10,000 and m=0 to 10,000; and for each group of paramagnetic ions ##STR59## chelated by each of the n chelating unit monomers --Ch-- in each of the p' oligomeric groups, independently, k=0 to 2.
Claim 75
Dependent Claim 52 words
The contrast agent of claim 73, wherein each polynitrilo chelating unit monomer comprises at least one COOH, COOR 1 , or COZ group; each R 1 being, independently, a C1-C20 substituted or unsubstituted, saturated or unsaturated, alkyl or cycloalkyl group or an anhydride; and each Z being, independently, Cl, Br, or I.
Claim 76
Dependent Claim 42 words
The contrast agent of claim 74, wherein at least one of said C1-C20 alkyl or cycloalkyl group is substituted with at least one moiety selected from the group of OH, NH 2 , SH, COOH, and PO 4 , or mixtures thereof.
Claim 77
Dependent Claim 18 words
The contrast agent of claim 74, wherein each R 1 is, independently, a polyhydroxy-substituted alkyl or cycloalkyl group.
Claim 78
Dependent Claim 27 words
The contrast agent of claim 76, wherein said polyhydroxy-substituted alkyl or cycloalkyl group is selected from the group consisting of sugar alcohols, monosaccharides, polysaccharides, and synthetic polymers.
Claim 79
Dependent Claim 57 words
The contrast agent of claim 73, wherein each polynitrilo chelating unit monomer consists, independently, of a chelating agent selected from the group consisting of ethylenediamine tetraacetic acid; diethylenetriamine pentaacetic acid; 1,5-di-methoxyethylene-iminocarbonyl-methylene-1,3,5-tricarboxymethylene-1,3,5,-triazapentane; 1,5-di-α,dihydroxypropeneimino-carbonyl-methylene-1,3,5-tricarboxymethylene-1,3,5-triazapentane; 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid; 1,4,7,10-tetraazacyclododecane-N,N',N"-triacetic acid; 3,6,9-triaza-12-oxa-3,6,9-tricarboxymethylene-10-carboxy-13-phenyl-tridecanoic acid; hydroxybenzyl-ethylenediamine diacetic acid; N,N'-bis(pyridoxyl-5-phosphate)ethylenediamine-N,N'-diacetic acid; 1,4,7-triazacyclononane-N,N',N"-triacetic acid; 1-oxa-4,7,10-triazacyclododecane-triacetic acid; 1,4,8,11-tetraazacyclotetradecane-N,N',N",N'"-tetraacetic acid; triethylenetetraamine hexaacetic acid; 1,2-diaminocyclohexane-N,N,N',N'-tetraacetic acid; and anhydrides thereof.
Claim 80
Dependent Claim 26 words
The contrast agent of claim 73, wherein each free radical monomer, independently, is selected from the group consisting of heterocyclic nitroxide monomers and non-heterocyclic nitroxide monomers.
Claim 81
Dependent Claim 104 words
The contrast agent of claim 79, wherein said heterocyclic nitroxide monomers have the following general structure: ##STR60## wherein a five member ring is pyrrolidine, oxazolidine, imidazolidine, or thiazolidine; a six member ring is piperidine; and each of Ra, Rb, Rc and Rd is, independently, a C1-C20 alkyl or cycloalkyl group, said alkyl or cycloalkyl group being interrupted or terminated with OH, SH, NH 2 , NHR 1 , COOH, COOR 1 , NCS, COCHCH 2 , or COZ, each R 1 being, independently, a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group or an anhydride, and each Z being, independently, Cl, Br, or I.
Claim 82
Dependent Claim 22 words
The contrast agent of claim 79, wherein said non-heterocyclic nitroxide monomers are selected from the group consisting of diphenylnitroxide and di-tert-butyl nitroxide.
Claim 83
Dependent Claim 82 words
The contrast agent of claim 73, wherein each nitroxide free radical monomer is, independently, selected from the group consisting of 2,2,6,6-tetramethylpiperidine-1-oxyl; 2,2,4,4-tetramethyl-pyrrolidine-1-oxyl; 2,2,4,4-tetramethylimidazolidine-3-oxyl; 2,2,4,4-tetramethyl-1,3-thiazolidine-3-oxyl; 2,2,4,4-tetramethyl-1,3-oxazolidine-3-oxyl; 2,2,6,6-tetramethylpyrimidine-1-oxyl; diphenyl-nitroxide; and di-tertbutylnitroxide; and wherein each nitroxide may have one or more OH, SH, NH 2 , NHR 1 , COOH, COOR 1 , NCS, COCHCH 1 , or COZ, each R 1 being, independently, a C1-C20 substituted or unsubstituted alkyl or cycloalkyl group or an anhydride, and each Z being, independently, Cl, Br, or I.
Claim 84
Dependent Claim 37 words
The contrast agent of claim 73, wherein each nitroxide free radical monomer is, independently, a monofunctionalized compound selected from the group consisting of 1-oxyl-2,2,6,6-tetramethyl-4-piperidinyl acrylate; 4-(iodomethylenecarbonylimino)-2,2,6,6-tetramethyl-piperdinyl-1-oxy; 4-(bromomethylenecarbonylimino)-2,2,6,6-tetramethyl-piperidinyl-1-oxy; 3-carboxy-2,2,5,5-tetramethylpyrolidinyl-1-oxy; 3-chlorocarbonyl-2,2,5,5-tetramethylpyrrolfdinyl-1-oxy; 3-aminomethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 3-hydroxymethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxyl; 3-hydroxy-2,2,5,5-tetramethylpyrrolidine-1-oxyl; 3-chloroformyl-2,2,5,5-tetramethylpyrrolidine-1-oxyl; 4-amino-2,2,6,6-tetramethylpiperidine-1-oxyl; 4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl; and 3-thiocabamoylmethylene-2,2,5,5-tetramethylpyrrolidinyl-1-oxy.
Claim 85
Dependent Claim 37 words
The contrast agent of claim 73, wherein each nitroxide free radical monomer is, independently, a difunctionalized compound selected from the group consisting of cis-1-oxyl-2,2,5,5-tetramethylpyrrolidine; trans-1-oxyl-2,2,5,5-tetramethylpyrrolidine; 3-amino-4-aminomethylene-2,2,5,5-tetramethylpyrrolidine; cis-2,5-dimethyl-2(aminomethyl)-5-(2-carboxyethyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2-(hydroxymethyl)-5-(methoxycarbonylmethyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2-(hydroxymethyl)-5-(2-hydroxyhexyl)-tetrahydropyrrole-1-oxyl; cis-2,5-dimethyl-2,5-bis(3-hydroxypropyl)-pyrrolidinyl-1-oxy; trans-2,5-dimethyl-2,5-bis(3-hydroxypropyl)-pyrrolidinyl-1-oxy; trans-2,5-dimethyl-2,5-bis(2-carboxyethyl)-pyrrolidinyl-1-oxy; cis-2,5-dimethyl-2,5-bis(2-hydroxy-5-methylphenyl)-tetrahydroxypyrrol-1-oxy; 3-amino-4-carboxy-2,2,5,5-tetramethylpyrrolidinyl-1-oxy; 2,5-di-tert-butyl-3,4-diethyloxycarbonyl-pyrrol-1-oxyl; and 1,4-bis(4-hydroxy-2,2,6,6-tetramethyl-1-oxyl-4-piperidyl)-butane.
Claim 86
Dependent Claim 21 words
The contrast agent of claim 73, wherein each paramagnetic ion is selected from the group consisting of transition and lanthanide elements.
Claim 87
Dependent Claim 31 words
The contrast agent of claim 73, wherein each paramagnetic ion is selected from the group consisting of Gd(III), Mn(II), Cu(II), Cr(III), Fe(II), Fe(III), Co(II), Er(II), Ni(II), Eu(III), Dy(III), Yb(III), and Ho(III).
Claim 88
Dependent Claim 21 words
The contrast agent of claim 73, wherein each paramagnetic ion is selected from the group consisting of Gd(III), Mn(II) and Fe(III).

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