EP0173629A1
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Antibody-metal ion complexes
Assignee: Cytogen Corp
•
Filing: 1985-08-29
•
Granted: —
•
Expires: 2005-08-29
Abstract
Abstract This invention relates to antibody-metal ion complexes having a metal ion coordinately bound to a compatible chelator covalently bound to an antibody or antibody fragment. Also described are methods for intermediates in the preparation of antibody-metal ion complexes. Therapeutic and in vitro and in vivo diagnostic methods utilizing such antibody-metal ion complexes are described.
Inventors
- 👤 Chyi Lee
- 👤 John Dennis Rodwell
- 👤 John Walter Frank Goers
- 👤 Richard Charles Siegel
- 👤 Vernon Leon Alvarez
- 👤 Thomas Joseph Mckearn
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-26 09:48
CPC Classifications
A; A61; A61K; A61K49/00; A61K49/06; A61K49/08; A61K49/10; A61K49/14; A61K49/16; A61K49/085; A61K51/00; A61K51/02; A61K51/04; A61K51/08; A61K51/10; A61K51/1093; G; G01; G01N; G01N33/00; G01N33/48; G01N33/50; G01N33/53; G01N33/531; G01N33/532; G01N33/534; G01N33/577; A61K2121/00; A61K2123/00
Claims Analysis
Total Claims: 36
Claim 1
Independent Claim
58 words
An antibody-chelator conjugate, comprising: a compatible chelator attached through a covalent bond to an antibody or antibody fragment, said antibody-chelator conjugate having substantially the same immunoreactivity and immunospecificity as the unconjugated antibody or antibody fragment, and wherein the covalent bond is selectively formed at a site located outside the antigen binding region of the antibody or antibody fragment.
Claim 2
Dependent Claim
58 words
An antibody-chelator conjugate, comprising: a compatible chelator attached through a covalent bond to an antibody or antibody fragment, said antibody-chelator conjugate having substantially the same immunoreactivity and immunospecificity as the unconjugated antibody or antibody fragment, and wherein the covalent bond is selectively formed at a site located outside the antigen binding region of the antibody or antibody fragment.
Claim 3
Dependent Claim
50 words
The antibody-chelator conjugate according to claim 1, wherein the compatible chelator is attached through a covalent bond to a carbohydrate moiety of an oxidized antibody or antibody fragment, said covalent bond selected from the group consisting of an imine, enamine, hydrazone, oxime, phenylhydrazone, semicarbazone, thiosemicarbazone, and a reduced form thereof.
Claim 4
Dependent Claim
27 words
The antibody-chelator conjugate according to claim 2, wherein the antibody fragment is selected from the group consisting of Fab fragments, (Fab') 2 fragments and half antibody molecules.
Claim 5
Dependent Claim
21 words
The antibody-chelator conjugate according to claim 2, wherein the antibody or antibody fragment is a monoclonal antibody or monoclonal antibody fragment.
Claim 6
Dependent Claim
34 words
The antibody-chelator conjugate according to claim 1, wherein the compatible chelator is an amine-containing derivative of a chelator selected from the group consisting of diethylenetriamine-pentaacetic acid, ethylenediaminetetraacetic acid, dimercaptosuccinic acid, 2,3-dimercaptopropanesulfonic acid and metallothionein.
Claim 7
Dependent Claim
55 words
The antibody-chelator conjugate according to claim 2, wherein the compatible chelator is selected from the group consisting of p-aminoaniline-diethylenetriaminepentaacetic acid, hydrazide- diethylenetriaminepentaacetic acid, phenylhydrazide- diethylenetriaminepentaacetic acid, hydroxylamine- diethylenetriaminepentaacetic acid, semicarbazide- diethylenetriaminepentaacetic acid, thiosemicarbazide- diethylenetriaminepentaacetic acid, polyethyleneimine-diethylenetriaminepentaacetic acid, p-phenylenediamine- diethylenetriaminepentaacetic acid, a-N-diethylenetriaminepentaacetic acid-L-lysine, glycyl-tyrosyl-lysine-diethylenetriaminepentaacetic acid, diethylenetriaminepentaacetic acid mono [(4-aminophenyl)methyl] amide and L-lysine benzyl ester- diethylenetriaminepentaacetic acid.
Claim 8
Dependent Claim
18 words
The antibody-chelator conjugate according to claim 2, wherein the compatible chelator is an amine-containing derivative of a cryptate.
Claim 9
Dependent Claim
28 words
The antibody-chelator conjugate according to claim 1, wherein the compatible chelator is attached through a covalent bond to a sulfur atom of a reduced antibody or Fab' fragment.
Claim 10
Dependent Claim
21 words
The antibody-chelator conjugate according to claim 8, wherein the antibody or Fab' fragment is a monoclonal antibody or monoclonal antibody fragment.
Claim 11
Dependent Claim
36 words
The antibody-chelator conjugate according to claim 8, wherein the compatible chelator is a haloalkyl- containing derivative of a chelator selected from the group consisting of diethylenetriaminepentaacetic acid, ethylenediaminetetraacetic acid, dimercaptosuccinic acid, 2,3-dimercaptopropanesulfonic acid, metallothionein and cryptates.
Claim 12
Dependent Claim
82 words
An antibody-metal ion complex, comprising: an antibody-chelator conjugate comprising a compatible chelator attached through a covalent bond to an antibody or antibody fragment, said antibody-chelator conjugate having substantially the same immunoreactivity and immunospecificity as the unconjugated antibody or antibody fragment, and wherein the covalent bond is selectively formed at a site located outside the antigen binding region of the antibody or antibody fragment, said antibody-chelator conjugate coordinatedly bound through said compatible chelator to a metal ion to form an antibody-metal ion complex.
Claim 13
Dependent Claim
82 words
An antibody-metal ion complex, comprising: an antibody-chelator conjugate comprising a compatible chelator attached through a covalent bond to an antibody or antibody fragment, said antibody-chelator conjugate having substantially the same immunoreactivity and immunospecificity as the unconjugated antibody or antibody fragment, and wherein the covalent bond is selectively formed at a site located outside the antigen binding region of the antibody or antibody fragment, said antibody-chelator conjugate coordinatedly bound through said compatible chelator to a metal ion to form an antibody-metal ion complex.
Claim 14
Dependent Claim
70 words
The antibody-metal ion complex, according to claim 11, wherein the antibody-chelator conjugate comprising a compatible chelator is attached through a covalent bond to a carbohydrate moiety of an oxidized antibody or antibody fragment, and said covalent bond is an imine, enamine hydrazone, oxime, phenylhydrazone, semicarbazone, thiosemicarbazone or a reduced form thereof, said antibody-chelator conjugate coordinately bound through said compatible chelator to a metal ion to form an antibody-metal ion complex.
Claim 15
Dependent Claim
28 words
The antibody-metal ion complex according to claim 12, wherein the antibody fragment is selected from the group consisting of Fab fragments, (Fab') 2 fragments and half antibody molecules.
Claim 16
Dependent Claim
22 words
The antibody-metal ion complex according to claim 12, wherein the antibody or antibody fragment is a monoclonal antibody or monoclonal antibody fragment.
Claim 17
Dependent Claim
35 words
The antibody-metal ion complex according to claim 12, wherein the compatible chelator is an amine-containing derivative of a chelator selected from the group consisting of diethylenetriaminepentaacetic acid, ethylenediaminetetraacetic acid, dimercaptosuccinic acid, 2,3-dimercaptopropanesulfonic acid and metallothionein.
Claim 18
Dependent Claim
54 words
The antibody-metal ion complex accoarding to claim 12, wherein the compatible chelator is selected from the group consisting of p-aminoaniline-diethylenetriaminepentaacetic acid, hydrazide- diethylenetriaminepentaacetic acid, phenylhydrazide- diethylenetriaminepentaacetic acid, hydroxylamine- diethylenetriaminepentaacetic acid,semicarbazide- diethylenetriaminepentaacetic acid, thiosemicarbazide- diethylenetriaminepentaacetic acid,polyethyleneimine-diethylenetriaminepentaacetic acid, p-phenylenediamine- diethylenetriaminepentaacetic acid, a-N-diethylenetriaminepentaacetic acid-L-lysine, glycyl-tyrosyl-lysine-diethylenetriaminepentaacetic acid, diethylenetriaminepentaacetic acid mono [(4-aminophenyl)methyl] amide and L-lysine benzyl ester- diethylenetriaminepentaacetic acid.
Claim 19
Dependent Claim
19 words
The antibody-metal ion complex according to claim 12, wherein the compatible chelator is an amine-containing derivative of a cryptate.
Claim 20
Dependent Claim
14 words
The antibody-metal ion complex according to claim 12, substantially free of non-chelated metal ions.
Claim 21
Dependent Claim
52 words
The antibody-metal ion complex, according to claim 11, wherein the antibody-chelator conjugate comprising a compatible chelator is attached through a covalent bond to a sulfur atom of a reduced antibody or Fab' fragment, said antibody-chelator conjugate coordinately bound through said compatible chelator to a metal ion to form an antibody-metal ion complex.
Claim 22
Dependent Claim
17 words
The antibody-metal ion complex according to claim 12 or 19, wherein the metal ion is a radioisotope.
Claim 23
Dependent Claim
14 words
The antibody-metal ion complex according to claim 20, wherein the radioisotope emits beta particles.
Claim 24
Dependent Claim
28 words
The antibody-metal ion complex according to claim 21, wherein the radioisotope is selected from the group consisting of 46 Scandium, 47 Scandium, Scandium, 72 Gallium and 73 Gallium.
Claim 25
Dependent Claim
14 words
The antibody-metal ion complex according to claim 20, wherein the radioisotope emits alpha particles.
Claim 26
Dependent Claim
27 words
The antibody-metal ion complex according to claim 23, wherein the radioisotope is selected from the group consisting of 211 Bismuth, 212 Bismuth, 213 Bismuth and 214 Bismuth.
Claim 27
Dependent Claim
14 words
The antibody-metal ion complex according to claim 20, wherein the radioisotope emits positron particles.
Claim 28
Dependent Claim
29 words
The antibody-metal ion complex according to claim 25, wherein the radioisotope is selected from the group consisting of 43 Scandium, 44 Scandium, 52 Iron, 55 Cobalt and 68 Gallium.
Claim 29
Dependent Claim
16 words
The antibody-metal ion complex according to claim 12 or 19, wherein the metal ion is paramagnetic.
Claim 30
Dependent Claim
32 words
The antibody-metal ion complex according to claim 27, wherein the metal ion is selected from the group consisting of 54 Iron, 56 Iron, 57 Iron, 58 Iron, 157 Gadolinium and 55 Manganese.
Claim 31
Dependent Claim
24 words
The antibody-metal ion complex according to claim 19, wherein the antibody or (Fab')2 fragment is a monoclonal antibody or monoclonal antibody (Fab') 2 fragment.
Claim 32
Dependent Claim
37 words
The antibody-metal ion complex according to claim 19, wherein the compatible chelator is an haloalkyl- containing derivative of a chelator selected from the group consisting of diethylenetriaminepentaacetic acid, ethylenediaminetetraacetic acid, dimercaptosuccinic acid, 2,3-dimercaptopropanesulfonic acid, metallothionein and cryptates.
Claim 33
Dependent Claim
14 words
The antibody-metal ion complex according to claim 19, substantially free of non-chelated metal ions.
Claim 34
Dependent Claim
66 words
A method for imaging specific tissue, comprising: administering to a human an effective amount of an antibody-metal ion complex according to claim 11, 12 or 19, wherein said antibody-metal ion complex is immunoreactive with and immunospecific for an antigenic determinant of said specific tissue and substantially non-immunoreactive with and non-immunospecific for non-specific tissue and said antigenic determinant is not found in substantial amount in non-specific tissue.
Claim 35
Dependent Claim
81 words
A composition for therapeutic treatment of cellular disorders, comprising a therapeutically effective amount of an antibody-metal ion complex according to claim 11, 12 or 19, said antibody-metal ion complex being immunoreactive with and immunospecific for a target site associated with said cellular disorder and substantially non-immunoreactive with and immunospecific for a target site associated with said cellular disorder and substantially non-immunoreactive with and non-immunospecific for tissue not associated with said cellular disorder, and wherein the metal ion emits cytotoxic beta particles.
Claim 36
Dependent Claim
57 words
A method for testing for antigen, comprising: (a) mixing an antibody-metal ion complex according to claim 11, 12 or 19, with a sample suspected of containing a particular antigen, the antibody-metal ion complex being immunoreactive with and immunospecific for said antigen, and (b) detecting any interaction of said antibody-metal ion complex with any antigen in the sample.
References Cited (Backward Citations)
DE3239410A1
Cited
USPTO Annuity & Maintenance Windows
Maintenance schedule is calculated for granted US utility patents.