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US5037630A
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Metal radionuclide labeled proteins for diagnosis and therapy
Assignee: Poniard Pharmaceuticals Inc
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Filing: 1989-10-18
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Granted: 1991-08-06
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Expires: 2009-10-18
Abstract
Abstract Protein conjugated chelated metal radionuclides are provided for use in vivo. Intermediates are provided for preparing the polypeptide compositions efficiently.
Inventors
- 👤 Alan R. Fritzberg
- 👤 Sudhakar Kasina
- 👤 Ananthachari Srinivasan
- 👤 Daniel S. Wilbur
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 14:14
CPC Classifications
C; C07; C07C; C07C271/00; C07C271/06; C07C271/08; C07C271/10; C07C271/22; A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0474; A61K51/0478; A61K51/08; A61K51/10; A61K51/1093; A61K51/12; B; B82; B82Y; B82Y5/00; C07C227/00; C07C227/04; C07C227/06; C07C227/08; A61K2123/00; Y; Y10; Y10S; Y10S530/00; Y10S530/866
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
179 words
A method for preparing a radiolabeled polypeptide which comprises: a) combining in an aqueous medium, a metal radionuclide in a reduced chelated exchangeable form; and a compound of the formula: ##STR31## wherein: one of Z 1 , Z 2 , Z 3 or Z 4 is RCW(HNRCW) n Y, and the others are H 2 or ═O; each R is independently selected from divalent organic radicals of from 1 to 6 carbon atoms and 0 to 2 heteroatoms; each W is independently selected from ═NH or ═O, with the proviso that the W bonded to the carbon atom bonded to Y is H 2 when Y is --NH 2 or NHNH 2 ; n is 0 or 1; T is an alkali metal ion or a sulfur protecting group comprising from 2 to about 10 carbon atoms; X is a bond, methylene, or CHZ 4 ; the A's are the same or different and are hydrogen or lower alkyl of from 1 to 6 carbon atoms; and Y is a polypeptide; whereby said radionuclide becomes chelated by said compound.
Claim 2
Independent Claim
179 words
A method for preparing a radiolabeled polypeptide which comprises: a) combining in an aqueous medium, a metal radionuclide in a reduced chelated exchangeable form; and a compound of the formula: ##STR31## wherein: one of Z 1 , Z 2 , Z 3 or Z 4 is RCW(HNRCW) n Y, and the others are H 2 or ═O; each R is independently selected from divalent organic radicals of from 1 to 6 carbon atoms and 0 to 2 heteroatoms; each W is independently selected from ═NH or ═O, with the proviso that the W bonded to the carbon atom bonded to Y is H 2 when Y is --NH 2 or NHNH 2 ; n is 0 or 1; T is an alkali metal ion or a sulfur protecting group comprising from 2 to about 10 carbon atoms; X is a bond, methylene, or CHZ 4 ; the A's are the same or different and are hydrogen or lower alkyl of from 1 to 6 carbon atoms; and Y is a polypeptide; whereby said radionuclide becomes chelated by said compound.
Claim 3
Dependent Claim
17 words
The method according to claim 1 wherein said polypeptide is an immunoglobulin or specific binding fragment thereof.
Claim 4
Dependent Claim
13 words
The method according to claim 2 wherein said immunoglobulin is a monoclonal antibody.
Claim 5
Dependent Claim
15 words
The method according to claim 3 wherein said monoclonal antibody is specific for cancer cells.
Claim 6
Dependent Claim
13 words
The method according to claim 4 wherein said cancer cells are melanoma cells.
Claim 7
Dependent Claim
31 words
The method according to claim 2 wherein said specific binding fragment is selected from the group consisting of a F(ab), F(ab'), F(ab') 2 , and F v fragment of an antibody.
Claim 8
Dependent Claim
14 words
The method according to claim 6 wherein said fragment is specific for cancer cells.
Claim 9
Dependent Claim
13 words
The method according to claim 7 wherein said cancer cells are melanoma cells.
Claim 10
Dependent Claim
33 words
The method according to claim 1, wherein said radionuclide is selected from the group consisting of 99m Tc, 188 Re, 186 Re, 67 Cu, 64 Cu, 212 Pb, 212 Bi, and 109 Pd.
References Cited (Backward Citations)
US4897255A
Cited
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