Patent US4897255A successfully refreshed from Google Patents.
US4897255A
Expired / Lapsed
US
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Metal radionuclide labeled proteins for diagnosis and therapy
Assignee: Poniard Pharmaceuticals Inc
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Filing: 1987-06-19
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Granted: 1990-01-30
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Expires: 2007-06-19
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
2026-10-25 22:03
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
220 words
A method for preparing a radiolabeled polypeptide which comprises: combined in an aqueous medium, said polypeptide and said compound of the formula ##STR32## wherein: M is a metal or metal oxide radionuclide ion; one of Z 1 , Z 2 , Z 3 , or Z 4 , is R'CW'(HNV')n'Y', and the others are H 2 or ═O; R' is an aliphatic divalent radical of from 1 to 6 carbon atoms and 0 to 2 heteroatoms; V' is of the formula R'CW'; W' is H 2 or =NH or =0, with the proviso that the W' bonded to the carbon atom bonded to Y' is H 2 when Y' is -NH2; X' is a bond, methylene or CHZ4; A' is H or lower alkyl of from 1 to 6 carbon atoms; n' is 0 to 1; and Y' is the leaving group of an active ester, said ester reacting with said polypeptide to form an amide or amidine bond with said polypeptide; or NH 2 ; or NHNH 2 , with the proviso that when Y' is NH 2 or NHNH 2 , said polypeptide has an oxo-group as a result of glycol cleavage of a sugar bound to said polypeptide, and said combining is under reductive amination conditions; wherein said compound forms a stable covalent bond to said polypeptide.
Claim 2
Independent Claim
220 words
A method for preparing a radiolabeled polypeptide which comprises: combined in an aqueous medium, said polypeptide and said compound of the formula ##STR32## wherein: M is a metal or metal oxide radionuclide ion; one of Z 1 , Z 2 , Z 3 , or Z 4 , is R'CW'(HNV')n'Y', and the others are H 2 or ═O; R' is an aliphatic divalent radical of from 1 to 6 carbon atoms and 0 to 2 heteroatoms; V' is of the formula R'CW'; W' is H 2 or =NH or =0, with the proviso that the W' bonded to the carbon atom bonded to Y' is H 2 when Y' is -NH2; X' is a bond, methylene or CHZ4; A' is H or lower alkyl of from 1 to 6 carbon atoms; n' is 0 to 1; and Y' is the leaving group of an active ester, said ester reacting with said polypeptide to form an amide or amidine bond with said polypeptide; or NH 2 ; or NHNH 2 , with the proviso that when Y' is NH 2 or NHNH 2 , said polypeptide has an oxo-group as a result of glycol cleavage of a sugar bound to said polypeptide, and said combining is under reductive amination conditions; wherein said compound forms a stable covalent bond to said polypeptide.
Claim 3
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.
Claim 4
Dependent Claim
17 words
The method according to claim 1, wherein said polypeptide is an immunoglobulin or specific binding fragment thereof.
Claim 5
Dependent Claim
12 words
The method according to claim 3 wherein immunoglobulin is a monoclonal antibody.
Claim 6
Dependent Claim
15 words
The method according to claim 4 wherein said monoclonal antibody is specific for cancer cells.
Claim 7
Dependent Claim
13 words
The method according to claim 5 wherein said cancer cells are melanoma cells
Claim 8
Dependent Claim
31 words
The method according to claim 3 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 9
Dependent Claim
14 words
The method according to claim 7 wherein said fragment is specific for cancer cells.
Claim 10
Dependent Claim
13 words
The method according to claim 8 wherein said cancer cells are melanoma cells.
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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) | 1993-01-29 | 1993-07-31 | 1994-01-30 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-01-29 | 1997-07-31 | 1998-01-30 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-01-29 | 2001-07-31 | 2002-01-30 | $7700.00 | Window Closed / Lapsed |