US4830847A
Expired / Lapsed
US
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Diphosphonate-derivatized macromolecules
Assignee: Procter and Gamble Co
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Filing: 1985-06-28
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Granted: 1989-05-16
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Expires: 2005-06-28
Abstract
Abstract Diphosphonate-derivatized macromolecules, such as proteins, suitable for use as technetium-99m-based scanning agents and as anticalcification agents are disclosed. The scanning agents are prepared by combining Tc-99m in a +3, +4 and/or +5 oxidation state with the diphosphonate-derivatized macromolecules. Also disclosed are pharmaceutical compositions containing these diphosphonate-derivatized macromolecules and methods for scintigraphic imaging using these diphosphonate-derivatized macromolecules labeled with Tc-99m.
Inventors
- 👤 James J. Benedict
- 👤 Charles R. Degenhardt
- 👤 James W. Poser
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 04:41
CPC Classifications
C; C08; C08H; C08H1/00; A; A61; A61K; A61K41/00; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/58; A61K47/61; A61K47/62; A61K47/68; A61K47/6835; A61K47/6883; A61K51/00; A61K51/02; A61K51/04; A61K51/0497; A61K51/06; A61K51/065; A61K51/08; A61K51/10; A61K51/1093; C08B; C08B37/00; C08B37/0006; C08B37/0036; C08B37/0039; C08F; C08F8/00; C08F8/40; A61K2123/00
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
68 words
A radiolabeled diphosphonate-derivatized polypeptide chelate comprising technetium 99 m complexed with a diphosphonate-derivatized polypeptide selected from the group consisting of: wherein (i) P is a polypeptide; (ii) n is an integer from 1 to 12; and (iii) X is selected from the group consisting of H, OH, and NH 2 , substituted amino, halogen and C 1 -C 4 alkyl; and the pharmaceutically-acceptable salts of these derivatized polypeptides.
Claim 2
Dependent Claim
68 words
A radiolabeled diphosphonate-derivatized polypeptide chelate comprising technetium 99 m complexed with a diphosphonate-derivatized polypeptide selected from the group consisting of: wherein (i) P is a polypeptide; (ii) n is an integer from 1 to 12; and (iii) X is selected from the group consisting of H, OH, and NH 2 , substituted amino, halogen and C 1 -C 4 alkyl; and the pharmaceutically-acceptable salts of these derivatized polypeptides.
Claim 3
Dependent Claim
18 words
The radiolabeled chelate of claim 1 wherein said diphosphonate-derivatized polypeptide is selected from the group consisting of ##STR45##
Claim 4
Dependent Claim
18 words
The radiolabeled chelate of claim 1 wherein said diphosponate-derivatized polypeptide is selected from the group consisting of: ##STR46##
Claim 5
Dependent Claim
21 words
The radiolabeled chelate of claim 1 wherein X is selected from the group consisting of NH 2 , OH and H.
Claim 6
Dependent Claim
21 words
The radiolabeled chelate of claim 2 wherein X is selected from the group consisting of NH 2 , OH and H.
Claim 7
Dependent Claim
21 words
The radiolabeled chelate of claim 3 wherein X is selected from the group consisting of NH 2 , OH and H.
Claim 8
Dependent Claim
19 words
The radiolabeled chelate of claim 6 wherein X is OH and n is an integer from 1 to 5.
Claim 9
Dependent Claim
91 words
A pharmaceutical composition for scintigraphic imaging in humans or animals which comprises: (a) a safe and effective amount of a diphosphonate-derivatized polypeptide selected from the group consisting of: ##STR47## wherein (i) P is a polypeptide; (ii) n is an integer from 1 to 12; and (iii) X is selected from the group consisting of H, OH, and NH 2 , substituted amino, halogen and C 1 -C 4 alkyl; and the pharmaceutically-acceptable salts of these derivatized polypeptides; (b) a pertechnetate reducing agent; (c) a stabilizer compound; and (d) a pharmaceutically-acceptable carrier.
Claim 10
Dependent Claim
91 words
A pharmaceutical composition for scintigraphic imaging in humans or animals which comprises: (a) a safe and effective amount of a diphosphonate-derivatized polypeptide selected from the group consisting of: ##STR47## wherein (i) P is a polypeptide; (ii) n is an integer from 1 to 12; and (iii) X is selected from the group consisting of H, OH, and NH 2 , substituted amino, halogen and C 1 -C 4 alkyl; and the pharmaceutically-acceptable salts of these derivatized polypeptides; (b) a pertechnetate reducing agent; (c) a stabilizer compound; and (d) a pharmaceutically-acceptable carrier.
Claim 11
Dependent Claim
17 words
The composition of claim 8 wherein said diphosphonate-derivatized polypeptide is selected from the group consisting of: ##STR48##
Claim 12
Dependent Claim
20 words
The composition of claim 9 wherein X is selected from the group consisting of NH 2 , OH and H.
Claim 13
Dependent Claim
18 words
A composition of claim 10 wherein X is OH and n is an integer from 1 to 5.
Claim 14
Dependent Claim
52 words
A pharmaceutical composition according to claim 8 in liquid form comprising from about 1% to about 20% of the diphosphonate derivatized polypeptide, from 0.0001% to about 10% of a pertechnetate reducing agent, from about 0.001% to about 20% of a stabilizer and from about 50% to about 98% of a pharmaceutically-acceptable carrier.
Claim 15
Dependent Claim
57 words
A pharmaceutical composition according to claim 8 in liquid form comprising from about 0.01% to about 20% of the diphosphonate-derivatized polypeptide, from about 1×10 -6 % to about 10% of a pertechnetate reducing agent, from about 1×10 -5 % to about 20% of a stabilizer compound and from about 50% to about 99.9% of a pharmaceutically-acceptable carrier.
Claim 16
Dependent Claim
10 words
A pharmaceutical composition according to claim 8 in lyophilized form.
Claim 17
Dependent Claim
50 words
A lyophilized pharmaceutical composition according to claim 14 comprising from about 5% to about 99% of the diphosphonate-derivatized polypeptide, from about 0.0005% to about 10% of a pertechnetate reducing agent, from about 0.005% to about 20% of a stabilizer and from about 0.01% to about 60% of a pharmaceutically-acceptable carrier.
Claim 18
Dependent Claim
49 words
A lyophilized pharmaceutical composition according to claim 14 comprising from 1% to about 50% of the diphosphonate-derivatized polypeptide, from about 0.0001% to about 10% of a pertechnetate reducing agent, from about 0.001% to about 20% of a stabilizer and from about 20% to about 98% of a pharmaceutically-acceptable carrier.
Claim 19
Dependent Claim
62 words
A method for scintigraphic imaging of tissues in humans or animals which comprises mixing the pharmaceutical composition of claim 8 with a pertechnetate-99 m solution, administering from about 1 ml to about 150 ml of said mixture to said human or animal and subsequently imaging said human or animal with a scintigraphic device capable of detecting the radiation emitted from said mixture.
Claim 20
Dependent Claim
61 words
A method for scintigraphic imaging of tissues in humans or animals which comprises mixing the pharmaceutical composition of claim 13 with a pertechnetate-99 m solution, administering from 1 ml to about 150 ml of said mixture to said human or animal and subsequently imaging said human or animal with a scintigraphic device capable of detecting the radiation emitted from said mixture.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1992-05-15 | 1992-11-14 | 1993-05-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-05-15 | 1996-11-14 | 1997-05-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-05-15 | 2000-11-14 | 2001-05-16 | $7700.00 | Window Closed / Lapsed |