US5202109A
Expired / Lapsed
US
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Conjugates for bone imaging and bone cancer therapy
Assignee: Poniard Pharmaceuticals Inc
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Filing: 1991-01-31
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Granted: 1993-04-13
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Expires: 2011-01-31
Abstract
Abstract The present invention provides conjugates formed from calcified tissues targeting agents and radiolabeled compounds. One such conjugate comprises a chelate and a targeting agent that is capable of associating with calcified tissue, wherein the chelate contains at least one nitrogen atom or at least one sulfur atom or combinations thereof as the donor atoms. Another aspect of the invention provides method for using the conjugates for diagnostic and therapeutic purposes, including those related to bone cancer.
Inventors
- 👤 Alan R. Fritzberg
- 👤 Jean-Luc E. Vanderheyden
- 👤 Sudhakar Kasina
- 👤 Jeffrey N. Fitzner
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 19:55
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/3804; C07F9/3839; C07F9/3873; A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0497; C07F13/00; C07F13/005; A61K2121/00; A61K2123/00
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
122 words
A conjugate of a radiolabeled compound and a targeting agent that is capable of associating with calcified tissue, wherein said targeting agent is a phosphorus-containing compound which contains a C--O--P bond, a P--O--P bond, a C--C--P bond, a P--C--P bond, a P--N--P bond or combinations thereof, and wherein said radiolabled compound comprises the formula: *X--Ar--R wherein *X is a radioisotope of iodine, bromine, fluorine, or astatine; Ar is aromatic or heteroaromatic ring; R is a chemical bond or a substituent containing 1 to 12 straight-chain carbon atoms that does not activate Ar toward electrophilic substitution on the order produced by hydroxy or amino substitution of the ring, wherein said bond or said substituent has attached thereto a functional group suitable for conjugation.
Claim 2
Dependent Claim
122 words
A conjugate of a radiolabeled compound and a targeting agent that is capable of associating with calcified tissue, wherein said targeting agent is a phosphorus-containing compound which contains a C--O--P bond, a P--O--P bond, a C--C--P bond, a P--C--P bond, a P--N--P bond or combinations thereof, and wherein said radiolabled compound comprises the formula: *X--Ar--R wherein *X is a radioisotope of iodine, bromine, fluorine, or astatine; Ar is aromatic or heteroaromatic ring; R is a chemical bond or a substituent containing 1 to 12 straight-chain carbon atoms that does not activate Ar toward electrophilic substitution on the order produced by hydroxy or amino substitution of the ring, wherein said bond or said substituent has attached thereto a functional group suitable for conjugation.
Claim 3
Dependent Claim
25 words
The conjugate of claim 1 wherein *X is 123 I, 125 I, 131 I, 75 Br, 76 Br, 77 Br, 18 F, or 211 At.
Claim 4
Dependent Claim
11 words
The conjugate of claim 1 wherein the calcified tissue is bone.
Claim 5
Dependent Claim
70 words
A method of detecting the presence or absence of a calcified tissue target site within a mammalian host, comprising the steps of: administering to a mammal a diagnostically effective dose of the conjugate of claim 1 wherein the conjugate is capable of associating with said target site; and detecting the biodistribution of said conjugate in said mammal to determine the presence or absence of said target site in said host.
Claim 6
Dependent Claim
14 words
The method of claim 4 wherein the calcified tissue target site is bone cancer.
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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) | 1996-04-12 | 1996-10-12 | 1997-04-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-04-12 | 2000-10-12 | 2001-04-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-04-12 | 2004-10-12 | 2005-04-13 | $7700.00 | Window Closed / Lapsed |