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US5407658A
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Analogs of cytochalasin B as radiopharmaceuticals for nuclear imaging of trans-membrane glucose transport
Assignee: University of California, San Diego
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Filing: 1994-05-24
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Granted: 1995-04-18
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Expires: 2014-05-24
Abstract
Abstract Analogs of cytochalasin B are used as radiopharmaceuticals to provide an image for the nuclear imaging of glucose transport across cell membranes. Like cytochalasin B, the analogs bind specifically to glucose transport protein, and in doing so, serve as markers indicating the amount of glucose transport protein present on the surfaces of cells. The analogs differ from cytochalasin B by the inclusion of a radionuclide in the region of the terminal phenyl group on cytochalasin B, where the radionuclide does not interfere with the binding specificity of the analog. Disclosed herein are such analogs as well as analogs with which readily accept radionuclides at the desired location on the structure, either by conjugation or substitution.
Inventors
- 👤 Robert S. Hattner
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 10:14
CPC Classifications
C; C07; C07D; C07D491/00; C07D491/02; C07D491/10; C07B; C07B59/00; C07B59/002
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
149 words
A method for detecting and imaging levels of glucose transport protein in a region of a patient's body where such levels are suspected to be abnormally high, said method comprising: (a) administering to said patient an imaging effective amount of a pharmaceutical agent comprising a compound having the formula ##STR9## in which R is a member selected from the group consisting of: a monovalent radionuclide, an aliphatic group, alicyclic group, or phenyl ring containing a monovalent radionuclide substituent, an aliphatic group, alicyclic group, or phenyl ring containing a polyvalent radionuclide substituent, and a chelate of a radionuclide, said radionuclide being selected from the group consisting of 121 I, 122 I, 123 I, 124 I, 125 I, 131 I, 74 Br, 75 Br, 76 Br, 77 Br, 34m Cl, 18 F, 211 At, 99m Tc, 111 In, 113m In and 67 Ga; and (b) imaging said region by nuclear imaging.
Claim 2
Independent Claim
149 words
A method for detecting and imaging levels of glucose transport protein in a region of a patient's body where such levels are suspected to be abnormally high, said method comprising: (a) administering to said patient an imaging effective amount of a pharmaceutical agent comprising a compound having the formula ##STR9## in which R is a member selected from the group consisting of: a monovalent radionuclide, an aliphatic group, alicyclic group, or phenyl ring containing a monovalent radionuclide substituent, an aliphatic group, alicyclic group, or phenyl ring containing a polyvalent radionuclide substituent, and a chelate of a radionuclide, said radionuclide being selected from the group consisting of 121 I, 122 I, 123 I, 124 I, 125 I, 131 I, 74 Br, 75 Br, 76 Br, 77 Br, 34m Cl, 18 F, 211 At, 99m Tc, 111 In, 113m In and 67 Ga; and (b) imaging said region by nuclear imaging.
Claim 3
Dependent Claim
33 words
A method in accordance with claim 1 in which R is a member selected from the group consisting of: a phenyl ring containing a monovalent radionuclide substituent, and a chelate of a radionuclide.
Claim 4
Dependent Claim
83 words
A method in accordance with claim 1 in which R is a member selected from the group consisting of: a phenyl ting containing a substituent which is a member selected from the group consisting of 121 I, 122 I, 123 I, 124 I, 125 I, 131 I, 74 Br, 75 Br, 76 Br, 77 Br, 34m Cl, 18 F and 211 At, and a chelate of a member selected from the group consisting of 99m Tc, 111 In, 113m In and 67 Ga.
Claim 5
Dependent Claim
113 words
A method in accordance with claim 1 in which R is a member selected from the group consisting of: a phenyl ring substituted in the meta-position with a member selected from the group consisting of 121 I, 122 I, 123 I, 124 I, 125 I, 131 I, 74 Br, 75 Br, 76 Br, 77 Br, 34m Cl, 18 F and 211 At, a chelate of a member selected from the group consisting of 111 In, 113m In and 67 Ga, in which the chelating ligand is a member selected from the group consisting of diethylenetriamine pentaacetic acid, ethylenediamine tetraacetic acid, nitrilotriacetic acid, and ethylene glycol-bis(β-aminoethyl ether)-N,N-tetraacetic acid, technetium diamino dimercaptide, and technetium hydrazinonicotinamide.
Claim 6
Dependent Claim
92 words
A method in accordance with claim 1 in which R is a member selected from the group consisting of: a phenyl ring substituted in the meta-position with a member selected from the group consisting of 121 I, 122 I, 123 I, 124 I, 125 I, and 131 I, a chelate of a member selected from the group consisting of 111 In, 113m In and 67 Ga, in which the chelating ligand is a member selected from the group consisting of diethylenetriamine pentaacetic acid and nitrilotriacetic acid, technetium diamino dimercaptide, and technetium hydrazinonicotinamide.
Claim 7
Dependent Claim
40 words
A method in accordance with claim 1 in which R is a phenyl ring substituted in the meta-position with a member selected from the group consisting of 121 I, 122 I, 123 I, 124 I, 125 I, and 131 I.
Claim 8
Dependent Claim
21 words
A method in accordance with claim 1 in which R is a phenyl ring substituted in the meta-position with 123 I.
References Cited (Backward Citations)
US4765972A
Cited
WO1993002105A1
Cited
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) | 1998-04-17 | 1998-10-17 | 1999-04-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2002-04-17 | 2002-10-17 | 2003-04-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2006-04-17 | 2006-10-17 | 2007-04-18 | $7700.00 | Window Closed / Lapsed |