Nucleosides for imaging and treatment applications
First Claim
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1. A method of imaging an organism, comprising the steps of:
- contacting the organism to be imaged with a compound of the formula;
wherein;
A=N, C;
B=H, hydroxy, halogen, acyl(C1-C6), alkyl alkoxy(C1-C6) D=O, S, NH2;
E=H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkoxy, substituted alkoxy, halogen, or any substituent which is readily cleaved in the body to generate H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkoxy, substituted alkoxy, or halogen;
at least one of W, X, Y, Z is a label or a label containing moiety having sufficient isotopic activity for imaging and the remainder of W, X, Y, Z=H, hydroxy, halogen, alkyl(C1-C6) substituted alkyl(C1-C6), alkoxy(C1-C6), substituted alkoxy(C1-C6);
J=C, S; and
K=O, C; and
imaging the organism.
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Abstract
Methods of diagnosing and/or of treating tumors by administering a nucleoside analogue which is activated by thymidylate synthase and/or thymidine kinase enzyme into a diagnostic or toxic metabolite, and uridine analogue compounds, and compositions of same having a pharmaceutically acceptable carrier. For diagnostic applications, compounds containing a label and methods of use of such compounds are described.
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Citations
18 Claims
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1. A method of imaging an organism, comprising the steps of:
- contacting the organism to be imaged with a compound of the formula;
wherein; A=N, C;
B=H, hydroxy, halogen, acyl(C1-C6), alkyl alkoxy(C1-C6) D=O, S, NH2;
E=H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkoxy, substituted alkoxy, halogen, or any substituent which is readily cleaved in the body to generate H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkoxy, substituted alkoxy, or halogen;
at least one of W, X, Y, Z is a label or a label containing moiety having sufficient isotopic activity for imaging and the remainder of W, X, Y, Z=H, hydroxy, halogen, alkyl(C1-C6) substituted alkyl(C1-C6), alkoxy(C1-C6), substituted alkoxy(C1-C6);
J=C, S; and
K=O, C; and
imaging the organism. - View Dependent Claims (3, 4, 5, 6, 7, 8, 9, 10)
- contacting the organism to be imaged with a compound of the formula;
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2. A method of determining the proliferation rate of a tissue, comprising the steps of:
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contacting the tissue with a compound of the formula;
wherein;
A=N, C;
B=H, hydroxy, halogen, acyl(C1-C6), alkyl alkoxy(C1-C6) D=0, S, NH2;
E=H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkoxy, substituted alkoxy, halogen, or any substituent which is readily cleaved in the body to generate H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkoxy, substituted alkoxy, or halogen;
at least one of W, X, Y, Z is a label or a label containing moiety having sufficient isotopic activity for imaging and the remainder of W, X, Y, Z=H, hydroxy, halogen, alkyl(C1-C6) substituted alkyl(C1-C6), alkoxy(C1-C6), substituted alkoxy(C1-C6);
J=C, S; and
K=O, C;
imaging the tissue; and
determining the amount of the compound incorporated into the tissue, wherein the amount of the compound incorporated into the tissue correlates to the proliferation rate of the tissue. - View Dependent Claims (11, 12, 13, 14, 15, 16, 17, 18)
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Specification
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Current AssigneeUnited States Department Of Health And Human Services (Government of the United States of America)
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Original AssigneeUnited States Department Of Health And Human Services (Government of the United States of America)
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InventorsAnderson, Lawrence, Collins, Jerry M., Klecker, Raymond W., Katki, Aspandiar G.
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Primary Examiner(s)Riley, Jezia
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Application NumberUS09/941,551Publication NumberTime in Patent Office866 DaysField of Search536/22.1, 536/23.1, 536/24.3, 536/25.3, 514/1, 514/44US Class Current514/44.00RCPC Class CodesC07H 19/06 Pyrimidine radicalsC07H 21/00 Compounds containing two or...
