Nucleosides for imaging and treatment applications
First Claim
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1. A compound of the formula:
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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 alkoxyl 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.
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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
21 Claims
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1. A compound of the formula:
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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 alkoxyl 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. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 15, 16, 17, 18, 19, 20, 21)
contacting a first molecule of the formula wherein R1, R2 and R5 may be the same or different and are blocking groups, R3 is a leaving group and R4, is H, with a second molecule containing a label under conditions causing the transfer of the label to the position occupied by R4; and contacting the resultant labeled first molecule with a molecule having the structure wherein A=N, C;
B=H, hydroxy, halogen, acyl (C1-C6), alkyl (C1-C6), 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 alkoxyl or halogen.
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5. A method according to claim 4, wherein the label is a positron emitter.
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6. A method according to claim 5, wherein the label is 18F.
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7. A method according to claim 4, wherein the second molecule containing a label is selected from the group consisting of KHF2 and diethylamino-sulfur trifluoride (DAST).
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8. A compound according to claim 1, wherein E is selected from H, methyl and I.
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9. A compound according to claim 2, wherein E is selected from H, methyl and I.
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10. A compound according to claim 1, wherein E is a substituent readily cleaved in the body to generate H, methyl or I.
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15. A compound according to claim 1, wherein A=N, B=H, D=O, and E=I.
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16. A compound according to claim 15, wherein X=Y=Z=H and W=18F.
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17. A compound according to claim 1, wherein at least one of X, Y or Z is 18F.
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18. A compound according to claim 1, wherein at least one D is S.
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19. A compound according to claim 1, wherein A is C.
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20. A compound according to claim 1, wherein B is H, halogen, acyl or alkyl.
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21. A compound according to claim 1, phosporylated at the 5′
- -hydroxyl group.
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11. A compound according of the formula
wherein 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 may be the same or different and are selected from H, hydroxy, halogen, alkyl (C1-C6) substituted alkyl (C1-C6), alkoxy (C1-C6) and substituted alkoxy (C1-C6).
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13. A compound of the formula
wherein 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 may be the same or different and are selected from H, hydroxy, halogen, alkyl (C1-C6) substituted alkyl (C1-C6), alkoxy (C1-C6) and substituted alkoxy (C1-C6).
Specification
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Current AssigneeUnited States As Represented By The Secretary Department of Health and Human Services
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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 NumberUS09/530,276Time in Patent Office1,411 DaysField of Search536/22.1, 536/23.1, 536/24.3, 536/25.3, 536/26.6, 514/1, 514/44US Class Current514/44.00RCPC Class CodesC07H 19/06 Pyrimidine radicalsC07H 21/00 Compounds containing two or...
