Nucleosides for imaging and treatment applications
First Claim
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1. A method of treating tumors or cancer, comprising:
- administering a uridine analogue selected by a method comprising the steps of;
providing a uridine analogue unsubstituted in the 5-position;
testing said uridine analog for activation by thymidylate synthase; and
selecting said uridine analog when found to be activated by thymidylate synthase;
in an effective amount to reduce or inhibit replication or spread of tumor or cancer cells.
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Abstract
Methods of diagnosing and/or of treating tumors by administering a nucleoside analog which is activated by thymidylate synthase and/or thymidine kinase enzyme into a diagnostic or toxic metabolite, and uridine analog 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
12 Claims
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1. A method of treating tumors or cancer, comprising:
- administering a uridine analogue selected by a method comprising the steps of;
providing a uridine analogue unsubstituted in the 5-position;
testing said uridine analog for activation by thymidylate synthase; and
selecting said uridine analog when found to be activated by thymidylate synthase;
in an effective amount to reduce or inhibit replication or spread of tumor or cancer cells. - View Dependent Claims (6, 7, 8, 9)
wherein; A=N, C;
B=H, hydroxy, halogen, acyl (C1-C6), alkyl, C1-C6),alkoxy (C1-C6) D=O, S, NH2; and
G=substituted or unsubstituted cyclic sugar, substituted or unsubstituted acyclic sugar, substituted or unsubstituted mono, di, or tri-phospho-cyclic-sugar phosphate;
substituted or unsubstituted mono, di, or tri-phospho-acyclic-sugar phosphate;
substituted or unsubstituted mono, di, or tri-phospho-cyclic sugar analogues, substituted or unsubstituted mono, di, or tri-phospho-acyclic sugar analogues wherein the substituents are alkyl (C1-C6) alkoxy (C1 to C6), halogen.
- administering a uridine analogue selected by a method comprising the steps of;
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2. A method of alleviating cytopathic effects associated with tumors, comprising administering to an afflicted patient an effective amount of a uridine analogue selected by a method comprising the steps of:
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providing a uridine analogue unsubstituted in the 5-position;
testing said uridine analog for activation by thymidylate synthase; and
selecting said uridine analog when found to be activated by thymidylate synthase;
such that said cytopathic effects are alleviated. - View Dependent Claims (10, 11)
wherein; A=N, C;
B=H, hydroxy, halogen, acyl (C1-C6), alkyl, C1-C6),alkoxy (C1-C6) D=O, S, NH2; and
G=substituted or unsubstituted cyclic sugar, substituted or unsubstituted acyclic sugar, substituted or unsubstituted mono, di, or tri-phospho-cyclic-sugar phosphate;
substituted or unsubstituted mono, di, or tri-phospho-acyclic-sugar phosphate;
substituted or unsubstituted mono, di, or tri-phospho-cyclic sugar analogues, substituted or unsubstituted mono, di, or tri-phospho-acyclic sugar analogues wherein the substituents are alkyl (C1-C6) alkoxy (C1 to C6), halogen.
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11. The method of claim 2, wherein the uridine analogue is selected form the group FAU, d-Urd and ara-U.
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3. A composition for reducing or inhibiting the replication or spread of tumor cells, comprising:
- a uridine analogue selected by a method comprising the steps of;
providing a uridine analogue unsubstituted in the 5-position;
testing said uridine analog for activation by thymidylate synthase; and
selecting said uridine analog when found to be activated by thymidylate synthase;
and a pharmaceutically acceptable carrier. - View Dependent Claims (4, 5)
wherein; A=N, C;
B=H, hydroxy, halogen, acyl (C1-C6), alkyl, C1-C6), alkoxy (C1-C6) D=O, S, NH2; and
G=substituted or unsubstituted cyclic sugar, substituted or unsubstituted acyclic sugar, substituted or unsubstituted mono, di, or tri-phospho-cyclic-sugar phosphate;
substituted or unsubstituted mono, di, or tri-phospho-acyclic-sugar phosphate;
substituted or unsubstituted mono, di, or tri-phospho-cyclic sugar analogues, substituted or unsubstituted mono, di, or tri-phospho-acyclic sugar analogues wherein the substituents are alkyl (C1-C6) alkoxy (C1 to C6), halogen.
- a uridine analogue selected by a method comprising the steps of;
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12. A method of treating cancer, comprising:
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administering a uridine analog in an amount effective to inhibit the replication or spread of cancer cells, said uridine analog selected by a method comprising the steps of;
providing a uridine analogue unsubstituted in the 5-position;
testing said uridine analog for activation by thymidylate synthase; and
selecting said uridine analog when found to be activated by thymidylate synthase.
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Specification