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01/25/07 - USPTO Class 514 |  54 views | #20070021323 | Prev - Next | About this Page  514 rss/xml feed  monitor keywords

Use of a nitroxide or a prodrug thereof in the prophylactic and therapeutic treatment of cancer

Title: Use of a nitroxide or a prodrug thereof in the prophylactic and therapeutic treatment of cancer


Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Peptide Containing (e.g., Protein, Peptones, Fibrinogen, Etc.) Doai

Brief Patent Description - Full Patent Description - Patent Claims

The Patent Description & Claims data below is from USPTO Patent Application 20070021323, Use of a nitroxide or a prodrug thereof in the prophylactic and therapeutic treatment of cancer.


1. A method for the prophylactic or therapeutic treatment of cancer in an animal, which method comprises administering to an animal at risk for developing a cancer or having a cancer a nitroxide or a prodrug thereof in an amount sufficient to prevent or treat said cancer, wherein said cancer is susceptible to prevention or treatment by said nitroxide or prodrug thereof.

2. The method of claim 1, wherein said nitroxide or prodrug thereof is alicyclic or heterocyclic.

3. The method of claim 2, wherein said nitroxide or prodrug thereof is a compound of Formula I or II: wherein R.sub.1 is selected from the group consisting of H, OH, OZ, O., .dbd.O and Y, wherein Y is a leaving group, which can be converted to H, OH, O or .dbd.O by reaction with a nucleophilic agent, and Z is selected from the group consisting of a C I.sub.20 aliphatic group, a monocyclic aromatic group, a bicyclic aromatic group, a multicyclic aromatic group, a C.sub.1-20 alicyclic group, a noncarbon/nonoxygen moiety, a carbohydrate, a lipid, a nucleic acid and a protein, wherein R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently selected from the group consisting of a C.sub.1-20 alkyl group, a C.sub.2-20 alkenyl group, a C.sub.2-20 alkynyl group, and --CH.sub.2--[CR'R''].sub.m--CH.sub.3, wherein R' is selected from the group consisting of hydrogen, a C.sub.1-20 aliphatic group, a monocyclic aromatic group, a bicyclic aromatic group, and a multicyclic aromatic group, and R'' is selected from the group consisting of hydrogen, a C.sub.1-20 aliphatic group, a monocyclic aromatic group, a bicyclic aromatic group, a multicyclic aromatic group, a C.sub.1-20 alicyclic group, a noncarbon/nonoxygen moiety, a carbohydrate, a lipid, a nucleic acid, and a protein, m.ltoreq.30, and R.sub.2 and R.sub.3 or R.sub.4 and R.sub.5 can be connected through one or more members, each of which is independently selected from the group consisting of carbon and a heteroatom, wherein R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are independently selected from the group consisting of hydrogen, a hydroxyl group, a C.sub.1-20 aldehydic group, a C.sub.1-20 keto group, a primary amino group, a secondary amino group, a tertiary amino group, a sulfido group, a disulfido group, a sulfato group, a sulfito group, a sulfonato group, a sulfinato group, a sulfenato group, a sulfamato group, a metal-containing group, a silicone group, a halide, a C.sub.1-20 ester-containing group, a carboxyl group, a phosphato group, a phosphino group, a phosphinato group, a phosphonato group, a C.sub.1-20 alkyl group, a C.sub.2-20 alkenyl group, a C.sub.2-20 alkynyl group, and --CH.sub.2--[CR'R''].sub.m--CH.sub.3, wherein R' is selected from the group consisting of hydrogen, a C.sub.1-20 aliphatic group, a monocyclic aromatic group, a bicyclic aromatic group, and a multicyclic aromatic group, and R'' is selected from the group consisting of hydrogen, a C.sub.1-20 aliphatic group, a monocyclic aromatic group, a bicyclic aromatic group, a multicyclic aromatic group, a C.sub.1-20 alicyclic group, a noncarbon/nonoxygen moiety, a carbohydrate, a lipid, a nucleic acid and a protein, and m.ltoreq.30, and wherein any one of R.sub.6, R.sub.7, R.sub.8 and R.sub.9 can be attached covalently or noncovalently to a polymer of synthetic or natural origin, wherein in Formula I, one of R.sub.6 and R.sub.7 and one of R.sub.8 and R.sub.9 can be absent such that a double bond joins the two carbon atoms to which the remaining R groups are attached, wherein n=0-20 in Formula I, and n=1-20 in Formula II, wherein X is a heteroatom, and wherein R.sub.10 and R.sub.11 are independently selected from the group consisting of a C.sub.1-20 aliphatic group, a monocyclic aromatic group, a bicyclic aromatic group, a multicyclic aromatic group, a C.sub.1-20 aliphatic/aromatic group, a heteroatomic group, a C.sub.1-20 ether-containing group, a C.sub.1-20 keto group, a C.sub.1-20 aldehydic group, a carboxamido group, a cyano group, an amino group, a carboxyl group, a selenium-containing group, a sulfato group, a sulfito group, a sulfenato group, a sulfinato group, and a sulfonato group, and wherein R.sub.10 and R.sub.11 can be connected through an aliphatic group and/or an aromatic group, or R.sub.10 and/or R.sub.11 can comprise a member selected from the group consisting of a carbohydrate, a lipid, a nucleic acid and a protein.

4. The method of claim 3, wherein said aliphatic group is branched, substituted and/or unsaturated.

5. The method of claim 4, wherein said aliphatic group is substituted with a member selected from the group consisting of oxygen, phosphorus, selenium, sulfur and nitrogen.

6. The method of claim 3, wherein said aromatic group comprises a five- or six-membered ring, in which each of the five or six members is independently selected from the group consisting of carbon and a heteroatom.

7. The method of claim 6, wherein said heteroatom is selected from the group consisting of nitrogen, oxygen, sulfur, phosphorus and boron.

8. The method of claim 3, wherein the metal of said metal-containing group is selected from the group consisting of a transition metal and a lanthanide.

9. The method of claim 6, wherein said aromatic group is substituted.

10. The method of claim 9, wherein said aromatic group is substituted with a heteroatom.

11. The method of claim 10, wherein said heteroatom is selected from the group consisting of nitrogen, oxygen, sulfur, phosphorus and boron.

12. The method of claim 3, wherein said alicyclic group is substituted and/or unsaturated.

13. The method of claim 11, wherein said alicyclic group is substituted with a heteroatom.

14. The method of claim 3, wherein said amino group is substituted.

15. The method of claim 14, wherein said amino group is substituted with up to three substituents selected from the group consisting of a C.sub.1-20 aliphatic group, a monocyclic aromatic group, a bicyclic aromatic group, a multicyclic aromatic group, and a C.sub.1-20 alicyclic group.

16. The method of claim 15, wherein said aromatic group comprises a five- or six-membered ring, in which each of the five or six members is independently selected from the group consisting of carbon and a heteroatom.

17. The method of claim 16, wherein said heteroatom is selected from the group consisting of nitrogen, oxygen, sulfur, phosphorus and boron.

18. The method of claim 15, wherein said aromatic group is substituted.

19. The method of claim 18, wherein said aromatic group is substituted with a heteroatom.

20. The method of claim 19, wherein said heteroatom is selected from the group consisting of nitrogen, oxygen, sulfur, phosphorus and boron.

21. The method of claim 3, wherein said noncarbon/nonoxygen moiety is selected from the group consisting of boron, sulfur, nitrogen and phosphorus.

22. The method of claim 1, wherein said cancer is due to a genetic defect of a cancer regulatory gene or a tumor suppressor gene.

23. The method of claim 22, wherein said tumor suppressor gene is the p53 gene.

24. The method of claim 2, wherein said cancer is due to a genetic defect of a cancer regulatory gene or a tumor suppressor gene.

25. The method of claim 24, wherein said tumor suppressor gene is the p53 gene.

26. The method of claim 3, wherein said cancer is due to a genetic defect of a cancer regulatory gene or a tumor suppressor gene.

27. The method of claim 26, wherein said tumor suppressor gene is the p53 gene.

Brief Patent Description - Full Patent Description - Patent Claims

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