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06/25/09 - USPTO Class 424 | 1 views | #20090162281 | Prev - Next | About this Page

Radionuclide labeling of vitamin b12 and co-enzymes thereof

Title: Radionuclide labeling of vitamin b12 and co-enzymes thereof

Brief Patent Description - Full Patent Description - Patent Claims

The Patent Description & Claims data below is from USPTO Patent Application 20090162281, Radionuclide labeling of vitamin b12 and co-enzymes thereof.

What is claimed is:

1. A pharmaceutically acceptable salt of compound of the formula: wherein the moiety is cobalamin, is a b-, d-, or e-carboxy residue of cobalamin; X is CN, OH, methyl, or adenosyl; Y is a linking group; and DET is independently selected from a chelating group comprising a radionuclide and a chelating group comprising a paramagnetic metal ion.

2. The compound of claim 1, wherein C(═O) is the b-carboxy residue of cobalamin.

3. The compound of claim 1, wherein C(═O) is the d-carboxy residue of cobalamin.

4. The compound of claim 1, wherein each DET is a chelating group comprising a radionuclide.

5. The compound of claim 4, wherein each radionuclide is independently selected from Antimony-124, Antimony-125, Arsenic-74, Barium-140, Beryllium-7, Bismuth-206, Bismuth-207, Cadmium-109, Cadmium-115, Cadmium-115m, Calcium-45, Cerium-139, Cerium-141, Cerium-144, Cesium-137, Chromium-51, Cobalt-55, Cobalt-56, Cobalt-57, Cobalt-58, Cobalt-60, Cobalt-64, Erbium-169, Europium-152, Gadolinium-153, Gold-195, Gold-199, Hafnium-175, Hafnium-175-181, Indium-111, Iridium-192, Iron-55, Iron-59, Krypton-85, Lead-210, Manganese-54, Mercury-197, Mercury-203, Molybdenum-99, Neodymium-147, Neptunium-237, Nickel-63, Niobium-95, Osmium-185+191, Palladium-103, Platinum-195m, Praseodymium-143, Promethium-147, Protactinium-233, Radium-226, Rhenium-186, Rhenium-188, Rubidium-86, Ruthenium-103, Ruthenium-106, Scandium-44, Scandium-46, Selenium-75, Silver-10m, Silver-111, Sodium-22, Strontium-85, Strontium-89, Strontium-90, Sulfur-35, Tantalum-182, Technetium-99m, Tellurium-125, Tellurium-132, Thallium-204, Thorium-228, Thorium-232, Thallium-170, Tin-113, Titanium-44, Tungsten-185, Vanadium-48, Vanadium-49, Ytterbium-169, Yttrium-88, Yttrium-90, Yttrium-91, Zinc-65, and Zirconium-95.

6. The compound of claim 5, wherein each radionuclide is independently selected from In111, Yt90, Tc99, Gd153, and Re186.

7. The compound of claim 1, wherein each chelating group is independently selected from EDTA, DTPA, DOTA, TETA, and DCTA.

8. The compound of claim 7, wherein each chelating group is DTPA.

9. The compound of claim 1, wherein each Y is independently selected from a divalent monomer, dimer, and trimer of —N(H)(CH2)2-6N(H)—.

10. The compound of claim 9, wherein each Y is —N(H)(CH2)4N(H)—.

11. A diagnostic or therapeutic unit dose form comprising a compound of the formula: wherein the moiety is cobalamin, is a b-, d-, or e-carboxy residue of cobalamin; X is CN, OH, methyl, or adenosyl; Y is a linking group; and DET is independently selected from a chelating group comprising a radionuclide and a chelating group comprising a paramagnetic metal ion; or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable vehicle.

12. The unit dose form of claim 11, wherein C(═O) is the b-carboxy residue of cobalamin.

13. The unit dose form of claim 11, wherein C(═O) is the d-carboxy residue of cobalamin.

14. The unit dose form of claim 11, wherein each DET is a chelating group comprising a radionuclide.

15. The unit dose form of claim 14, wherein each radionuclide is independently selected from Antimony-124, Antimony-125, Arsenic-74, Barium-140, Beryllium-7, Bismuth-206, Bismuth-207, Cadmium-109, Cadmium-115, Cadmium-15m, Calcium-45, Cerium-139, Cerium-141, Cerium-144, Cesium-137, Chromium-51, Cobalt-55, Cobalt-56, Cobalt-57, Cobalt-58, Cobalt-60, Cobalt-64, Erbium-169, Europium-152, Gadolinium-153, Gold-195, Gold-199, Hafnium-175, Hafnium-175-181, Indium-111, Iridium-192, Iron-55, Iron-59, Krypton-85, Lead-210, Manganese-54, Mercury-197, Mercury-203, Molybdenum-99, Neodymium-147, Neptunium-237, Nickel-63, Niobium-95, Osmium-185+191, Palladium-103, Platinum-195m, Praseodymium-143, Promethium-147, Protactinium-233, Radium-226, Rhenium-186, Rhenium-188, Rubidium-86, Ruthenium-103, Ruthenium-106, Scandium-44, Scandium-46, Selenium-75, Silver-110m, Silver-111, Sodium-22, Strontium-85, Strontium-89, Strontium-90, Sulfur-35, Tantalum-182, Technetium-99m, Tellurium-125, Tellurium-132, Thallium-204, Thorium-228, Thorium-232, Thallium-170, Tin-113, Titanium-44, Tungsten-185, Vanadium-48, Vanadium-49, Ytterbium-169, Yttrium-88, Yttrium-90, Yttrium-91, Zinc-65, and Zirconium-95.

16. The unit dose form of claim 11, wherein each radionuclide is independently selected from In111, Yt90, Tc99 Gd153 and Re186.

17. The unit dose form of claim 11, wherein each chelating group is independently selected from EDTA, DTPA, DOTA, TETA, and DCTA.

18. The unit dose form of claim 17, wherein each chelating group is DTPA.

19. The unit dose form of claim 11, wherein each Y is independently selected from a divalent monomer, dimer, and trimer of —N(H)(CH2)2-6N(H)—.

20. The unit dose form of claim 19, wherein each Y is —N(H)(CH2)4N(H)—.

21. The unit dose form of claim 11, formulated for parenteral administration.

22. The unit dose form of claim 11, formulated for intravenous administration.

23. The unit dose form of claim 11, formulated for intravenous administration.

24. The unit dose form of claim 11, formulated for intraperitoneal administration.

25. The unit dose form of claim 11, formulated for oral administration.

26. The unit dose form of claim 11, wherein the pharmaceutically acceptable vehicle is saline.

Brief Patent Description - Full Patent Description - Patent Claims

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