초록 ▼

A compound useful for in vivo imaging of organs and tumors is provided of formula: wherein is a cobalamin, is derived from a corrin carboxylic acid group of said cobalamin, Y is a linking group and X is a chelating group, optionally comprising a detectable radionuclide or a paramagnetic m

A compound useful for in vivo imaging of organs and tumors is provided of formula: wherein is a cobalamin, is derived from a corrin carboxylic acid group of said cobalamin, Y is a linking group and X is a chelating group, optionally comprising a detectable radionuclide or a paramagnetic metal ion, and n is 1-3.

대표청구항 ▼

What is claimed is: 1. A method of imaging a tumor in a mammal comprising: administering an effective amount of a compound of the formula: to the mammal, 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 gro

What is claimed is: 1. A method of imaging a tumor in a mammal comprising: administering an effective amount of a compound of the formula: to the mammal, 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; DET is independently selected from a chelating group comprising a radionuclide and a chelating group comprising a paramagnetic metal ion; n is 2-3; or a pharmaceutically acceptable salt thereof; wherein each Y is independently selected from a divalent monomer, dimer, and trimer of--N(H)(CH2)2-6N(H)--. 2. 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; DET is independently selected from a chelating group comprising a radionuclide and a chelating group comprising a paramagnetic metal ion; and n is 2-3; or a pharmaceutically acceptable salt thereof; wherein each Y is independently selected from a divalent monomer, dimer, and trimer of--N(H)(CH2)2-6N(H)--. 3. The compound of claim 2, wherein each DET is a chelating group comprising a radionuclide. 4. The compound of claim 3, 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-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. 5. The compound of claim 4, wherein each radionuclide is independently selected from In111, Yt90, Tc99, Gd153, and Re186. 6. The compound of claim 2, wherein each chelating group is independently selected from EDTA, DTPA, DOTA, TETA, and DCTA. 7. The compound of claim 6, wherein each chelating group is DTPA. 8. The compound of claim 2, wherein each Y is--N(H)(CH2)4N(H)--. 9. The compound of claim 2, wherein n is 2. 10. The compound of claim 2, wherein n is 3. 11. A met method of treating a tumor in a mammal comprising: administering an effective amount of a compound of the formula: to the mammal, 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; DET is independently selected from a chelating group comprising a radionuclide and a chelating group comprising a paramagnetic metal ion; n is 2-3; or a pharmaceutically acceptable salt thereof; wherein each Y is independently selected from a divalent monomer, dimer, and trimer of--N(H)(CH2)2-6N(H)--. 12. The method of claim 1 or 11, wherein each DET is a detectable chelating group comprising a detectable radionuclide. 13. The method of claim 12, wherein each detectable 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-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. 14. The method of claim 13, wherein the radionuclide is independently selected from In111, Yt90, Tc99, Gd153, and Re186. 15. The method of claim 1 or 11, wherein each chelating group is independently selected from EDTA, DTPA, DOTA, TETA, and DCTA. 16. The method of claim 15, wherein each chelating group DTPA. 17. The method of claim 1 or 11, wherein each Y is--N(H)(CH2)4N(H)--. 18. The method of claim 1 or 11, wherein n is 2. 19. The method of claim 1 or 11, wherein n is 3. 20. The method of claim 1, comprising administering to the mammal a detectable amount of the compound in combination with a pharmaceutically acceptable vehicle, and detecting the presence of the compound in a tumor of the kidney, liver, pancreas, spleen, or gastrointestinal tract of the mammal. 21. The method of claim 11, comprising administering to the mammal an effective amount of the compound in combination with a pharmaceutically acceptable vehicle, and treating a tumor of the kidney, liver, pancreas, spleen, or gastrointestinal tract of the mammal. 22. The method of claim 20 or 21, wherein the administration is parenteral. 23. The method of claim 22, wherein the administration is intravenous. 24. The method of claim 23, wherein the administration is intraperitoneal. 25. The method of claim 20 or 21, wherein the administration is oral.