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US 6,806,363 B1Granted
Cobalamin conjugates useful as antitumor agents
AssigneesMayo Foundation for Medical Education and Research, Minnesota, Regents of the University
InventorsDouglas A. Collins, Henricus P. C. Hogenkamp
Life of this patent
Estimating the term…
Abstract
The invention provides cobalamin compounds linked to a neutron capture therapy target (e.g. Boron-10 or Gadolinium-157), and optionally linked to a detectable moiety, as well as pharmaceutical compositions comprising the compounds, and methods for using the compounds in medical diagnosis and therapy.
Claims57
A compound of formula I
- linked to a molecule comprising B-10, wherein X is CN, OH, CH3, adenosyl or a molecule comprising B-10 and optionally linked to a linker comprising a detectable radionuclide or a therapeutic radionuclide;
- or a pharmaceutically acceptable salt thereof.
A compound of formula I
- linked to one or more groups of the formula Q—L—W—Det, wherein X is CN, OH, CH3, adenosyl, a molecule comprising B-10 or Q—L—W—Det;
- wherein Det is a chelating group comprising Gd-157;
- L is a linker or absent;
- and W and Q are each independently —N(R)C(═O)—, —C(═O)N(R)—, —OC(═O)—, —C(═O)O—, —O—, —S—;
- —S(O)—, —S(O)2—, —N(R)—, —C(═O)—, or a direct bond;
- wherein each R is independently H or (C1-C6)alkyl;
- or a pharmaceutically acceptable salt thereof.
4 more elements
A compound of formula I
- linked to a molecule comprising B-10;
- wherein the compound of formula I is linked to a group of the formula Q—L—W—Det, wherein X is CN, OH, CH3, adenosyl, a molecule comprising B-10 or Q—L—W—Det;
- wherein
- a) Det is a chelating group comprising a therapeutic radionuclide or a diagnostic radionuclide;
- b) L is a linker or absent;
- and
- c) Q and W are each independently —N(R)C(═O)—, —C(═O)N(R)—, —OC(═O)—, —C(═O)O—, —O—, —S—, —S(O)—, —S(O)2—, —C(═O)—, —N(R)—, or a direct bond;
- wherein each R is independently H or (C1-C6)alkyl;
- or a pharmaceutically acceptable salt thereof.
6 more elements
A compound of formula I
- linked to a molecule comprising B-10, wherein X is CN, OH, CH3, adenosyl or a molecule comprising B-10 comprising at least one detectable radionuclide or a therapeutic radionuclide;
- or a pharmaceutically acceptable salt thereof.
A compound of formula I
- linked
- 1) to a molecule comprising B-10 or a chelating group comprising Gd-157;
- and
- 2) to at least one molecule of the formula Q—L—W—Det, wherein X is CN, OH, CH3, adenosyl, a molecule comprising B-10 or Q—L—W—Det;
- wherein each Det is independently a chelating group comprising a metallic radionuclide;
- each L is independently a linker or absent;
- and each W and Q are each independently —N(R)C(═O)—, —C(═O)N(R)—, —OC(═O)—, —C(═O)O—, —O—, —S—, —S(O)—, —S(O)2—, —C(═O)—, —N(R)—, or a direct bond;
- wherein each R is independently H or (C1-C6)alkyl;
- or a pharmaceutically acceptable salt thereof.
6 more elements
Dependencies are inferred from the claim text.