Patent classifications
C07D475/04
Methods and Compositions for Improved F-18 Labeling of Proteins, Peptides and Other Molecules
The present application discloses compositions and methods of synthesis and use of .sup.18F- or .sup.19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the .sup.18F or .sup.19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may then be directly or indirectly attached to the targeting molecule. In other embodiments, the .sup.18F or .sup.19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the bifunctional chelating agent bound to .sup.18F- or .sup.19F-metal complex may be conjugated to the molecule to be labeled at a reduced temperature, e.g. room temperature.
Methods and Compositions for Improved F-18 Labeling of Proteins, Peptides and Other Molecules
The present application discloses compositions and methods of synthesis and use of .sup.18F- or .sup.19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the .sup.18F or .sup.19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may then be directly or indirectly attached to the targeting molecule. In other embodiments, the .sup.18F or .sup.19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the bifunctional chelating agent bound to .sup.18F- or .sup.19F-metal complex may be conjugated to the molecule to be labeled at a reduced temperature, e.g. room temperature.
SYNTHESIS AND COMPOSITION OF AMINO ACID LINKING GROUPS CONJUGATED TO COMPOUNDS USED FOR THE TARGETED IMAGING OF TUMORS
The present disclosure relates to compounds that are useful as near-infrared fluorescence probes, wherein the compounds include i) a pteroyl ligand that binds to a target receptor protein, ii) a dye molecule, and iii) a linker molecule that comprises an amino acid or derivative thereof. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds.
COMPOSITION COMPRISING (6S)-5-METHYL TETRAHYDROFOLIC ACID OR SALT THEREOF, AND PREPARATION AND USE THEREOF
Disclosed are a composition including (6S)-5-methyl tetrahydrofolic acid or a salt thereof, and preparation and use thereof. In the composition, the content of (6S)-5-methyl tetrahydrofolic acid or the salt thereof is not less than 98.0%, the content of a related impurity JK12A is not greater than 0.1%, and 5-methyl tetrahydropterioic acid is not detectable.
Compositions comprising folic acid derivatives, their preparations and methods of use
Described herein are methods for making folic acid derivatives, intermediates, pharmaceutical compositions and uses thereof.
Compositions comprising folic acid derivatives, their preparations and methods of use
Described herein are methods for making folic acid derivatives, intermediates, pharmaceutical compositions and uses thereof.
Stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid
The invention is directed towards stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid and its hemisulfate salt as well as pharmaceutical compositions and uses thereof in therapy, preferably chemotherapy.
18F-labelled folates
The present invention is directed towards new .sup.18F-folate radiopharmaceuticals, wherein the fluorine-18 is covalently linked to the aminobenzoyl moiety, which connects the condensed pyrimidine heterocycle to the amino acid portion within folate structures, as well as their precursors and their non-radioactive references, a method of their preparation, as well as their use in diagnosis of a cell or population of cells expressing a folate-receptor and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.
18F-labelled folates
The present invention is directed towards new .sup.18F-folate radiopharmaceuticals, wherein the fluorine-18 is covalently linked to the aminobenzoyl moiety, which connects the condensed pyrimidine heterocycle to the amino acid portion within folate structures, as well as their precursors and their non-radioactive references, a method of their preparation, as well as their use in diagnosis of a cell or population of cells expressing a folate-receptor and monitoring of cancer and inflammatory and autoimmune diseases and therapy thereof.
FOLATE SALTS
The invention relates to crystalline folate salts. The salt consists of a folate anion and an organic cation. The folate anion is 5-methyl-(6S)-tetrahydrofolic acid, and the cation is an organic compound which is an alkanolamine selected from the group consisting of choline, N-methylaminoethanol, 2-amino-2-methylpropanol and 2-dimethylaminoethanol.