Patent classifications
A61K51/0472
Tetrahydroxamate chelators of zirconium89 and niobium90 for use in diagnostic applications
Disclosed is a compound of formula (I) or (II) in which R.sup.1-R.sup.4, R.sup.1-R.sup.5, Z.sup.1+-Z.sup.4, and Z.sup.1-Z.sup.4 are as described herein. Also disclosed are a .sup.89Zr- or .sup.90Nb-containing complex of a compound of formula (I) or (II) and a method for obtaining a diagnostic image, such as a positron emission tomography (PET) image.
NEW 2, 1 L -DIAZA-[3.3](2,6)PYRIDINOPHANE COMPOUNDS AND THEIR APPLICATION AS LIGANDS OF ESSENTIAL METAL ION BASED MRI CONTRAST AGENTS AND 52MN BASED PET CONTRAST AGENTS
The one subject of the invention is the compounds of general formula (I), their isomers, their physiologically acceptable salts and/or Mn(II), Fe(II), Fe(III), Co(II) and Ni(II) complexes. The other subject of the invention is the application of the above compounds. The compounds of general formula (I): wherein NRR.sub.1 group may refer to: a) NRR.sub.1 with N atom in the ring means a ring of 4 to 7, that in certain cases may contain another heteroatom, and in specific cases the ring may be replaced with an aryl group (of 5 to 7 carbon atoms) substituted with COOH, OH, OCH.sub.3, NO.sub.2, NH.sub.2, NCS, NHS-activated ester, aryl (of 5 to 7 carbon atoms), or nitro-, amino- or isothiocyanate group, or b) in the NRR.sub.1 group R means a H atom, alkyl, aryl, nitroaryl, aminoaryl or isothiocyanate-aryl group (of 1 to 6 carbon atoms) and R.sub.4 is a H atom, alkyl (of 1 to 6 carbon atoms) or (CH.sub.2).sub.nCOOH group, whereas n=1 to 10 integer, or c) NRR.sub.1 group is one of the following groups: (formula II) whereas R.sub.2 is a H atom, carboxyl- or alkyl-carbonyl group (of 1 to 4 carbon atoms); (formula III) and R.sub.2 is a H atom or alkyl or aryl group (of 1 to 6 carbon atoms), and X means independently from one another H atom, CH.sub.3, COOH, OH, OCH.sub.3, alkoxy- (of 2 to 6 carbon atoms), NO.sub.2, NH.sub.2, NCS, NHS-activated ester, alkyl (of 2 to 12 carbon atoms) or aryl (of 5 to 7 carbon atoms) group, in certain cases the latter may be substituted with hydroxyl, hydroxyalkyl (of 1 to 6 carbon atoms), nitro, amino or isothiocyanate group.
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Radiolabeling and formulation for scale up of .SUP.64.Cu-DOTATATE
The present disclosure relates to methods to create a robust procedure capable of supplying commercial quantities of a radioactive diagnostic agent indicated for use with positron emission tomography (PET) for localization of somatostatin receptor positive neuroendocrine tumors (NETs) in adult patients.
Labeled inhibitors of prostate specific membrane antigen (PSMA) biological evaluation, and use of imaging agents
The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+ PC3 PIP tumors.
RADIOLABELING AND FORMULATION FOR SCALE UP OF 64Cu-DOTATATE
The present disclosure relates to methods to create a robust procedure capable of supplying commercial quantities of a radioactive diagnostic agent indicated for use with positron emission tomography (PET) for localization of somatostatin receptor positive neuroendocrine tumors (NETs) in adult patients.
LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) BIOLOGICAL EVALUATION, AND USE OF IMAGING AGENTS
The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+ PC3 PIP tumors.
COUPLED IDENTIFICATION AND TREATMENT OF CANCER
Provided are methods to treat cancer, in which (1) a patient is first identified as having a cancer that is likely to be susceptible to gallium therapy, by the use of a gallium scan or other procedure that shows whether the cancer is gallium-avid, and (2) the patient is then treated with a pharmaceutically acceptable gallium composition.
RADIOTRACERS AND THERAPEUTICS BINDING TO FIBROBLAST ACTIVATION PROTEIN (FAP)
The present invention relates to a ligand-SIFA conjugate, comprising, within in a single molecule two separate moieties: (a) one or more ligands which are capable of binding to Fibroblast Activation Protein (FAP), and (b) a silicon-fluoride acceptor (SI FA) moiety which comprises a covalent bond between a silicon atom and a fluorine atom.
Labeled inhibitors of prostate specific membrane antigen (PSMA) biological evaluation, and use of imaging agents
The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+PC3 PIP tumors.
Compositions, methods of synthesis and use of carbohydrate targeted agents
The invention provides D02S derivatives conjugated to monosaccharide ligands directly or through a linker and optionally chelated to a metal, wherein the D02S derivatives having the following structure: wherein R.sub.1, R.sub.2 are each independently OH or O-alkyl; R.sub.1 is a hydrogen, a linker, or a ligand; R.sub.3 is a linker and/or a ligand; and n is an integer from 1 to 10; the linker is an amino acid, a peptide, an amino alcohol, a polyethylylene glycol, an alkyl, an alkenyl, an alkynyl, an azide, an aromatic compound, a carboxylic acid, or an ester, the alkyl, alkenyl, or alkynyl is optionally substituted with an alkyl, a halogen, a nitro group, a hydroxyl group, an amino group, or a carboxyl group; the ligand is a GLUT1 targeting moiety.