Patent classifications
A61K51/0453
COMPOUND FOR SPECIFICALLY BINDING TO AMYLOID B-PROTEIN
Provided is a compound for specifically binding to amyloid -protein. The compound has thereon a nuclide with a large thermal neutron capture cross section and the compound is capable of specifically binding to the amyloid -protein. The property of the compound allows it to be used in conjunction with a neutron capture therapy device to eliminate amyloid -protein. Similarly, when the compound is labelled with radioactive element .sup.11C, the compound can also be used in conjunction with PET/CT for determining the part of the brain where amyloid -protein is deposited, for diagnosing Alzheimer's disease. Also disclosed is a preparation process for the compound. The beneficial effect of the present disclosure is to make the therapy and diagnosis of Alzheimer's disease more targeted by providing the compound for specifically binding to amyloid -protein.
Method for Producing Flutemetamol
Provided is a method for producing flutemetamol including the steps of: reacting a precursor compound represented by a predetermined general formula with a radioactive fluoride to obtain a .sup.18F labeling compound represented by a predetermined general formula; allowing a strong base to act on the reaction mixture of the above step containing the precursor compound and the .sup.18F labeling compound; after the above step, purifying the .sup.18F labeling compound using a reverse phase solid phase extraction cartridge; and removing a protective group to obtain [.sup.18F]flutemetamol.
PET probes of radiofluorinated carboximidamides for IDO-targeted imaging
.sup.18F labeled IDO1 imaging constructs are constructed for positron emission tomography (PET). Synthetic methodology involves the coupling of a 1-fluoro-2-halo-4-aminobenzene and a 4-mino-N-hydroxy-1,2,5-oxadiazole-3-carboximidoyl chloride wherein at least one of the coupled compounds comprises an .sup.18F. The .sup.18F labeled IDO1 imaging constructs are useful for imaging cancer cells in a patient.
18/19F-LABELLED COMPOUNDS WHICH TARGET THE PROSTATE SPECIFIC MEMBRANE ANTIGEN
This disclosure relates to novel compounds comprising a zwitterionic trifluoroborate prosthetic group which target prostate-specific membrane antigen (PSMA), e.g. in prostate cancer. The compounds have Formula I, wherein each R1 is an anionic group, L is a linker and R2B-F3 is N(R.sup.3).sub.2CH.sub.2BF.sub.3, a pyridinium group substituted with BF.sub.3 or methyl BF.sub.3, or an azole group substituted with methyl BF3. Methods and uses of imaging and treating PSMA-expressing cancers are also disclosed.
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METHOD OF DIAGNOSING AND/OR MONITORING THERAPY OF ATHEROSCLEROSIS
The present invention is directed to novel non-invasive diagnostic took to dispose numerous disease states and/or conditions. The presets invention, represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these disease states. The novel imaging probe is capable of detecting infected cells, as well tissue. The methods described herein are able to diagnose, treat and/or monitor the therapy of numerous diseases and conditions including atherosclerosis, atherothrombosis, cerebral vascular disease, cerebral ischemia, cerebral infarct and meningitis as well as pneumonitis, pericarditis, multiple sclerosis, lupus erythematosus and pancreatitis, among others.
NEUTRON CAPTURE THERAPY SYSTEM FOR ELIMINATING AMYLOID ß-PROTEIN
A neutron capture therapy system capable of eliminating amyloid -protein includes a neutron capture therapy device and a compound capable of specifically binding to the amyloid -protein having a nuclide with a large thermal neutron capture cross section. The neutron capture therapy device includes a neutron source, a beam shaping assembly and a collimator, the neutrons released by the neutron source pass through the beam shaping assembly and are slowed into a neutron beam within a certain energy range. The neutron beam irradiates the compound, and the energy generated by the reaction thereof can destroy the structure of the amyloid -protein. The neutron capture therapy system can specifically eliminate the amyloid -protein, and reduce the damage to the tissues surrounding the amyloid -protein.
DEVELOPMENT OF A NOVEL PET PROBE FOR TARGETED BACTERIAL IMAGING
A probe for positron emission tomography (PET) is disclosed. The probe is selected from the group consisting of yersini-abactin (Ybt) labeled with Copper-64; staphylopine (StP) labeled with Copper-64; yersiniabactin (Ybt) labeled with Zirconium-89; and staphylopine (StP) labeled with Zirconium-89.
PSMA targeted fluorescent agents for image guided surgery
Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.
NOVEL DEUTERIUM SUBSTITUTED POSITRON EMISSION TOMOGRAPHY (PET) IMAGING AGENTS AND THEIR PHARMACOLOGICAL APPLICATION
The present invention relates to deuterated compounds according to Formula I-A, Formula II-A, Formula II-D, and Formula III-A. These compounds can be used as PET imaging agents for evaluating Parkinson's Disease, Alzheimer Disease, and for determining specific serotonin reuptake inhibitor (SSRIi) activity for treatment of depression. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I-A, Formulae II-A, Formula II-D, or Formula III-A, or a pharmaceutically acceptable salt thereof.
Probes for 18F Positron Emission Tomography Imaging
The present invention contemplates a method for synthesizing [.sup.18F] fluoride complexes suitable for performing radio-labeling reactions to generate [.sup.18F] fluorinated species for use as imaging agents. The present invention further contemplates kits for making [.sup.18F] fluoride complexes suitable for performing radio-labeling reactions to generate [.sup.18F] fluorinated species. The present invention further contemplates a method of using [.sup.18F] fluoride prosthetic group for targeted tissue and disease imaging.