A61K51/0453

Radiopharmaceutical synthesis methods

The invention relates to products and methods that provide increased yields of certain radiopharmaceuticals.

NRF AND HIF ACTIVATORS/HDAC INHIBITORS AND THERAPEUTIC METHODS USING THE SAME
20200039933 · 2020-02-06 ·

Compounds that inhibit histone (HDACI) and/or activate Nrf2 and HIF, and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC and/or activation of Nrf2 and HIF provide a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.

Control of chronic neuropathic pain and allodynia
10548994 · 2020-02-04 · ·

In one embodiment, the invention provides a method of treating a subject suffering from chronic neuropathic pain and/or allodynia by administering a therapeutically-effective amount of at least one LFA1 antagonist to the subject. In a preferred embodiment, the invention provides a method of treating a subject suffering from chronic neuropathic pain and/or allodynia, the method comprising administering intrathecally to the subject a therapeutically-effective amount of microparticles comprising PLGA-encapsulated pDNA-IL-10, optionally in combination with a therapeutically-effective amount of intrathecally-administered CpG oligodeoxynucleotide (CpG ODN) and/or at least one LFA1 antagonist.

METHOD FOR LABELING RADIOISOTOPE RADIOLABELING COMPOUND AND KIT COMPRISING THE SAME FOR LABELING RADIOISOTOPE

The present disclosure relates to a method for labeling a radioisotope, a radiolabeling compound, a kit including the same, and a method for labeling a radioisotope, including: providing a diaminophenyl compound represented by Chemical Formula I below and including a biomolecule, a fluorescent dye or a nanoparticle compound bound thereto; and reacting the diaminophenyl compound and a radioisotope-labeled aldehyde compound represented by Chemical Formula II below at room temperature; and a related technology:

##STR00001## in Chemical Formula I, A is CH.sub.2 or O; a is 0 or an integer of 1 to 10; X is CH.sub.2 or CONH; Y is CH.sub.2 or

##STR00002##

and Z is the biomolecule, the fluorescent dye or the nanoparticle compound,

##STR00003## in Chemical Formula II, b is 0 or an integer of 1 to 10; and L is CH.sub.2 or CONH; and Q is or

##STR00004## M, M and M in Q are radioisotopes.

Radiotracer Derivatives Of Trimethoprim For Diagnostic Imaging
20190381197 · 2019-12-19 ·

The present invention provides radiolabeled trimethoprim which are useful in imaging tests such as PET scans. The compounds show robust bacterial uptake in vitro and identify infections from inflammation or tumor when administered to a subject. The compounds show rapid and sensitive detection of Ec DHFR containing tumors from control tumors and background tissue. In one aspect, a compound having the structure of formula (I) is provided or a pharmaceutically acceptable salt or prodrug thereof, wherein R is defined herein. Also provided are compositions containing these compounds, positron emission tomography reporter probe comprising these compounds, and methods of imaging a bacterial infection, tracking or monitoring bacteria, distinguishing a bacterial infection from inflammation or tumor, monitoring genetically fused protein expression, and monitoring genetically engineered cells in clinical scenarios such as immunotherapy for cancer treatment.

##STR00001##

CLEARING AGENT
20190382435 · 2019-12-19 · ·

It is an object of the present invention to provide a clearing agent, by which after a fusion of the streptavidin mutant and a molecular probe has been administered, the fusion, which is not localized in a target site such as an affected site but remains in the body, can be promptly removed (cleared) from the body. The present invention provides a compound represented by the following formula (1) or a salt thereof:

##STR00001##

wherein X1a, X1b, X2a and X2b each independently represent O or NH; Y.sup.1 and Y.sup.2 each independently represent C or S; Z.sup.1 and Z.sup.2 each independently represent O, S or NH; V.sup.1 and V.sup.2 each independently represent S or S.sup.+O.sup.; n1 and n2 each independently represent an integer of 0 or 1; L10 and L12 each independently represent a divalent linking group; L11 represents a trivalent linking group; L14 represents a divalent linking group; and Sugar represents a sugar residue.

IN VIVO STABLE HG-197(M) COMPOUNDS, METHOD FOR THE PRODUCTION THEREOF AND USE THEREOF IN NUCLEAR MEDICAL DIAGNOSTICS AND ENDORADIONUCLIDE THERAPY (THERANOSTICS)

The present invention relates to in vivo stable .sup.197(m)Hg compounds according to formula (I) for use in nuclear medical diagnostics and endoradionuclide therapy (theranostics), particularly the treatment of cancer, a method for the production of the .sup.197(m)Hg compounds comprising the step of radiolabeling of organic precursor compounds with NCA .sup.197(m)Hg by electrophilic substitution; and the use of the .sup.197(m)Hg compounds for nuclear medical diagnostics and endoradionuclide therapy (theranostics), particularly the treatment of cancer.

Method for producing [18F]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.

Method for removing acetaldehyde

A method for removing or controlling or quantifying the presence of aldehydes, in particular acetaldehyde, is described. Such a method is useful in prolonging the shelf life of a pharmaceutical product.

11C -LABELED O6 -BENZYLGUANINE, PET PROBE CAPABLE OF VISUALIZING O6 -METHYL GUANINE METHYL-TRANSFERASE ACTIVITY, AND PRODUCTION METHOD OF THE SAME

An object of the invention is to provide a .sup.11C-labeled O.sup.6-benzylguanine capable of obtaining a PET image and a process for producing the same.

The .sup.11C-labeled O.sup.6-benzylguanine of the invention is represented by the following chemical formula (a).

##STR00001##

The .sup.11C-labeled O.sup.6-benzylguanine is produced by: a coupling step of cross-coupling a methyl iodide labeled with .sup.11C and the following organotin compound (b) (R.sup.1 represents an alkyl group, and R.sup.2 and R.sup.3 represent a leaving group which can be eliminated with a base.) in the presence of a palladium complex, a phosphine ligand, and cuprous halide in an aprotic lactam; and a desorption step of desorbing the leaving groups R.sup.2 and R.sup.3 of the coupling product obtained by the coupling step with a base.

##STR00002##