A61K51/0455

MACROCYCLIC COMPLEXES OF ALPHA-EMITTING RADIONUCLIDES AND THEIR USE IN TARGETED RADIOTHERAPY OF CANCER

The present technology provides compounds as well as compositions including such compounds useful in targeted radiotherapy of cancer and/or mammalian tissue overexpressing prostate specific membrane antigen (PSMA) where the compounds are represented by the following:

##STR00001## or a pharmaceutically acceptable salt thereof,

##STR00002## or a pharmaceutically acceptable salt thereof,

##STR00003## or a pharmaceutically acceptable salt thereof,
wherein M.sup.1 is independently at each occurrence an alpha-emitting radionuclide. Equivalents of such compounds are also disclosed.

LIGAND COMPOUND OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR AND APPLICATION THEREOF

Provided is a ligand compound of 7 nicotinic acetylcholine receptor, which can be represented by any one of the following general formulas, wherein (1) represents a halogen. The ligand compound is an improved ligand compound of 7 nicotinic acetylcholine receptor. The ligand compound can be used as a PET imaging agent after being radio-chemically marked.

System, device and method for preparing tracers and transferring materials during radiosynthesis

A system, apparatus, and method for transferring chemical solutions and synthesizing a tracer. For transferring chemical solutions, the system comprises a primary container; a secondary container; a first line in communication with the primary container and the secondary container. The first line facilitates the flow of gas and/or liquid between the primary container and the secondary container. A valve located upstream of the secondary container and downstream of the primary container regulates flow within the first line; a second line in communication with the secondary container. For synthesizing a tracer, the system includes a source of a solution having a radionuclide. A first container has a tracer precursor and is in communication with the source of solution.

Azacyanine dyes and use thereof

The application provides fluorescent dyes, which are cyanine dyes that incorporate additional aza moieties in the indolenium heterocycles and/or in the methine chains connecting them. Symmetrical and unsymmetrical chemically reactive azacyanine dyes are described for conjugation, as well as their bioconjugates for in-vitro and in-vivo assays and fluorescence imaging.

METHOD FOR PRODUCING RADIOHALOGEN-LABELED COMPOUND AND METHOD FOR PRODUCING RADIOPHARMACEUTICAL

Provided is a method for producing a radiohalogen-labeled compound, the method comprises: a step in which a radiohalogen-labeling precursor compound (S-L) having a leaving group (L) capable of being nucleophilically substituted by a radioactive halide ion (X.sup.) is subjected to a radiohalogenation reaction to obtain a reaction mixture RM1 which contains the radiohalogen-labeling precursor compound (S-L) and a reaction product (SX) resulting from the radiohalogenation reaction; a step in which the reaction mixture RM1 is mixed with a polyvalent acid or a salt thereof to obtain a reaction mixture RM2; and a step in which the reaction product (SX) is purified from the reaction mixture RM2 by a solid phase extraction method.

TARGETED, METAL-CATALYZED FLUORINATION OF COMPLEX COMPOUNDS WITH FLUORIDE ION VIA DECARBOXYLATION

Methods of preparing fluorinated compounds by carboxylative fluorination using fluoride are contained herein. Fluorinated compounds are provided. Methods of using fluorinated compounds are contained herein.

PROBES FOR IMAGING HUNTINGTIN PROTEIN

Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.

##STR00001##

COMPOSITION FOR CROSS TALK BETWEEN ESTROGEN RECEPTORS AND CANNABIONOID RECEPTORS

A composition for cross talk between estrogen receptors and cannabinoid receptors including a chelator and a receptor ligand is provided. A method of synthesizing the composition is also provided, and the composition may be further prepared in pharmaceutical formulations or kits for therapy or molecular imaging.

Radiopharmaceutical synthesis methods

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

Anthranilic acid derivatives
10561748 · 2020-02-18 ·

The present invention is directed to a novel compound of Formula 1 wherein the radiolabeled compound of Formula 1 is capable of being used as a radiotracer in PET imaging of a targeted localized tissue and targeted radionuclide therapy of one or more conditions that may be regulated or normalized via inhibition of transporter such as Pgp, BCRP or MRP I. The novel compounds of Formula 1 can also be used as substrates for binding with one or more ABC transporters. In particular, the present invention aids in diagnosis and therapeutic treatment of MDR disorders in all forms of cancers and neurological disorders of the central nervous system. The present invention further provides methods of preparation of compounds of Formula 1 and novel intermediates used in the preparation of compounds of Formula 1.