A61K51/0446

Boron-based dual imaging probes, compositions and methods for rapid aqueous F-18 labeling, and imaging methods using same

A composition useful as a PET and/or fluorescence imaging probe a compound a compound of Formula I, including salts, hydrates and solvates thereof: ##STR00001## wherein R.sub.1-R.sub.7 may be independently selected from hydrogen, halogen, hydroxy, alkoxy, nitro, substituted and unsubstituted amino, cycloalkyl, carboxy, carboxylic acids and esters thereof, cyano, haloalkyl, aryl, X is selected from the group consisting of C and N; and A is selected of hydrogen, halogen, hydroxy, alkoxy, nitro, substituted and unsubstituted amino, alkyl, cycloalkyl, carboxy, carboxylic acids and esters thereof, cyano, haloalkyl, aryl, including phenyl and aminophenyl, and heteroaryl.

NSAID-DERIVED CONJUGATE COMPOUNDS FOR IMAGING
20240358866 · 2024-10-31 ·

Compounds derived from celecoxib, valdecoxib, and indomethacin, and methods of use thereof, are disclosed. The compounds are useful for, inter alia, identifying and localizing the site of pathology and/or inflammation responsible for the sensation of pain in a patient; for identifying the sites of primary, secondary, benign, or malignant tumors; and for diagnosing infection or confirming or ruling out suspected infection. The compounds contain a radioactive agent which permits imaging. The compounds concentrate at sites of increased cyclooxygenase expression, such as areas of increased COX-2 expression, thus revealing the sites of increased prostaglandin production, which is correlated with pain and inflammation, and correlated with tumor presence and/or location. Identifying areas of increased COX expressing can also aid in screening for infections, assessing efficacy of diagnosis and treatment of rheumatoid arthritis, and assessing the need for treatment with opioid drugs.

Carbazole compounds for in vivo imaging

The present invention concerns in vivo imaging and in particular in vivo imaging of translocator protein (TSPO, formerly known as the peripheral benzodiazepine receptor). An indole-based in vivo imaging agent is provided that overcomes problems relating to known TSPO-binding radiotracers. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said precursor compound. Other aspects of the invention include a method for the synthesis of the in vivo imaging agent of the invention comprising use of the precursor compound of the invention, a kit for carrying out said method, and a cassette for carrying out an automated version of said method. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.

4,4-DISUBSTITUTED CYCLOHEXYL BRIDGED HEPTAMETHINE CYANINE DYES AND USES THEREOF
20240393330 · 2024-11-28 ·

The invention relates to a family of compounds that comprise fluorescent cyanine dyes. The compounds are near infrared absorbing heptamethine cyanine dyes with a 4,4-disubstituted cyclohexyl ring as part of the polymethine chromophore. The compounds are generally hydrophilic and can be chemically linked to biomolecules, such as proteins, nucleic acids, and therapeutic small molecules. The compounds can be used for imaging in a variety of medical, biological and diagnostic applications.

HETEROBIVALENT AND HOMOBIVALENT AGENTS TARGETING FIBROBLAST ACTIVATION PROTEIN ALPHA AND/OR PROSTATE-SPECIFIC MEMBRANE ANTIGEN

Imaging and radiotherapeutic agents targeting fibroblast-activation protein-? (FAP-?) and/or prostate-specific membrane antigen (PSMA) and their use in imaging and treating FAP-? and/or PSMA-related diseases and disorders are disclosed.

RADIOFLUORINATED AGENTS FOR PET IMAGING SELECTIVELY TARGETING FIBROBLAST ACTIVATION PROTEIN
20240366807 · 2024-11-07 ·

Disclosed are compounds useful for imaging cells that overexpress FAP, and for treating cancer. Also disclosed are methods of making said compounds.

4,4-disubstituted cyclohexyl bridged heptamethine cyanine dyes and uses thereof
09897604 · 2018-02-20 · ·

The invention relates to a family of compounds that comprise fluorescent cyanine dyes. The compounds are near infrared absorbing heptamethine cyanine dyes with a 4,4-disubstituted cyclohexyl ring as part of the polymethine chromophore. The compounds are generally hydrophilic and can be chemically linked to biomolecules, such as proteins, nucleic acids, and therapeutic small molecules. The compounds can be used for imaging in a variety of medical, biological and diagnostic applications.

Metal oxide catalyzed radiofluorination

Inter alia, the first titania-catalyzed [.sup.18F]-radiofluorination in highly aqueous medium is provided. In embodiments, the method utilizes titanium dioxide, 1:1 acetonitrile-thexyl alcohol solvent mixture and tetrabutylammonium bicarbonate as a base. Radiolabeling may be directly performed with aqueous [.sup.18F]fluoride without the need for drying/azeotroping step, which reduces radiosynthesis time while keeping high fluoride conversion. The general applicability of the synthetic strategy to the synthesis of the wide range of PET probes from tosylated precursors is demonstrated.

PHARMACEUTICAL COMPOSITION CONTAINING TAGGED SITE-ANTIHUMAN ANTIBODY FAB FRAGMENT COMPLEX
20250009897 · 2025-01-09 ·

Provided is a stable pharmaceutical composition comprising a labeling moiety-anti-human antibody Fab fragment conjugate, and the like. In the pharmaceutical composition comprising a labeling moiety-anti-human antibody Fab fragment conjugate, citric acid, phosphoric acid, 2-[4-(2-hydroxyethyl)-1-piperazinyl]ethanesulfonic acid or trishydroxymethyl aminomethane is added as a buffering agent, sucrose or glycerin is added as a stabilizer, a nonionic surfactant is added, and the pH is adjusted to 6.5 to 7.5. This enables suppression of generation of multimers and insoluble subvisible particles during preservation of the labeling moiety-anti-human antibody Fab fragment conjugate.

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.