A61K49/085

Highly Efficient Myeloperoxidase Activatable Imaging Agents
20230124429 · 2023-04-20 ·

Provided herein are compounds useful as imaging agents. Exemplary compounds provided herein are useful as myeloperoxidase imaging agents using magnetic resonance or nuclear imaging techniques. Methods for preparing the compounds provided herein and diagnostic methods using the compounds are also provided.

Method of synthesizing .SUP.18.F radiolabeled biomolecular agents

A method for preparing .sup.18F radiolabeled biomolecules and agents for .sup.18F-PET imaging is disclosed herein. A perfluoroaryl-conjugated target tracer is synthesized and purified with temperature and solvent conditions that are mild for the tracer molecule. The purified perfluoroaryl-conjugated target tracer is then labeled with .sup.18F using .sup.18F salts within a short reaction time, and with temperature and solvent conditions that are mild for the tracer molecule. The method provides a quick and convenient process that maintains the biological activities of the target molecules. The radio-labeled biomolecules may be used as contrast agents for Positron Emission Tomography (PET).

HYPOXIA-TARGETING CONTRAST AGENT AND METHODS OF USE THEREOF

The present disclosure provides for a novel hypoxia-targeting contrast agent for noninvasive detection of hypoxia using magnetic resonance imaging. Also disclosed is a process of preparing the novel hypoxia-targeting contrast agent, as well as methods of using the novel hypoxia-targeting contrast agent.

TEXAPHYRIN-PT(IV) CONJUGATES AND COMPOSITIONS FOR USE IN OVERCOMING PLATINUM RESISTANCE

The present disclosure relates platinum(IV) and texaphyrin linked conjugates and compositions comprising a texaphyrin and a platinum(IV) agent. The present disclosure also provides pharmaceutical compositions of the conjugates and compositions. Also, provided herein are methods of using the instant compounds in the treatment of cancer such as a platinum resistant cancer.

Long-lived gadolinium based tumor targeted imaging and therapy agents

Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula: ##STR00001##
or a salt therof. R.sub.1 includes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is —H, —OH, —COOH, —COOX, —OCOX, or —OX, wherein X is an alkyl or an arylalkyl; R.sub.2 is —N.sup.+H.sub.3, —N.sup.+H.sub.2Z, —N.sup.+HZ.sub.2, or —N.sup.+Z.sub.3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.

SEQUENTIAL TARGETING IN CROSSLINKING NANO-THERANOSTICS FOR TREATING BRAIN TUMORS
20230076792 · 2023-03-09 ·

The present invention provides a compound of Formula (I) as defined herein. The present invention also provides a nanoparticle comprising a plurality of the conjugates of the present invention, and methods of using the nanoparticles for drug delivery, treating a disease, and methods of imaging.

MULTIFUNCTIONAL COMPOUNDS FOR USE IN MEDICAL IMAGING AND THERAPY
20230149569 · 2023-05-18 ·

The disclosure provides multifunctional compounds for use in medical imaging and therapy, the compounds comprising two or more of (i) a chelating ligand moiety (CL); (ii) an optical probe moiety (OP); and (iii) a biological targeting moiety (BT). The disclosure further provides related compositions and methods.

Homing agents

The present disclosure provides peptide constructs for diagnostic imaging and therapeutic applications, using pegylated peptides which exhibit specific binding for a target molecule of interest, such as a biomarker of a disease or disorder.

Immunologically Active Peptide-Biliverdin Conjugate, Preparation Method Therefor and Application Thereof

The present disclosure relates to an immunologically active peptide-biliverdin conjugate (I), a preparation method therefor and an application thereof in cancer diagnosis, and/or tumor immunotherapy, and/or tumor “photothermal immunotherapy” (tumor photothermal therapy combined with immunotherapy). The conjugate to which the present disclosure relates not only may stimulate an organism to generate a tumor-immune effect, but also may relieve and/or eliminate tumor inflammation, remodel a tumor inflammatory microenvironment and achieve photothermal cancer immunodiagnosis and immunotherapy. The conjugate to which the present disclosure relates has high biocompatibility, good stability and an extended half-life. The conjugate is prepared from an immunologically active peptide and biliverdin by means of chemical synthesis. A peptide end of the conjugate exercises the function of immunoregulation, and a pigment end thereof exercises functions such as tumor imaging diagnosis, tumor photo-thermal ablation, immune inflammatory microenvironment regulation and the like. The conjugate may significantly enhance the antitumor effect and effectively inhibit tumor metastasis and recurrence.

TARGETED CONTRAST AGENTS COMPRISING A HYDRAZIDE FUNCTIONAL GROUP
20170340757 · 2017-11-30 ·

Described herein is a contrast agent for administration to a subject. The contrast agent includes a targeting portion that includes a hydrazide functional group; a metal ion bound to a metal-complexable portion; and a linker joining the targeting portion and the metal-complexable portion of the contrast agent. The portion that is not bound to a metal ion localizes the contrast agent to necrotic tissue in the subject.