A61K49/085

METHOD OF SYNTHESIZING 18F RADIOLABELED BIOMOLECULAR AGENTS
20230310663 · 2023-10-05 ·

Methods of preparing .sup.18F targeting biomolecules and small molecules with biological activity for therapeutic and/or diagnostic applications using fluorinated aromatic compounds. A fluorinated conjugated target tracer is synthesized and purified with temperature and solvent conditions that are mild for the tracer molecule. The purified fluorinated-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).

RECOMBINANT CHIMERIC PROTEIN FOR SELECTINS TARGETING

The invention discloses a recombinant protein (P-selectin glycoprotein ligand-1 and Neural Retina-specific Leucine Zipper) PSGL-1-NRL chimeric protein comprising a Selectin Binding domain and a non-covalent dimerization domain, which is a leucine zipper and is more preferably the leucine zipper domain of the human or mouse Neural Retina-specific Leucine Zipper. The chimeric protein further comprises a covalent dimerization domain with at least one cysteine suitable to form a disulfide bridge with another chimeric protein to form a homodimer.

In the chimeric protein, the PSGL-1 domain corresponds to the extracellular region of Human PSGL-1 and is more preferably the selectin binding region of the mature protein.

The chimeric protein is correctly post-translationally modified and is efficiently expressed in a mammalian system. It is sulfated, O-linked glycosylated and sialylated and binds P, E and L selectin, allowing in vivo and in vitro targeting for diagnostic or therapeutic purposes.

NANOBODY BASED IMAGING AND TARGETING OF ECM IN DISEASE AND DEVELOPMENT

Methods for developing disease-related nanobodies and related products and kits are provided. The disease-specific proteins are extracellular matrix (ECM) proteins, domains or epitopes that are associated with various aspects of disease and are not present, or are present in very low quantities, in non-diseased individuals. Highly effective nanobodies capable of specifically binding to these ECM protein epitopes useful in in vivo imaging assays, the detection, diagnosis and treatment of diseases as well as monitoring therapeutic progress in a patient with a disease are provided herein.

COMPOUNDS FOR USE AS IRON(III) MRI CONTRAST AGENTS
20220259244 · 2022-08-18 ·

Provided are macrocyclic compounds and compounds with two or more macrocyclic groups, iron coordinated macrocyclic compounds, and iron coordinated compounds with two or more macrocyclic groups. The iron is high-spin iron(III). The iron coordinated compounds may exhibit a negative redox potential (e.g., relative to a normal hydrogen electrode at a biologically relevant pH, for example, a pH of 6.5-7.5). The compounds can be used as MRI contrast agents.

Polyrotaxanes bearing mixed cyclodextrin species and uses thereof

Various embodiments of the present invention are directed to polyrotaxanes comprising a poloxamer core and at least one cyclodextrin and methods for treating Niemann-Pick type C (NPC) and imaging (e.g., MRI) using the polyrotaxanes of the various embodiments of the present invention.

INTERCELLULAR ADHESION MOLECULE 1 (ICAM1) ANTIBODY DRUG CONJUGATE AND USES THEREOF

The disclosure provides compositions comprising intercellular adhesion molecule 1 (ICAM1) antibody and methods for using the same for therapeutic applications, for example, treating pancreatic cancer and predicting drug response.

Molecular probes for imaging of myelin

A molecular probe for labeling myelin includes a fluorescent trans-stilbene derivative.

COATED PLANT VIRUS IMAGING AGENTS
20220211881 · 2022-07-07 ·

An imaging nanoparticle comprising a plant virus particle having an interior surface and an exterior surface, an imaging agent that is linked to the interior and/or exterior surface, and a layer of biocompatible mineral such as silica coated over the exterior surface, is described. The imaging nanoparticle can be used in method of generating an image of a tissue region of a subject, by administering to the subject a diagnostically effective amount of an imaging nanoparticle and generating an image of the tissue region of the subject to which the imaging nanoparticle has been distributed.

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.

CYCLEN BASED COMPOUNDS, COORDINATION COMPOUNDS, PEPTIDES, PHARMACEUTICAL PREPARATION, AND USE THEREOF

Cyclen based compounds of general formula (I) are disclosed. X is nitrogen and Y, Z are —CH—, or X, Z are —CH— and Y is nitrogen, or X, Y are —CH— and Z is nitrogen. R.sup.1 is independently selected from H; COOH; benzyloxycarbonyl; fluorenylmethyloxycarbonyl; tert-butoxycarbonyl; methylcarbonyl; trifluoromethylcarbonyl; benzyl; triphenylmethyl; tosyl; mesyl; benzyloxymethyl; phenylsulfonyl; ethoxycarbonyl; 2,2,2-trichloroethyloxycarbonyl; methoxycarbonyl; methoxymethyloxycarbonyl; R.sup.2 is selected from H; methylcarbonyl; tert-butyldimethylsilyl; (C1-C4)alkyl; R.sub.3 is independently selected from H; (C1-C6)alkyl.