A61K49/085

Manganese-based chelate conjugates for molecular MR imaging

Provided herein are examples of metal chelating ligands that have high affinity for manganese. The resultant metal complexes can be used as MRI contrast agents, and can be functionalized with moieties that bind to or cause relaxivity change in the presence of biochemical targets.

TARGETED CONTRAST AGENTS FOR MRI OF ALPHA-SYNUCLEIN DEPOSITION

A liposomal composition (“ADx-003”) is provided, ADx-003 comprising a first phospholipid; a sterically bulky excipient that is capable of stabilizing the liposomal composition; a second phospholipid that is derivatized with a first polymer; a macrocyclic gadolinium-based imaging agent; and a third phospholipid that is derivatized with a second polymer, the second polymer being conjugated to a targeting ligand, the targeting ligand being represented by Formula I:

##STR00001##

wherein X is —CH.sub.2—, —CH.sub.2—CH.sub.2—, —CHO—, or —O—CO—; Y is —CH—CH═CH— or

##STR00002##

A and B are independently selected from C and N; R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently selected from —H, halogen, —OH, and —CH.sub.3; and R.sub.5, R.sub.6, and R.sub.7 are independently selected from —H, halogen, —OH, —OCH.sub.3, —NO.sub.2, —N(CH.sub.3).sub.2, C.sub.1-C.sub.6 alkyl, or a substituted or unsubstituted C.sub.4-C.sub.6 aryl group, except that when A and/or B is N the adjacent R.sub.5 and/or R.sub.7 is —H, or a pharmaceutically acceptable salt thereof.

BIOCOMPATIBLE MAGNETIC MATERIALS

A biocompatible magnetic material containing an iron oxide nanoparticle and one or more biocompatible polymers, each having formula (I) below, covalently bonded to the iron oxide nanoparticle:

##STR00001##

in which each of variables R, L, x, and y is defined herein, the biocompatible magnetic material contains 4-15% Fe(II) ions relative to the total iron ions. Also disclosed in a method of preparing the biocompatible magnetic material.

Macrocyclic Agents for Targeted Dual-Modality PET and MRI Imaging of Cancer
20220105207 · 2022-04-07 ·

Dual-modality contrast agents are disclosed herein, having the general formula:

##STR00001##

R.sub.1 includes a chelating moiety that is chelated to a Mn.sup.2+ isotope. The disclosed contrast agents differentially target a wide range of malignant tumor tissues, and can be simultaneously used as contrast agents for both magnetic resonance imaging (MRI) and positron emission topography (PET) imaging. Accordingly, the disclosed contrast agent can be used in diagnosing and monitoring solid tumor cancers.

GRAPHENE QUANTUM DOTS-GADOLINIUM ION CHELATE AS MAGNETIC RESONANCE IMAGING CONTRAST AGENT AND PREPARATION METHOD THEREOF
20220072161 · 2022-03-10 · ·

A graphene quantum dots-gadolinium ion chelate (Gd@GQDs) nanomaterial with hydrophilic groups on the surface has a preparation method that includes: preparing graphene oxide by using a Hummers method; subsequently, subjecting the graphene oxide to heating, oxidation, and purification to obtain pure graphene quantum dots; and finally, chelating the graphene quantum dots with Gd.sup.3+ to form stable Gd@GQDs. The Gd@GQDs is easily dispersed in water, phosphate buffered solution (PBS), biological medium and other aqueous system, has good biocompatibility and low cytotoxicity, shows an excellent T.sub.1-weighted contrast performance in a 1.5-Tesla magnetic resonance testing system, and has a relaxation rate r.sub.1 as high as 72 mM.sup.−1s.sup.−1, the value of r.sub.1 being 20 times higher than that of the current commercial T.sub.1-weighted magnetic resonance imaging contrast agent Gd-DTPA.

PEPTIDES AND COMPOSITIONS FOR TARGETED TREATMENT AND IMAGING
20210322508 · 2021-10-21 ·

The invention disclosed herein provides compositions and methods of treating cancer and other diseases related to activated immune cells using modulators of the TREM-1/DAP-12 signaling pathway. The compositions, including peptides and peptide variants, modulate TREM-1-mediated immunological response as standalone and combination-therapy treatment regimen. Further, methods are provided for predicting the efficacy of TREM-1 modulatory therapies in patients. In one embodiment, the present invention relates to targeted treatment, prevention and/or detection of cancer including but not limited to lung cancer including non-small cell lung cancer, pancreatic cancer, giant cell tumor of the tendon sheath, tenosynovial giant cell tumor, pigmented villonodular synovitis, cancer cachexia, etc., and other cancers associated with myeloid cell activation and recruitment. Additionally, the present invention relates to the targeted treatment, prevention and/or detection of scleroderma including but not limited to calcinosis, Raynaud's phenomenon, esophageal dysmotility, scleroderma, or telangiectasia syndrome (CREST). The invention further relates to personalized medical treatments.

RADIOLABELED LIGANDS FOR TARGETED PET/SPECT IMAGING AND METHODS OF THEIR USE

The present disclosure provides compounds, complexes, compositions, and methods for the detection of cancer. Specifically, the compounds, complexes, compositions of the present technology include pH (low) insertion peptides. Also disclosed herein are methods of using the complexes and compositions of the present technology in diagnostic imaging to detect cancer in a subject.

DETECTION OF HIGH-RISK UNSTABLE ATHEROSCLEROTIC PLAQUE
20210298611 · 2021-09-30 ·

The technology relates to a method for detecting high-risk unstable atherosclerotic plaque in a subject, the method comprising: a) administering to the subject a magnetic resonance imaging (MRI) contrast agent capable of being activated by myeloperoxidase (MPO) in atherosclerotic plaque; b) allowing the contrast agent to be activated by myeloperoxidase in atherosclerotic plaque; c) obtaining an image of the atherosclerotic plaque from the subject using such molecular MRI, wherein enhanced imaging is indicative of unstable plaque. In some embodiments an MPO inhibitor is administered to a subject identified as having a high-risk unstable atherosclerotic plaque.

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.

CYCLODEXTRIN-LINKED POLYVALENT LIGANDS FOR COMPLEXATION OF METAL IONS

Compounds are described which include polyvalent ligands linked to a cyclodextrin scaffold which exhibit strong binding affinities for lanthanides and favorable characteristics with respect to altering the relaxation time of coordinated water molecules. The compounds are useful as contrast agents in applications such as magnetic resonance imaging. The polyvalent ligands are also useful in applications requiring chelation of metal ions in other applications such as water treatment, sequestration of metal ions and treatment of diseases or conditions caused by exposure to toxic or radioactive metal ions.