A61K49/08

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.

EQUILIBRIUM ADSORPTION METHOD FOR MAKING A SILICA NANOCARRIER SPION COMPOSITION

Silica nanocarriers hybridized with superparamagnetic iron oxide nanoparticles (“SPIONs”) and curcumin through equilibrium or enforced adsorption technique. Methods for dual delivery of SPIONs and curcumin to a target for diagnosis or therapy, for example, for SPION-based magnetic resonance imaging or for targeted delivery of curcumin to a cell or tissue. The technique can be extend to co-precipitation of mixed metal oxide involving Ni, Mn, Co and Cu oxide. The calcination temperature can be varied from 500-900° C. The nanocombination is functionalized with chitosan, polyacrylic acid, PLGA or another agent to increase its biocompatibility in vivo.

EQUILIBRIUM ADSORPTION METHOD FOR MAKING A SILICA NANOCARRIER SPION COMPOSITION

Silica nanocarriers hybridized with superparamagnetic iron oxide nanoparticles (“SPIONs”) and curcumin through equilibrium or enforced adsorption technique. Methods for dual delivery of SPIONs and curcumin to a target for diagnosis or therapy, for example, for SPION-based magnetic resonance imaging or for targeted delivery of curcumin to a cell or tissue. The technique can be extend to co-precipitation of mixed metal oxide involving Ni, Mn, Co and Cu oxide. The calcination temperature can be varied from 500-900° C. The nanocombination is functionalized with chitosan, polyacrylic acid, PLGA or another agent to increase its biocompatibility in vivo.

NANOSILICA CARRIER WITH SPIONS AND A CURCUMINOID

Silica nanocarriers hybridized with superparamagnetic iron oxide nanoparticles (“SPIONs”) and curcumin through equilibrium or enforced adsorption technique. Methods for dual delivery of SPIONs and curcumin to a target for diagnosis or therapy, for example, for SPION-based magnetic resonance imaging or for targeted delivery of curcumin to a cell or tissue. The technique can be extend to co-precipitation of mixed metal oxide involving Ni, Mn, Co and Cu oxide. The calcination temperature can be varied from 500-900° C. The nanocombination is functionalized with chitosan, polyacrylic acid, PLGA or another agent to increase its biocompatibility in vivo.

NANOSILICA CARRIER WITH SPIONS AND A CURCUMINOID

Silica nanocarriers hybridized with superparamagnetic iron oxide nanoparticles (“SPIONs”) and curcumin through equilibrium or enforced adsorption technique. Methods for dual delivery of SPIONs and curcumin to a target for diagnosis or therapy, for example, for SPION-based magnetic resonance imaging or for targeted delivery of curcumin to a cell or tissue. The technique can be extend to co-precipitation of mixed metal oxide involving Ni, Mn, Co and Cu oxide. The calcination temperature can be varied from 500-900° C. The nanocombination is functionalized with chitosan, polyacrylic acid, PLGA or another agent to increase its biocompatibility in vivo.

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.

Nitrogen-containing macrocyclic conjugates as radiopharmaceuticals

The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.