A61K49/101

MANGANESE COMPLEXES WITH SUBSTITUTED BISPHOSPHONATES USEFUL AS IMAGING AND THERAPEUTIC AGENTS
20190111160 · 2019-04-18 ·

Provided herein is a compound useful as a magnetic resonance imaging (MRI) contrast agent and a therapeutic agent, said compound having a structure represented by: YXZ wherein, X is Mn(II), and Y and Z are each independently a bisphosphonate coupled to one or more therapeutic agents. Methods of use of the compound for MRI imaging and treatment for cancer or a microbial infection are also provided.

Composition Intended to Vectorise an Anti-Cancer Agent
20190099496 · 2019-04-04 ·

A composition in the form of a water-in-oil emulsion comprising: from 20% to 40% (v/v) of aqueous phase, in the form of droplets, comprising an anti-cancer agent and a densifying agent chosen from the complexes of nonionic macrocyclic chelate with a paramagnetic metal, from 60% to 80% (v/v) of lipid phase comprising an iodized oil and at least one surfactant of formula (I) in a proportion, by weight of surfactant relative to the total volume of the composition, of 0.3% to 5%, formula (I) of said surfactant being the following:

##STR00001##

in which: s is 0 or 1, m is an integer from 2 to 30, R.sub.1 represents a group of formula (II)

##STR00002## in which n is an integer from 4 to 10, o is an integer from 1 to 4, p is an integer from 3 to 7, q is an integer from 2 to 10, and r is 0 or 1, R.sub.2 represents a hydrogen atom or is identical to R.sub.1, and each R.sub.3 independently represents a hydrogen atom or is identical to R.sub.1.

Compositions and methods for imaging

The present disclosure provides compositions for in vivo imaging of hydrogen peroxide; and methods for detecting hydrogen peroxide in vivo. The compositions and methods find use in various diagnostic applications, which are also provided.

CEST systems exhibiting a concentration independent responsiveness

The present invention relates to the use of non-equivalent mobile protons belonging to NMR distinguishable stereoisomers of a CEST agent in a ratiometric based CEST imaging procedure and to Lanthanide (III) complex compounds displaying at least two NMR-distinguishable stereoisomers in solution useful as concentration independent CEST responsive agents.

MANGANESE-BASED CHELATE CONJUGATES FOR MOLECULAR MR IMAGING
20190001003 · 2019-01-03 ·

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.

MANGANESE-ENHANCED MAGNETIC RESONANCE IMAGING
20240277246 · 2024-08-22 ·

The present invention relates to manganese-enhanced MRI, more specifically to a method for determining a cardiomyocyte cellular manganese uptake rate of a subject, contrast agent comprising a manganese contrast agent, or a pharmaceutically acceptable salt thereof, for use in a method for in vivo diagnosis of heart disease in a subject, a computer-implemented method of determining a cardiomyocyte cellular manganese uptake rate in a subject, a data processing apparatus comprising means for carrying out said computer-implemented method, a computer program comprising instructions which, when the program is executed by a computer, cause the computer to carry out said computer-implemented method, and a computer-readable medium having stored thereon said computer program.

Combination Formulation

The present invention relates to in vivo imaging and in particular to magnetic resonance imaging (MRI). Provided by the present invention is a pharmaceutical formulation suitable for use in an MRI procedure and which offers advantages over known such formulations. A particular dose of the pharmaceutical formulation of the invention is also envisioned as well as the use of said dose in a method of in vivo imaging. This present invention provides for simultaneous administration of a liver specific agent and a second MR contrast agent that is capable of better/further enhancing the dynamic vascular phase in a patient. The method of the invention has the advantage of simplicity and patient comfort, compared to sequential injections. Furthermore, the method of the invention provides the advantage that it can enable a lower cumulative dose of contrast agents.

Lymph targeting nuclear magnetic contrast agent using brown algae polysaccharide as carrier and preparation method and use thereof

Disclosed is a lymph targeting nuclear magnetic contrast agent using a brown algae polysaccharide as a carrier, and a preparation method and a use thereof. A macromolecular contrast agent with good water solubility was prepared by using the brown algae polysaccharide as the carrier, using mannose or mannose derivatives as a mannose receptor (MBP) recognition group, and using a paramagnetic metal ion chelate as a nuclear magnetic resonance imaging group. The binding capacity of lymphoid tissue was improved. The mannose or mannose derivative group introduced into the synthesized contrast agent molecule achieves the goal of binding to the enriched mannose receptors in the lymphoid tissues. At the same time, after the contrast agent is injected subcutaneously, both lymph vessels and lymph nodes were clearly visualized under MRI scanning The intensification rate and enhancement time of the lymph node signal at one side of the animal body injected with the contrast agent was significantly enhanced, so as to achieve a clear mapping and precise positioning of the lymph nodes and the lymph vessels. It is of great significance for the detection and diagnosis of lymph system diseases.

Paramagnetic solid lipid nanoparticles (pSLNs) containing metal amphiphilic complexes for MRI

The present invention relates to paramagnetic solid lipid nanoparticles (pSLNs) comprising an amphiphilic paramagnetic metal chelating moiety selected from: a diazepine derivative of Formula I and a tetraazocyclododecane derivative of Formula (II): being said chelating moiety complexed to a paramagnetic metal ion selected from the group consisting of: Gd(III), Mn(II), Cr(III), Cu(II), Fe(III), Pr(III), Nd(III), Sm(III), Tb(III), Yb(III), Dy(III), Ho(III) and Er(III), or salts thereof. The invention further relates to the process for preparation of said solid lipid nanoparticles comprising amphiphilic complexes of paramagnetic metals (pSLNs) and to the use of pSLNs as MRI contrast agents in the diagnostic field.

Inflammation imaging and therapy

An imaging agent comprising a conjugate of an oligosaccharide moiety with an imaging moiety. The oligosaccharide is Lewis A or Lewis B or a mimetic thereof, or a pharmaceutically acceptable salt or PEGylated form of Lewis A or Lewis B or its mimetics. Lewis A and Lewis B and its mimetics are also provided for use in the therapeutic treatment of inflammatory diseases, autoimmune diseases and cancer.