A61K49/124

Delivery system in micellar form having modular spectral response based on enzyme-responsive amphiphilic PEG-dendron hybrid polymers

The present invention relates to new molecular design that allows micelles to report their activation and disassembly by an enzymatic trigger. The molecular design is based on introduction of a labeling moiety selected from a fluorescent dye, a dark quencher, combinations of dyes or dyes/quenchers, and a fluorinated moiety (a .sup.19F-magenetic resonance (MR) probe for turn ON/OFF of a .sup.19F-MR signal) through covalent binding to the focal point of amphiphilic polymer-dendron hybrids with the labeling moiety. At the assembled micellar state, the dyes are closely packed and hence the probability for intermolecular interactions increases significantly, leading to alteration of the fluorescent properties (signal quench or shift) or the .sup.19F-MR signal (OFF state) of the micelles. Upon enzymatic cleavage of the hydrophobic end-groups from enzyme-responsive dendron, the polymers become hydrophilic and disassemble. This structural change is then translated into a spectral change as dye-dye interactions are halted and the dyes regain their intrinsic fluorescent properties, or alternatively by turn ON the .sup.19F-MR signal. The high modularity of the design allows the introduction of various types of dyes and thus enables rational adjustment of the spectral response. Two major types of responses are described: Turn-On/Off and spectral shift, depending on the type of labeling dye. The present invention further provides methods of use of the hybrid delivery system and to a kit comprising the same.

SALICYLIC ACID-BASED POLYMERIC CEST CONTRAST AGENTS TARGETING PROSTATE-SPECIFIC MEMBRANE ANTIGEN AND USES THEREOF

Salicylic acid-based polymeric CEST contrast agents targeting prostate-specific membrane antigen, pharmaceutical composition comprising the same and methods of use thereof are disclosed.

HIGH RELAXIVITY GADOLINIUM CHELATE COMPOUNDS FOR USE IN MAGNETIC RESONANCE IMAGING

The present invention relates to a new class of high relaxivity extracellular gadolinium chelate complexes, to methods of preparing said compounds, and to the use of said compounds as MRI contrast agents.

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Salicylic acid-based polymeric CEST contrast agents targeting prostate-specific membrane antigen and uses thereof

Salicylic acid-based polymeric CEST contrast agents targeting prostate-specific membrane antigen, pharmaceutical composition comprising the same and methods of use thereof are disclosed.

BIODEGRADABLE DENDRITIC STRUCTURE, METHODS AND USES THEREOF

The present disclosure relates to biodegradable and biocompatible dendritic repeating unit/scaffold (bRU), to a method of: synthesis of biodegradable and biocompatible dendritic repeating unit/scaffold (bRU) and to the biomedical applications of biodegradable and biocompatible dendritic repeating unit/scaffold (bRU). This bRU is useful as scaffold to synthesize fully biodegradable dendrimers and/or mix or hybrid biodegradable dendrimers, presenting a biodegradable shell and a hydrolytically stable/non-degradable core of already existing dendritic systems, in particular it relates to a Biodegradable dendritic structure of formula (I)

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COMPOUNDS FOR USE AS IRON(III) MRI CONTRAST AGENTS
20200079806 · 2020-03-12 ·

Provided are macrocyclic compounds and compounds with two or more macrocyclic groups, iron coordinated macro-cyclic 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.

Formulation of contrast media and process of preparation thereof

The present disclosure relates to a liquid pharmaceutical formulation comprising a DOSA-derived tetra-chelate of formula (I), in which M is an ion of a paramagnetic metal, preferably a Gd.sup.3+ ion, and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined in the claims, in a pharmaceutical acceptable solvent. The present disclosure also relates to a method of preparation of said liquid pharmaceutical formulation and to a method of imaging involving said liquid pharmaceutical formulation.

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.

CEST SYSTEMS EXHIBITING A CONCENTRATION INDEPENDENT RESPONSIVENESS

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

CEST systems exhibiting a concentration independent responsiveness

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