C07F5/003

FIBROBLAST ACTIVATION PROTEIN LIGANDS FOR TARGETED DELIVERY APPLICATIONS

The present invention relates to ligands of Fibroblast Activation Protein (FAP) for the active delivery of various payloads (e.g. cytotoxic drugs, radionuclides, fluorophores, proteins and immunomodulators) at the site of disease. In particular, the present invention relates to the development of FAP ligands for targeting applications, in particular diagnostic methods and/or methods for therapy or surgery in relation to a disease or disorder, such as cancer, inflammation or another disease characterized by overexpression of FAP.

Targeted near-infrared imaging by metal-organic frameworks

Metal-organic frameworks (MOFs) comprising amines on the organic linker can be used for cell targeting. In particular, primary amine groups represent one of the most versatile chemical moieties for conjugation to biologically relevant molecules, including antibodies and enzymes. Different chemical conjugation schemes can be used to conjugate biological molecules to the amino functionality on the organic linker. For example, carbodiimide chemistry can be used to link a primary amine to available carboxyl groups on the protein. For example, sulfhydryl crosslinking chemistry can be used via Traut's reagent scheme. As a demonstration of the invention, the ability of EpCAM antibody-targeted MOFs to bind to a human epithelial cell line (A549), a common target for imaging studies, was confirmed with confocal microscopy.

GROUP III AND LANTHANIDE BIS-PHENYL-PHENOXY METAL-LIGAND COMPLEXES

Embodiments of this disclosure are directed to catalyst systems comprising a metal-ligand complex according to formula (I).

##STR00001##

ELECTRO-POLARIZABLE COMPLEX COMPOUND AND CAPACITOR
20170372842 · 2017-12-28 ·

The present disclosure provides an electro-polarizable complex compound having the following general formula:


[M.sup.4+(L).sub.m].sup.xK.sub.n,  (I)

where complexing agent M is a four-valence metal; ligand L comprises one or more heteroatomic fragments comprising one or more neutral or anionic metal-coordinating heteroatoms and one or more electrically resistive fragments, m represents the number of ligands; x represents the oxidative state of the metal-ligand complex; K is a counter-ion or zwitterionic polymers which provides an electro-neutrality of the complex compound, n represents the number of counter-ions. The metal-coordinating heteroatoms form a first coordination sphere, and the number of heteroatoms in this first coordination sphere does not exceed 12.

Process for polymerizing beta-butyrolactone

A catalyst/initiator system that can be used for polymerizing β-butyrolactone is described. The catalyst/initiator system includes a rare earth metal, a chiral ligand, at least one nucleophilic ligand, optionally at least one solvent ligand, and optionally an alkali based co-catalyst. The chiral ligand can have the structure of Formula A, as shown below: ##STR00001##
wherein Y represents rare earth metal Yttrium, Ph represents Phenyl radical and thf represents tetrahydrofuran solvent ligand.

FUNCTIONALIZED LINEAR LIGANDS AND COMPLEXES THEREOF
20170360956 · 2017-12-21 ·

The invention relates to chemical compounds and complexes that can be used in therapeutic and diagnostic applications.

LANTHANIDE-CHELATOR COMBINATORIAL BARCODING
20170348665 · 2017-12-07 ·

Disclosed herein are methods for tracking solutions, (e.g., reaction conditions in solutions). In some embodiments, the method comprises: contacting a first lanthanide-chelator complex to a first solution to generate a first barcoded solution, wherein the first lanthanide-chelator complex comprises a first lanthanide chelated by a first chelator; contacting a second lanthanide-chelator complex to a second solution to generate a second barcoded solution, wherein the second lanthanide-chelator complex comprises a second lanthanide chelated by a second chelator; mixing the first barcoded solution and the second barcoded solution to form one or more mixtures; and identifying the first lanthanide ions in the mass spectrum and the second lanthanide ions in the mass spectrum to track the condition of each of the one or more mixtures.

GROUP III AND LANTHANIDE BIS-PHENYL-PHENOXY METAL-LIGAND COMPLEXES

Embodiments of this disclosure are directed to catalyst systems comprising a metal-ligand complex according to formula (I):

##STR00001##

A METHOD FOR PREPARING GADOBUTROL

The present disclosure relates to a novel method for preparing high-purity gadobutrol. The present disclosure can be easily applied to a large scale production because purity of intermediate can be managed via simple and mild process and accordingly, high-purity or ultra high-purity gadobutrol that has higher purity than previous gadobutrol can be prepared in high yield therethrough.

Lanthanide Toolbox for Organelle Specific Molecular Imaging
20170342090 · 2017-11-30 ·

The present invention relates to a water-soluble, simple, stable tris(N-(tert-butyl)acetamide) cyclen-based europium complex HGEu001 which exhibits the specific subcellular localization in the primary cilium with a quantum yield as high as 10% in water and a lifetime of 0.56 ms lifetime. In particular, the present invention provides simplicity of the design and synthesis of a complex. Comprehensive studies were performed in numerous cell lines, such as HeLa, SN-K-SH and MRC5; the motif structure, HGEu002, has also been synthesized as the negative control for in vitro imaging studies. The two photon in vitro imaging were done in three dimensions to emphasize on the specific localization in primary cilium of HGEu001. This is one of the very limited examples for direct primary cilium imaging.