18 results about "Macrocyclic ligand" patented technology

The invention relates to ligands and complexes of metal ions with the ligands useful in various applications, including therapeutic and diagnostic applications.

Methods, systems, and compositions for oxidation are provided. The method includes combining a macrocyclic ligand and a metal complex catalyst, an electrolyte, a substrate, and water to form an aqueous composition. The method includes applying a voltage to the aqueous composition and oxidizing the substrate in the presence of a catalyst.

The invention discloses hydrogel microspheres capable of loading radioactive isotopes and a preparation method of the hydrogel microspheres. The microsphere is formed by copolymerizing a macrocyclic ligand structure, a hydrophilic monomer and a cross-linking agent, and a macrocyclic ligand is connected with a polymer main chain through a bridging structure containing p-aminobenzoic acid and aliphatic diamine and can efficiently and stably complex various radioactive isotopes. The microspheres have the characteristics of being close to water in density, good in suspension property, smooth in surface and rich in elasticity, and are easily and uniformly distributed in tumor peripheral blood vessels. The preparation method comprises the following two routes: firstly synthesizing the functional monomer and then copolymerizing, or firstly preparing the microspheres and then gradually grafting. The problems that existing microsphere nuclides are prone to falling off, high in density and poor in suspension property are effectively solved, and the microsphere is suitable for interventional radioactive embolism treatment.

The application belongs to the technical field of medical detection, and particularly relates to a polysaccharide contrast agent capable of renal metabolism and a preparation method thereof. The polysaccharide contrast agent has a structure as shown in formula (I), a particle size less than or equal to 8 nm, and can be rapidly metabolized through the kidney. The preparation method is to graft a metal macrocyclic ligand to a nano-crosslinked polysaccharide particle, and to prepare through a deprotection and metal ion chelation step. Since the contrast agent has the characteristic of renal metabolism, phagocytosis of the reticuloendothelial system is reduced, in vivo deposition of the contrast agent is reduced, and thus the biological safety is improved. Since a macrocyclic chelating ligand is used, good kinetic stability is achieved, the risk of in vivo metal ion deposition is reduced, and when applied to in vivo imaging, clear imaging of cardiovascular, lymph node, liver and other parts can be achieved. The preparation method is simple and easy to implement, reaction conditions are mild, is conducive to large-scale production and clinical transformation, and has a wide biomedical application prospect.

The present invention relates to macrocyclic FKBP51-binding compounds having improved characteristics, as well as solvates, hydrates and / or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and / or diluents. Said compounds have been identified as especially potent ligands of FK506 binding proteins (FKBPs also called MIPs in bacteria), especially human FKBP51 and are useful for treatment of diseases such as psychiatric, metabolic and neurological disorders as well as pain and cancers. Said substituted derivatives may further be used as agents for inducing protein-protein interactions (PPIs) acting as molecular glues (FIG. 10).

The invention discloses a Gd (III) complex solvent paramagnetic relaxation enhanced probe and a preparation method thereof, and belongs to the technical field of biological macromolecule nuclear magnetic resonance analysis. The Gd (III) complex is provided with a large cyclic ligand, diethylene triamine pentaacetic acid dianhydride (DTPAA) and 1, 8-diamino-3, 6-dioxaoctane are subjected to a reaction under the catalysis of triethylamine, and a cyclic compound DTPA-BAE is generated; and carrying out coordination with gadolinium oxide to obtain the Gd (III) complex Gd-DTPA-BAE. Due to the fact that the ligand is in a large ring shape instead of a chain shape, Gd < 3 + > is not prone to being separated, the chemical stability of the Gd-DTPA-BAE serving as the solvent paramagnetic relaxation enhancing probe is higher, the coordination number is as high as 10, hydrophobicity is weak, the system error of solvent relaxation enhancing determination is reduced, and the accuracy of protein dynamic structure determination is improved.

The present invention relates to new macrocyclic ligands substituted by at least one picolinic ester group, to radioactive complexes thereof and to their use in medical imaging and / or therapy, in particular in interventional radiology. The present invention also relates to new processes for the preparation of the ligands according to the invention, and also to intermediates in the preparation thereof.

Aspects of the present disclosure relate to compounds which have enhanced oral bioavailability. A transition metal complex includes a transition metal coordinated by a macrocycle comprising the pentaaza 15-membered macrocyclic ring corresponding to Formula A and two axial ligands having the formula —OC(O)X1.each of the two axial ligands has the formula —OC(═O)X1 wherein each X1 is independently substituted or unsubstituted phenyl or —C(—X2)(—X3)(—X4);each X2 is independently substituted or unsubstituted phenyl, or substituted or unsubstituted alkyl;each X3 is independently hydrogen, hydroxyl, alkyl, amino, —X5C(═O)R13 where X5 is NH or O, and R13 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or —OR14, where R14 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or together with X4 is (=O); andeach X4 is independently hydrogen or together with X3 is (=O).

The invention relates to a process for the preparation of a macrocyclic ligand of formula (L) : involving: i) decomplexation of a complex of formula (II) : which complex consists of at least 80% diastereomeric excess, which diastereomeric excess comprises a mixture of isomers II-RRR and II-SSS of formulae: ii) removal of the gadolinium salt formed in step i) for example by filtration, and iii) recovery of the free macrocyclic ligand of formula (L). The invention also relates to a composition comprising a diastereomeric enriched complex of formula (II) and a macrocyclic ligand of formula (L).

A process for preparing a tetra-substituted aminobiphenol macrocyclic ligand having the structure (I), including the step of treating a precursor compound having the structure (II) with a compound having the structure R6-L where L is a leaving group (hereafter compound (III)) in the presence of a base.

The invention discloses a bifunctional albumin nanoparticle, a preparation method, a pharmaceutical composition and application. The nanoparticle takes albumin as a carrier, the surface of the nanoparticle is modified with a macrocyclic ligand chelating agent chelated with gadolinium ions, and the nanoparticle is internally wrapped with a hydrophobic boron-containing compound. The bifunctional albumin nanoparticle has good T1 weighted magnetic resonance imaging capability, can be used for tracking distribution and enrichment of boron-containing drugs in vivo in real time, realizes collaborative application with a boron neutron capture therapy, and is beneficial to evaluation of a treatment window and improvement of treatment accuracy; the particle size is uniform, the zeta potential is stable, the drug loading capacity and the tissue penetrability are good, and targeted enrichment on tumor tissues is facilitated; according to the bifunctional albumin nano-particles, human serum albumin is preferably selected as a nano-particle carrier, so that the bifunctional albumin nano-particles have excellent biocompatibility and good in-vivo stability, are high in safety and are beneficial to clinical transformation.

The present invention relates to a method of degrading biofilm by contacting it with an aqueous mixture comprising a peroxide compound and a manganese complex, wherein the aqueous mixture comprises a macrocylic ligand. The invention also relates to a method of degrading a biofilm by contacting it with an aqueous mixture comprising a peroxide compound and a macrocyclic ligand.

The invention discloses a dye with a Donor-Acceptor (D-A) structure, a laser gain medium containing the dye and application of the dye, and aims to solve the key technical problem that the gain capacity of the existing dye is reduced due to aggregation quenching under high concentration. The structural general formula of the organic dye molecules is shown in the specification. R1 is selected from alkyl, hydroxyl-substituted alkyl, sulfonic acid-substituted alkyl, carboxylic acid-substituted alkyl, alkylene and phenyl, R2 is selected from alkyl, phenyl, alkoxy phenyl and alkylphenyl, X is selected from S or O, and n is selected from 1, 2 and 3; the dye can form an aggregate through intermolecular interaction under high concentration, two new energy levels independent of a single-molecule excited state are generated, a four-energy-level system beneficial to population inversion is constructed, and low-threshold amplified spontaneous emission (ASE) can still be achieved even if the quantum yield is lower than 0.49%; the macrocyclic ligand can regulate and control the microenvironment of the cavity to inhibit aggregation and quenching among dye molecules, improve the solubility of the dye, optimize the excited state behavior and further reduce the ASE threshold value. Meanwhile, accurate regulation and control of ASE emission wavelength can be realized by adjusting electron-donating groups in dye molecules.

This invention relates to a method for the electrocatalytic oxidation of anisole to anisole sulfoxide using iron-based complexes, belonging to the fields of homogeneous catalysts and electrocatalytic oxidation technology. The invention utilizes an iron-based complex formed by coordination between a tetraamide macrocyclic ligand (TAML-H4) and metallic iron as a homogeneous molecular catalyst, with water as the sole oxygen source, to construct an electrocatalytic anisole oxidation system. Through the synergistic effect of the catalyst and water, a proton-coupled electron transfer and single-electron oxidation process occurs at the anolyte, resulting in the loss of two electrons and two protons to generate a high-valence iron-oxygen active intermediate [Fe]. Ⅴ (O)(TAML)] – This invention achieves highly efficient and selective oxidation of anisole, generating the high-value-added product benzyl sulfoxide at the anode. It eliminates the need for additional strong oxidants, employs mild reaction conditions, boasts high atom economy, and is environmentally friendly, making it suitable for the green conversion of sulfides in the synthesis of fine chemicals. This provides a feasible pathway for the industrial production of sulfoxide compounds.

A process for the preparation of a tetra-substituted amino bisphenol macrocyclic ligand of structure (I) comprising the step of treating a precursor compound of the invention having structure (II) with a compound of the invention having structure R6-L (III) in the presence of a base and the corresponding tetra-amino bisphenol macrocyclic ligand.

The present disclosure provides a chemical-biological treatment method for removing nitrogen contaminants from nitrogen-containing wastewater. The method comprises pre-treating the nitrogen-containing wastewater with an oxidant in the presence of a catalyst to form an oligomer mixture; precipitating the oligomer mixture by further addition of an oxidizing agent to obtain a solid precipitate and a supernatant wherein the supernatant comprises one or more inorganic nitrogen compounds; separating the supernate from the solid precipitate; and contacting the supernatant with a microbial culture to convert the one or more inorganic nitrogen compounds to nitrogen wherein the catalyst comprises an iron-tetraamido macrocyclic ligand (Fe-TAML) or a peroxidase; and wherein the microbial culture comprises denitrifying bacteria and anaerobic ammonia oxidizing bacteria.

Methods, systems, and compositions for oxidation are provided. The method comprises combining a macrocyclic ligand and metal complex catalyst, an electrolyte, the substrate, and water to form an aqueous composition. The method comprises applying an electrical voltage to the aqueous composition and oxidizing the substrate in the presence of the catalyst.