Patent classifications
A61K49/0039
Boronated Multifunctional Targeting Drug Conjugates, Their Uses and Methods for Their Preparation
Tri-component multi-functional boronated complexes (B-complexes), featuring reversible covalent bonds, are described, which incorporate a drug; a water-soluble moiety (e.g. polyethylene glycol (PEG) chains, cyclodextrins); and a targeting unit. A B-complex core was assembled in one step, and proved to be stable in different biocompatible conditions, such as human plasma, though reversible for example in the presence of glutathione (GSH). This platform enabled the modular construction of the multifunctional conjugates exhibiting high selectivity towards, for example, folate-receptor-positive MDA-MB-231 cancer cells, having an IC.sub.50 in the low nanomolar range.
Bioorthogonal turn-on probes
This present application relates to fluorescent tetrazine-containing compounds consisting of a single pi-system. For example, a compound of Formula (I): or a salt thereof, wherein: F is a fluorophore, L is a conjugated linker, and Tz is a substituted or unsubstituted tetrazine; wherein the linker bridges the Tz and F moieties in a single conjugated pi-system. Also provided herein are methods of using the compounds provided herein for biomedical imaging.
Boronated multifunctional targeting drug conjugates, their uses and methods for their preparation
Tri-component multi-functional boronated complexes (B-complexes), featuring reversible covalent bonds, are described, which incorporate a drug; a water-soluble moiety (e.g. polyethylene glycol (PEG) chains, cyclodextrins); and a targeting unit. A B-complex core was assembled in one step, and proved to be stable in different biocompatible conditions, such as human plasma, though reversible for example in the presence of glutathione (GSH). This platform enabled the modular construction of the multifunctional conjugates exhibiting high selectivity towards, for example, folate-receptor-positive MDA-MB-231 cancer cells, having an IC.sub.50 in the low nanomolar range.
Selective hydrogen sulfide probe and uses thereof
Provided herein is a compound of formula I: ##STR00001##
and the use thereof for detecting the presence of hydrogen sulfide in cells or tissues in vitro or in vivo. The detecting may be useful, for example, in diagnosing cancer or other diseases related to imbalanced hydrogen sulfide (H.sub.2S) production such as neurodegenerative diseases.
NON-INVASIVE ENERGY UPCONVERSION METHODS AND SYSTEMS
Products, compositions, systems, and methods for modifying a target structure which mediates or is associated with a biological activity, including treatment of conditions, disorders, or diseases mediated by or associated with a target structure, such as a virus, cell, subcellular structure or extracellular structure. The methods may be performed in situ in a non-invasive manner by placing a nanoparticle having a metallic shell on at least a fraction of a surface in a vicinity of a target structure in a subject and applying an initiation energy to a subject thus producing an effect on or change to the target structure directly or via a modulation agent. The nanoparticle is configured, upon exposure to a first wavelength .sub.1, to generate a second wavelength .sub.2 of radiation having a higher energy than the first wavelength .sub.1. The methods may further be performed by application of an initiation energy to a subject in situ to activate a pharmaceutical agent directly or via an energy modulation agent, optionally in the presence of one or more plasmonics active agents, thus producing an effect on or change to the target structure. Kits containing products or compositions formulated or configured and systems for use in practicing these methods.
Multimodal ultrasound and photoacoustic contrast agent based on polymeric microparticles
The invention provides a multimodal ultrasound and photoacoustic contrast agent based on polymeric microparticles having a gas core and carrying at least one photoacoustic agent in its shell that stabilizes the gas core, for use in ultrasound and photoacoustic imaging. Such multimodal ultrasound and photoacoustic contrast agent is also suitable as a carrier of drugs and for use in photodynamic therapy, and for tissue imaging ex vivo.
Boronated Multifunctional Targeting Drug Conjugates, Their Uses and Methods for Their Preparation
Tri-component multi-functional boronated complexes (B-complexes), featuring reversible covalent bonds, are described, which incorporate a drug; a water-soluble moiety (e.g. polyethylene glycol (PEG) chains, cyclodextrins); and a targeting unit. A B-complex core was assembled in one step, and proved to be stable in different biocompatible conditions, such as human plasma, though reversible for example in the presence of glutathione (GSH). This platform enabled the modular construction of the multifunctional conjugates exhibiting high selectivity towards, for example, folate-receptor-positive MDA-MB-231 cancer cells, having an IC.sub.50 in the low nanomolar range.
BORYL ETHERS, CARBONATES, AND CYCLIC ACETALS AS OXIDATIVELY-TRIGGERED DRUG DELIVERY VEHICLES
A compound, or a pharmaceutically acceptable salt thereof, having a structure of:
##STR00001##
wherein L is a cleavable linker group;
X is a cargo moiety-containing group; and
R.sup.1 and R.sup.2 are each independently hydrogen, alkyl, or substituted alkyl; or R.sup.1 and R.sup.2 together form a boronic ester ring or a substituted boronic ester group.
Method for imaging cell using fluorescence-labeled sugar derivative having coumarin derivative bound thereto, and imaging agent
The present invention has an object of providing a sugar derivative emitting blue fluorescence color which can be used for imaging of cells or intracellular molecules and a method for imaging cells using the derivative. Further, the present invention has an object of providing a method for detecting cancer cells at high accuracy by imaging, and an imaging agent used for this method. The present invention provides a fluorescently labeled sugar derivative having 3-carboxy-6,8-difluoro-7-hydroxycoumarin or 3-carboxymethyl-6,8-difluoro-7-hydroxy-4-methylcoumarin as a fluorescent molecular group in its molecule, and a cell imaging agent and an imaging method using the derivative. Further, the present invention provides an imaging agent and an imaging method for cancer cells using an L-glucose derivative having the above-described fluorescent molecular group in its molecule.
POLY(N-BUTYL CYANOACRYLATE) NANOPARTICLE WITH DUAL MODIFICATIONS, PREPARATION METHOD AND USE THEREOF
The invention relates to a poly(n-butyl cyanoacrylate) nanoparticle with dual modifications, a drug delivery system comprising the nanoparticle, and a method for preparing the nanoparticle or the drug delivery system. The nanoparticle is modified with a first modifier and a second modifier on the surface, the first modifier is a hydrophilic polymer, and the second modifier is an amino acid and/or a lipid. The invention further relates to a use of the nanoparticle in promoting drug penetration across the blood brain barrier in a subject.