Patent classifications
C09B23/0008
Dyes and compositions, and processes for using same in analysis of protein aggregation and other applications
Provided are dyes and compositions which are useful in a number of applications, such as the detection and monitoring protein aggregation, kinetic studies of protein aggregation, neurofibrillary plaques analysis, evaluation of protein formulation stability, protein thermal stability shift assay and analysis of molecular chaperone activity. These dyes and compositions are also useful as probes in nucleic acid and protein detection.
Tamoxifen derivatives for treatment of neoplastic diseases, especially with high HER2 protein level
The subject of the invention are new mitochondrially targeted E/Z isomers of aliphatic triphenylphosphonium derivatives of tamoxifen where the aliphatic chain is alkyl or alkenyl, and their corresponding tertiary amine salts and/or their mixture (MitoTAX). Alkyl triphenylphosphonium derivatives of tamoxifen have the general formula (I), where n=8 to 12 and where Z is selected from the group of organic salts or inorganic salts. Alkenyl triphenylphosphonium derivatives of tamoxifen have the general formula IA, where n=6 to 10 and where Z has the above mentioned meaning. These compounds are applicable for the treatment of neoplastic disease, especially those with high HER2 protein levels. The drug for the treatment of neoplastic diseases according to the invention contains at least one E/Z isomer of aliphatic triphenylphosphonium derivatives of tamoxifen of the general formula (I) and/or IA or their corresponding salts of tertiary amine.
Integrin targeting agents and in-vivo and in-vitro imaging methods using the same
The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.
CYANINE COMPOUNDS
Compounds used as labels with properties comparable to known fluorescent compounds. The compounds can be conjugated to proteins and nucleic acids for biological imaging and analysis. Synthesis of the compounds, formation and use of the conjugated compounds, and specific non-limiting examples of each are provided.
APPLICATION OF REDUCED DYES IN IMAGING
The present invention provides novel compounds and methods for hydrocyanines derived from near-infrared cyanine dyes, as reactive oxygen species probes in imaging. In certain embodiments, the present invention provides reduced dyes as substrates for ELISA and Western blots.
Fluorescent Imaging Agents
Provided is a family of intramolecularly quenched imaging agents for use in both in vivo and in vitro imaging that contain at least one enzymatically cleavable oligopeptide and two fluorophores or a fluorophore and a quencher. When subjected to proteolytic cleavage, at least one fluorophore is unquenched and becomes capable of producing a fluorescent signal upon excitation with light of an appropriate wavelength. Also provided are in vivo and in vitro imaging methods using such imaging agents.
POLARIZING PLATE, APPARATUS, HEAD-MOUNTED DISPLAY, ORGANIC ELECTROLUMINESCENT DISPLAY DEVICE, AND IMAGING SYSTEM
A polarizing plate that, when being applied to an apparatus in which at least one of a display element or a visible light imaging element and an infrared light sensing system are combined, detection performance of the infrared light sensing system is excellent, and display performance is excellent when the apparatus includes the display element or imaging performance is excellent when the apparatus includes the imaging element; an apparatus; a head-mounted display; an organic electroluminescent display device; and an imaging system. In the polarizing plate, an average transmittance at a wavelength of 400 to 700 nm is 70% or more, a maximum value of a polarization degree at a wavelength of 800 to 1500 nm is 80% or more, and when a wavelength at which the polarization degree is the maximum value is defined as a wavelength 1, a transmittance T(1) at the wavelength 1 satisfies predetermined relationships.
NEAR-IR GLUCOSE SENSORS
Glucose-sensing luminescent dyes, polymers, and sensors are provided. Additionally, systems including the sensors and methods of using these sensors and systems are provided.
Sterically shielded heptamethine cyanine dyes
The near-infrared window of fluorescent heptamethine cyanine dyes greatly facilitates biological imaging because there is deep penetration of the light and negligible background fluorescence. But dye instability, aggregation, and poor pharmacokinetics are current drawbacks that limit performance and the scope of possible applications. All these limitations are simultaneously overcome with a new molecular design strategy that produces a charge balanced and sterically shielded fluorochrome. The key design feature is a meso-Aryl group that simultaneously projects two shielding arms directly over each face of a linear heptamethine polyene. Cell and mouse imaging experiments compared a shielded heptamethine cyanine dye (and several peptide and antibody bioconjugates) to benchmark heptamethine dyes and found that the shielded systems possess an unsurpassed combination of photophysical, physiochemical and biodistribution properties that greatly enhance bioimaging performance.
METHODS AND COMPOSITIONS RELATED TO MODIFIED FLUOROPHORES
The present invention provides a novel one-step synthesis method for producing cyanine-based fluorophores with modified polymethine chains to prevent aggregation, enhancing their utility in biomedical research. These fluorophores, such as unsymmetrical heptamethine cyanines like SAT-IR-746, exhibit improved sensitivity, photostability, and brightness, making them ideal for applications such as live-cell imaging, biomolecule labeling, and near-infrared fluorescence microscopy. The synthesis process involves the preparation of a pyridinium benzoxazole (PyBox) intermediate from a substituted pyridine derivative and 2-chlorobenzoxazole, followed by condensation with sulfonated and substituted indolenines to form asymmetrical cyanine dyes, achieving high yields (e.g., 55-82% for SAT-IR series compounds). By addressing the aggregation issue common in traditional cyanine dyes through -position substitution on the polymethine chain, this invention enables more accurate and reliable labeling and tracking of biomolecules without quenching, facilitating advanced imaging techniques and deeper insights into biological processes.