A61K49/0019

PYCLEN-BASED MACROCYCLIC LIGANDS, CHELATES THEREOF AND USES THEREOF

A ligand of Formula (A):

##STR00001## or a carboxylate salt thereof; wherein Y.sup.1, Y.sup.2 and Y.sup.3 each independently represents COOH or a picolinate of Formula (i):

##STR00002##

wherein each R.sup.1 independently represents a chromophore group; L.sup.1, L.sup.2 and L.sup.3 each independently represents a single bond or a linker; and X.sup.1, X.sup.2 and X.sup.3 each independently represents a hydrogen atom, a coupling function or a bio-vectorizing group. Also, a process for manufacturing the ligand and to a process for manufacturing a chelate by complexation by the ligand of a rare-earth cation, preferably a lanthanide cation. Further, a use of the ligand and/or the chelate in biological imaging and/or photoluminescence imaging.

BLOOD-BRAIN BARRIER PERMEABLE PEPTIDE COMPOSITIONS
20210017262 · 2021-01-21 ·

Blood-brain barrier permeable peptide compositions that contain variable antigen binding domains from camelid and/or shark heavy-chain only single-domain antibodies are described. The variable antigen binding domains of the peptide compositions bind to therapeutic and diagnostic biomarkers in the central nervous system, such as the amyloid-beta peptide biomarker for Alzheimer's disease. The peptide compositions contain constant domains from human IgG, camelid IgG, and/or shark IgNAR. The peptide compositions include heavy-chain only single-domain antibodies and compositions with one or more variable antigen binding domain bound to one or more constant domains.

SEMICONDUCTOR SWCNT SLURRY FOR BIOIMAGING AND METHOD FOR INSPECTING THE SAME

An object is to provide a method of inspection enabling a slurry of a batch resulting in abnormal accumulation to be identified in advance, and to provide an SWCNT slurry for bioimaging that has undergone the inspection.

In order to solve the above problems, the present invention provides a method for inspecting a semiconductor single-walled carbon nanotube (SWCNT) slurry for bioimaging, the slurry comprising: semiconductor SWCNTs oxidized by being directly irradiated with ultraviolet rays in atmosphere and a dispersant composed of an amphiphilic substance that coats surfaces of the SWCNTs, the method comprising: using at least two types of methods selected from the group consisting of absorption spectroscopy, a photoluminescence method, and particle size measurement, confirming that an average particle size of the semiconductor SWCNTs is smaller than 10 nm, isolated dispersibility of the semiconductor SWCNTs is high, and/or the semiconductor SWCNTs are oxidized.

SCAFFOLDS AND MULTIFUNCTIONAL INTERMEDIATES FOR IMAGING PSMA AND CANCER THERAPY

Carbamate and beta-amino acid urea-based scaffolds that have high binding affinity to PSMA are disclosed. These scaffolds can be radiolabeled and used for imaging cells and tumors that express PSMA or for cancer radiotherapy. These compounds also can comprise a fluorescent dye and be used for imaging cells and tumors that express PSMA or for photodynamic therapy.

Super-resolution fluorescent imaging probe

[Problem] To provide a novel fluorescent probe for super-resolution imaging that uses fluorescent light emission characteristics that originate from an intermolecular nucleophilic addition-dissociation equilibrium reaction, and to provide a super-resolution fluorescent imaging method that uses the probe. [Solution] A fluorescent probe for super-resolution imaging that comprises a compound represented by formula (I) or a salt thereof [in the formula, X represents an oxygen atom, C(R.sup.a)(R.sup.b), or Si(R.sup.a)(R.sup.b) (wherein R.sup.a and R.sup.b each independently represent a hydrogen atom or an alkyl group), R.sup.1 represents a hydrogen atom or an optionally substituted aryl (provided that, if R.sup.1 is a phenyl group, the benzene ring of the phenyl group does not have a substituent at position 2 or position 6), R.sup.2 and R.sup.3 each independently represent 1-3 identical or differing substituents that are independently selected from the group that consists of hydrogen atoms, hydroxyl groups, halogen atoms, optionally substituted alkyl groups, optionally substituted sulfo groups, optionally substituted carboxyl groups, optionally substituted ester groups, optionally substituted amide groups, and optionally substituted azide groups, R.sup.4 and R.sup.5 each independently represent a hydrogen atom or an optionally substituted alkyl group or N(R.sup.4)(R.sup.5) forms an amide group or a carbamate group (provided that, if R.sup.4 or R.sup.5 is an alkyl group, each may form, together with R.sup.2, a ring structure that contains the nitrogen atom that is bonded thereto), and R.sup.6 and R.sup.7 each independently represent a hydrogen atom or an optionally substituted alkyl group or N(R.sup.6)(R.sup.7) forms an amide group or a carbamate group (provided that, if R.sup.6 or R.sup.7 is an alkyl group, each may form, together with R.sup.3, a ring structure that contains the nitrogen atom that is bonded thereto)], the fluorescent probe for super-resolution imaging being characterized in that the compound represented by formula (I) or the salt thereof undergoes a nucleophilic addition-dissociation equilibrium reaction with a nucleophilic compound that contains an SH group.

Multifunctional infrared-emitting composites

Disclosed is a method of non-invasive infrared imaging, comprising (a) administering a composition containing infrared-emitting particles which contain rare earth elements that emit in the short-wavelength infrared (SWIR) spectrum, where the particles are encapsulated with a biocompatible matrix to form downconverting encapsulated particles; and (b) irradiating with infrared radiation, where both excitation and emission spectra of the encapsulated particles are in the infrared region. Analogous methods of image-guided biomedical intervention, and drug tracking and delivery are also disclosed. Also disclosed is a composition for biomedical applications, containing infrared-emitting particles which contain rare earth-elements that emit in the short-wavelength infrared (SWIR) spectrum, where the particles are encapsulated with a biocompatible matrix to form downconverting encapsulated particles.

Toll-like receptor 2 ligands and methods of making and using thereof

Disclosed are monoacylated Toll-like receptor 2 ligands which can be used in both the development of targeted agents for the imaging and treatment of pancreatic cancer as well as other cancers, and as an adjuvant for cancer immunotherapy. The monoacylated compounds disclosed herein have a higher binding affinity for TLR2 relative to a known potent diacylated agonists, but only the bioactivity. Competition of the monoacylated compound with the diacylated compound for binding TLR2 was confirmed. Hence, the reported monoacylated compounds are inhibitors/antagonists of TLR2 activation.

TURN-ON NEAR INFRARED FLUORESCENT PROBES FOR IMAGING LYSOSOMAL ROS IN LIVE CELLS AT SUBCELLULAR RESOLUTION
20200309698 · 2020-10-01 ·

This invention is in the field of fluorescence imaging and relates to a new near infrared (NIR) reactive oxygen species (ROS) sensor designed with controlled fluorescence on-off switching mechanism.

Blood-brain barrier permeable peptide compositions comprising a VAB domain of an anti-amyloid-beta camelid single-domain heavy-chain only antibody
10738109 · 2020-08-11 · ·

Blood-brain barrier permeable peptide compositions that contain variable antigen binding domains from camelid and/or shark heavy-chain only single-domain antibodies are described. The variable antigen binding domains of the peptide compositions bind to therapeutic and diagnostic biomarkers in the central nervous system, such as the amyloid-beta peptide biomarker for Alzheimer's disease. The peptide compositions contain constant domains from human IgG, camelid IgG, and/or shark IgNAR. The peptide compositions include heavy-chain only single-domain antibodies and compositions with one or more variable antigen binding domain bound to one or more constant domains.

GASTROINTESTINAL TRACT DETECTION METHODS, DEVICES AND SYSTEMS

The present disclosure relates to gastrointestinal (GI) tract detection methods, devices and systems.