Patent classifications
A61K49/0021
TWO-PHOTON ABSORBING FLUOROPHORES AND METHOD FOR CELLULAR IMAGING USING THE SAME
The present invention relates to new one-photon or two-photon absorbing fluorophores, a method for preparing the same, and a method for cellular imaging using the same, and more particularly, to new two-photon absorbing fluorophores having higher fluorescence quantum yield and two-photon absorption cross-section value than those of the conventional two-photon absorbing fluorophore, acedan, and thus are promisingly applicable in bioimaging. The design strategy and the compounds according to the present invention may practically utilized for developing new D-π-A fluorophores.
Composition and A Method For Diagnosing And Treating Bacterial Infection
The present invention relates to a composition and a method for use in diagnosing and treating bacterial infection. The composition comprises a novel compound with aggregation-induced emission characteristics adapted to target bacterial and biofilm with fluorescence. The compound is further adapted to generate reactive oxygen species for inhibiting and killing bacteria. The compound can be administered as a stand-alone anti-bacterial fluorescent modular probe or in combination with commercial drugs for enhanced therapeutic efficiencies with fewer side effects.
Two piece sensor assembly and method of use
Disclosed herein is a two-piece sensor assembly that includes an attachment collar configured to attach to a body surface of a patient and comprising at least one opening, and a skin sensor configured to seat into the at least one opening in the attachment collar. The skin sensor includes at least one radiation source configured to irradiate the body surface with at least one interrogation light, and at least one detector configured to detect at least one response light incident from the direction of the body surface.
NOVEL COMPOUNDS FOR IMAGING TAU PROTEINS THAT ACCUMULATE IN BRAIN
The present invention provides a compound represented by the following formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof:
##STR00001##
wherein: R.sub.1 and R.sub.2 are each separately selected from the group consisting of hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl; R.sub.3 is hydrogen or halogen; ring A is a benzene ring or a pyridine ring; ring B is selected from the group consisting of the following formulas (i), (ii), (iii), and (iv):
##STR00002## in the formula (ii), Ra is alkyl; R.sub.4 and R.sub.5 are each separately selected from the group consisting of hydrogen, hydroxy, alkoxy, haloalkoxy, halohydroxyalkoxy, and aminoalkyl; and
##STR00003##
represents a double bond or a triple bond. The above compound can be used as a molecular probe for imaging tau proteins that accumulate in the brain.
CONJUGATES
The present invention provides a conjugate of formula (I) and its use in methods of treatment, and also methods for delivering an active agent into a cell. The methods may be used to deliver an active agent into a nematode, flatworm, parasite or bacterium. The conjugate of formula (I) is: (formula (I)), wherein -D- is C.sub.1-4 alkylene or C.sub.2-4 alkenylene, preferably C.sub.2-4 alkenylene, where the alkylene or alkenylene is optionally substituted with alkyl or halo; A- is an active agent for delivery; and —R.sup.A, —R.sup.B, —R.sup.T1, —R.sup.T2, —R.sup.1, —R.sup.2, —R.sup.3, —X— and -L- are as defined herein.
##STR00001##
Probe for a biological specimen and labelling method and screening method using the probe
Provided is a novel probe for a biological specimen for labelling by itself and clearly visualizing one of a specific cell and a specific cell organ in a living body, the probe having excellent spectral characteristics and exhibiting excellent storage stability. The probe for a biological specimen contains, as an active agent, at least one kind of compound represented by a general formula (I). ##STR00001##
Methods and compositions for detecting drusen and predicting age-related macular degeneration
Labels and methods are provided for detecting deposits, including drusen, sub-retinal deposits, basal laminar and linear deposits, and the like. The labels can detect the presence, progression, or regression of hydroxyapatite, which can be indicative of the presence or the potential to develop such deposits. The labels can include a conjugate comprising a hydroxyapatite binding moiety and a label moiety, which can provide a detectable signal upon binding of the conjugate to hydroxyapatite. The labels and methods can be utilized to detect deposits in eye tissue, such as the retina, brain tissue, or the like. Methods are also provided for utilizing the present labels to predict or diagnose a neurodegenerative disease, including age-related macular degeneration. Accordingly, some methods can predict or diagnose age-related macular degeneration, including early signs or advanced forms thereof, based on the presence of hydroxyapatite in a tissue sample obtained from a subject.
Therapeutic inhibitor for EBV-associated tumor with tailor responsive optical imaging
This invention provides a nucleus-permeable small-molecule inhibitor, L.sub.2P.sub.4 (where L.sub.2 is 4-(4-(Diethylamino)styryl)-N-carboxymethylpyridinium chloride and P.sub.4 is an amino acid sequence comprising CAhxYFMVFGGRrRK and they were coupled through amide bond) and synthesis thereof, which effectively targets the dimerization interface of EBNA1, a critical process for the growth of EBVs and the associated tumors. The present invention also provides method of treating and imaging EBV-associated cancers.
Ocular detection of amyloid proteins
Described are methods for the detection, in the eye of an individual, of protein aggregates or other misfolded proteins associated with disease using peptide or peptide mimic probes that preferentially associate with the protein aggregates or misfolded proteins, which can be accomplished non-invasively.
Imaging beta-amyloid peptides aggregation
The present invention is in the field of pharmaceuticals and chemical industries. In particular, one aspect of the present invention relates to methods for labeling, imaging and detecting the beta-amyloid (Aβ) peptides, oligomers, and fibrils in vitro and in vivo via magnetic resonance and florescence imaging by using modified carbazole-based fluorophores. A further aspect of the present invention relates to a method of reducing and preventing aggregation of beta-amyloid peptides for Alzheimer's disease (AD) as well as of treating and/or preventing Alzheimer's disease by using the modified carbazole-based fluorophore. The modified carbazole-based fluorophore according to an embodiment of the present invention is prepared by conjugating a carbazole-based fluorophore with magnetic nanoparticles to form a conjugate which is permeable to blood brain barrier of a subject being introduced therewith.