Patent classifications
A61K51/00
Bioreducible N-oxide-based probes for imaging of hypoxia
Hypoxia occurs when limited oxygen supply impairs physiological functions and is a pathological hallmark of many diseases including cancer and ischemia. Thus, detection of hypoxia can guide treatment planning and serve as a predictor of patient prognosis. Current methods suffer from invasiveness, poor resolution and low specificity. To address these limitations, various hypoxia-responsive probes (HyPs) for photoacoustic imaging are disclosed. The emerging modality converts safe, non-ionizing light to ultrasound waves, enabling acquisition of high-resolution 3D images in deep tissue. The HyPs feature an N-oxide trigger that is reduced in the absence of oxygen by haem proteins such as CYP450 enzymes. Reduction of HyPs produce a spectrally distinct product, facilitating identification via photoacoustic imaging. HyPs exhibit selectivity for hypoxic activation in vitro, in living cells and in multiple disease models in vivo. HyPs are also compatible with NIR fluorescence imaging, establishing its versatility as a multimodal imaging agent.
SUBSTITUTED ORGANOFLUOROBORATES AS IMAGING AGENTS
Fluoridated organofluoroborates comprising at least one .sup.18F atom and precursors thereto, for use in PET scanning.
Development and application of tumor diagnostic radioactive probe targeting folic acid receptor
The present invention pertains to a novel liposome-based contrast agent that is for suppressing absorption in the reticuloendothelial system and for tumor-specific delivery of a radiolabeled substance. More specifically, the present invention pertains to: a liposome contrast agent containing a lipid and a compound of chemical formula 1, which is a radiolabeled substance, the liposome contrast agent being characterized in that the lipid is composed of (a) cholesterol, (b) 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC), and (c) 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N [methoxy(polyethylene glycol)-2000] (DSPE-PEG2000); and a cancer diagnostic composition containing the liposome contrast agent as an active ingredient. If a liposome system, containing a contrast substance of chemical formula 1 having a unique lipid composition provided by the present invention, is manufactured, the tumor-to-organ uptake ratio of the contrast substance in the reticuloendothelial system increases significantly, thus greatly increasing the tumor diagnostic efficiency of the compound of chemical formula 1.
2-[5-(imidazol-1-ylmethyl)pyridin-3-yl]benzimtdazole derivative compound, and medicament including same
Provided are a compound represented by the following formula (1): ##STR00001##
wherein X.sub.1 represents a hydrogen atom or a halogen atom, X.sub.2 represents a fluorine atom or a nitrile group, and X.sub.3 represents a radioactive halogen atom, or a salt thereof, and a medicament including the same.
Fucoidans as ligands for the diagnosis of degenerative pathologies
The present invention relates to the diagnosis of clinical conditions characterized by undesirable and/or abnormal selectin expression. In particular, the invention provides for the use of fucoidans for the detection of selectins using imaging techniques including ultrasonography, scintigraphy and MRI. Selectin-targeted imaging agents are provided that comprise at least one fucoidan moiety associated with at least one detectable moiety. Methods and kits are described for using these imaging agents in the diagnosis of clinical conditions such as thrombosis, myocardial ischemia/reperfusion injury, stroke and ischemic brain trauma, neurodegenerative disorders, tumor metastasis and tumor growth, and rheumatoid arthritis.
Fucoidans as ligands for the diagnosis of degenerative pathologies
The present invention relates to the diagnosis of clinical conditions characterized by undesirable and/or abnormal selectin expression. In particular, the invention provides for the use of fucoidans for the detection of selectins using imaging techniques including ultrasonography, scintigraphy and MRI. Selectin-targeted imaging agents are provided that comprise at least one fucoidan moiety associated with at least one detectable moiety. Methods and kits are described for using these imaging agents in the diagnosis of clinical conditions such as thrombosis, myocardial ischemia/reperfusion injury, stroke and ischemic brain trauma, neurodegenerative disorders, tumor metastasis and tumor growth, and rheumatoid arthritis.
PHARMACEUTICAL COMBINATION FOR THE TREATMENT OF CANCER
The present invention relates to combinations of at least two components, component A and component B, component A being an immune checkpoint inhibitor, and component B being a pharmaceutically acceptable salt of the alkaline-earth radio-nuclide radium-223, the combination being useful for the treatment or prophylaxis of cancer.
PHARMACEUTICAL COMBINATION FOR THE TREATMENT OF CANCER
The present invention relates to combinations of at least two components, component A and component B, component A being an immune checkpoint inhibitor, and component B being a pharmaceutically acceptable salt of the alkaline-earth radio-nuclide radium-223, the combination being useful for the treatment or prophylaxis of cancer.
Use of berberine or derivative thereof in preparing myocardial perfusion imaging agent
Berberine or its derivatives are used in the preparation of myocardial perfusion imaging agents It has been verified using in vitro investigations, in vivo biodistribution, and small animal PET dynamic imaging, etc., that .sup.18F-labeled berberine derivatives can specifically accumulate in cardiomyocytes or heart tissues, and has good distribution properties of targetting heart muscle in living animals, together with high contrast values of heart v.s. peripheral tissue (liver, lung, blood, muscle, bone, etc.).
Radiofluorination method
The present invention relates to a method of labelling biological molecules with .sup.18F, via attachment to fluorine to a macrocyclic metal complex of a non-radioactive metal, where the metal complex is conjugated to the biological molecule. Also provided are pharmaceutical compositions, kits and methods of in vivo imaging.