A61K51/048

NOVEL RADIOMETAL-BINDING COMPOUNDS FOR DIAGNOSIS OR TREATMENT OF PROSTATE SPECIFIC MEMBRANE ANTIGEN-EXPRESSING CANCER

This application relates to compounds of Formula (I-a) or Formula (I-b), or is salts or solvates thereof. R.sup.1 is (CH.sub.2).sub.5CH.sub.3 or comprises 2-4 fused benzene rings. R.sup.2 is I, Br, F, Cl, H, OH, OCH.sub.3, NH.sub.2, NO.sub.2 or CH.sub.3. R.sup.3 is a peptide-bonded glycine, aspartate or glutamate or is glutamate peptide bonded through C.sub.delta. L is CH.sub.2NH, (CH.sub.2).sub.2NH, (CH.sub.2).sub.3NH, or (CH.sub.2).sub.4NH. R.sup.4 is a radiometal chelator optionally bound by a radiometal. Variable n is 1-3. The compounds may be useful for imaging prostate specific membrane antigen (PSMA)-expressing tissues or for treating PSMA-expressing diseases (e.g. cancer).

Indicator Fluids, Systems, and Methods for Assessing Movement of Substances Within, To or From a Cerebrospinal Fluid, Brain or Spinal Cord Compartment of a Cranio-Spinal Cavity of a Human
20200170509 · 2020-06-04 ·

The present invention discloses indicator fluids, reference indicator fluid, and usage thereof, and systems and methods for assessing movement of molecular substances within, to or from a cerebrospinal fluid, brain or spinal cord compartment of a human cranio-spinal cavity. Indicator fluid moving from the cerebrospinal fluid compartment enables measurements of levels of indicator fluid in blood or urine and assessment of the cranio-spinal cavity's ability to remove molecular substances. The indicator fluids may be contrast agents used for imaging, such as by computed tomography imaging, and magnetic resonance imaging, or imaging utilizing radioactive substances by positron emission tomography, single-photon emission computed tomography or scintigraphy. Using these imaging modalities, the invention describes indicator fluids, systems and methods enabling assessment of movement of substances within, to or from a cerebrospinal fluid, brain or spinal cord compartment of a cranio-spinal cavity, and from the human cranio-spinal cavity to lymphatic pathways or kidneys.

Composition for preventing or treating ischemic diseases, containing liposomes in which VEGF-derived peptides are supported

The present invention relates to: a pharmaceutical composition for preventing or treating ischemic diseases, containing liposomes into which vascular endothelial growth factor (VEGF)-derived peptides are loaded; a method for treating ischemic diseases, comprising the step of administering the pharmaceutical composition to an individual suspected of having an ischemic disease; a use of the liposomes; and a kit for evaluating, using the liposomes, the amount of liposomes, into which VEGF-derived peptides are loaded, delivered to ischemic lesions and of loaded materials released and absorbed. The composition, of the present invention, for preventing or treating ischemic diseases, containing liposomes into which VEGF-derived peptides are loaded, the liposomes having an average particle size of 90 to 110 nm and a particle distribution of 50 to 200 nm and being surface-modified with polyethylene glycol, is capable of significantly increasing the absorption of VEGF compared with treatment using solely VEGF, thereby effectively treating ischemic diseases such as myocardial infarction, middle cerebral artery stenosis, lower limb ischemia, and cerebral infarction. In addition, the kit provided in the present invention can be useful in evaluating the amount of liposomes, into which VEGF-derived peptides are loaded, delivered to ischemic lesions and of loaded materials released and absorbed, in a treatment step for a patient with ischemic diseases.

Stable, concentrated radionuclide complex solutions

The present invention relates to radionuclide complex solutions of high concentration and of high chemical stability, that allows their use as drug product for diagnostic and/or therapeutic purposes. The stability of the drug product is achieved by at least one stabilizer against radiolytic degradation. The use of two stabilizers introduced during the manufacturing process at different stages was found to be of particular advantage.

Stable, concentrated radionuclide complex solutions

The present invention relates to radionuclide complex solutions of high concentration and of high chemical stability, that allows their use as drug product for diagnostic and/or therapeutic purposes. The stability of the drug product is achieved by at least one stabilizer against radiolytic degradation. The use of two stabilizers introduced during the manufacturing process at different stages was found to be of particular advantage.

COMPOSITIONS AND METHODS FOR CANCER IMAGING AND RADIOTHERAPY

The present invention relates to a conjugated compound comprising a marker M pharmaceutically acceptable, and a peptide or pseudo-peptide P having at most 30 amino acid residues and able to bind the Low-Density Lipoprotein Receptor (LDLR) and to its use in a method of labelling and/or detecting and/or treating cancerous cells in a subject by administration of the conjugated compound to the subject an analysis of the presence and/or the amount of marker.

ULTRASOUND RESPONSIVE MICRO-COMPOSITE MARKERS

Ultrasound imaging is a non-invasive, non-radioactive, and low cost technology for diagnosis and identification of implantable medical devices in real time. Developing new ultrasound activated coatings is important to broaden the utility of in vivo marking by ultrasound imaging. Ultrasound responsive macro-phase segregated micro-composite thin films were developed to be coated on medical devices composed of multiple materials and with multiple shapes and varying surface area. The macro-phase segregated films having silica micro-shells in polycyanoacrylate produces strong color Doppler signals with the use of a standard clinical ultrasound transducer. Electron microscopy showed a macro-phase separation during slow curing of the cyanoacrylate adhesive, as air-filled silica micro-shells were driven to the surface of the film. The air sealed in the hollow space of the silica shells acted as an ultrasound contrast agent and echo decorrelation of air exposed to ultrasound waves produces color Doppler signals.

Stable, concentrated radionuclide complex solutions

The present invention relates to radionuclide complex solutions of high concentration and of high chemical stability, that allows their use as drug product for diagnostic and/or therapeutic purposes. The stability of the drug product is achieved by at least one stabilizer against radiolytic degradation. The use of two stabilizers introduced during the manufacturing process at different stages was found to be of particular advantage.

Stable, concentrated radionuclide complex solutions

The present invention relates to radionuclide complex solutions of high concentration and of high chemical stability, that allows their use as drug product for diagnostic and/or therapeutic purposes. The stability of the drug product is achieved by at least one stabilizer against radiolytic degradation. The use of two stabilizers introduced during the manufacturing process at different stages was found to be of particular advantage.

COMPOSITIONS AND METHODS FOR CANCER IMAGING AND RADIOTHERAPY

The present invention relates to a conjugated compound comprising a marker M pharmaceutically acceptable, and a peptide or pseudo-peptide P having at most 30 amino acid residues and able to bind the Low-Density Lipoprotein Receptor (LDLR) and to its use in a method of labelling and/or detecting and/or treating cancerous cells in a subject by administration of the conjugated compound to the subject an analysis of the presence and/or the amount of marker.