Patent classifications
A61K51/0478
COMPOUNDS AND COMPOSITIONS FOR TARGETING MACROPHAGES AND OTHER MANNOSE-BINDING C-TYPE LECTIN RECEPTOR HIGH EXPRESSING CELLS AND METHODS OF TREATING AND DIAGNOSIS USING SAME
Provided are compounds and compositions for targeting macrophages and other mannose-binding c-type lectin receptor high expressing cells and methods of treatment and diagnosis using such compounds and compositions.
CONJUGATES DERIVED FROM NON-STEROIDAL ANTI-INFLAMMATORY DRUGS AND METHODS OF USE THEREOF IN IMAGING
Conjugates derived from non-steroidal anti-inflammatory drugs (NSAIDs) and methods of use thereof are disclosed, useful for, inter alia, identifying and localizing the site of pathology and/or inflammation responsible for the sensation of pain in a patient; for identifying the sites of primary, secondary, benign, or malignant tumors; and for diagnosing infection or confirming or ruling out suspected infection. The NSAID-based conjugates contain an imaging moiety. The conjugates concentrate at sites of increased cyclooxygenase expression, thus revealing the sites of increased prostaglandin production, which is correlated with pain and inflammation, and correlated with tumor presence and/or location. Identifying areas of increased COX expressing can also aid in screening for infections.
CONJUGATES DERIVED FROM NON-STEROIDAL ANTI-INFLAMMATORY DRUGS AND METHODS OF USE THEREOF IN IMAGING
Conjugates derived from non-steroidal anti-inflammatory drugs (NSAIDs) and methods of use thereof are disclosed, useful for, inter alia, identifying and localizing the site of pathology and/or inflammation responsible for the sensation of pain in a patient; for identifying the sites of primary, secondary, benign, or malignant tumors; and for diagnosing infection or confirming or ruling out suspected infection. The NSAID-based conjugates contain an imaging moiety. The conjugates concentrate at sites of increased cyclooxygenase expression, thus revealing the sites of increased prostaglandin production, which is correlated with pain and inflammation, and correlated with tumor presence and/or location. Identifying areas of increased COX expressing can also aid in screening for infections.
Pet imaging of zinc transport
A method for producing a solution including a positron emitting zinc cation of .sup.63Zn, and the method comprises bombarding a solution target including .sup.63Cu with high energy protons to produce a solution including a positron emitting zinc cation. A method for detecting or ruling out Alzheimer's disease in a patient comprises administering to a patient a detectable amount of a compound including a positron emitting zinc cation, wherein the zinc cation is targeted to beta-amyloid in the patient, and acquiring an image to detect the presence or absence of beta-amyloid in the patient.
METHOD OF IMAGING WITH A CHELATING AGENT
The present disclosure relates to a method for imaging cancer by administering to a patient a labeled chelating compound and an unlabeled chelating compound.
Methods and kits for preparing radionuclide complexes
A method for preparing a complex comprising a radioisotope of gallium for use in radiotherapy or in a medical imaging procedure, said method comprising adding a gallium radioisotope solution obtained directly from a gallium radionuclide generator to a composition comprising a pharmaceutically acceptable buffer and optionally also a pharmaceutically acceptable basic reagent, in amounts sufficient to increase the pH to a level in the range of 3 to 8, wherein the composition further comprises a chelator that is able to chelate radioactive gallium within said pH range and at moderate temperature, said chelator being optionally linked to a biological targeting agent. Kits and compositions for use in the method are also described and claimed.
CONJUGATES COMPRISING COVALENT BINDERS FOR TARGETING INTRACELLULAR KRAS G12C PROTEINS
Provided herein are radiopharmaceutical compositions, conjugates and uses thereof. In one aspect, provided herein are covalently modified KRAS proteins comprising a radiolabeled compound or conjugate. In some embodiments, the radiolabeled compound described herein comprises a covalently bound radioisotope. In some embodiments, the radiolabeled conjugate comprises a targeting ligand and a metal chelator configured to bind a radionuclide. The radiolabeled compound or conjugate described herein can form a covalent bond with a cysteine residue (such as G12C) in the mutated KRAS protein. Further provided herein are methods of treating and diagnosing cancer by administering the described radiolabeled compounds, conjugates, and compositions to a subject, thereby forming the covalently modified KRAS G12C protein.
COMPOUNDS, COMPOSITIONS AND ASSOCIATED METHODS USING ZIRCONIUM-89 IN IMMUNO-POSITRON EMISSION TOMOGRAPHY
Disclosed are novel compounds, complexes, compositions and methods using Zirconium-89 combined with azamacrocyclic chelators in connection with PET. The compositions and methods should provide better diagnostic, prognostic and therapeutic oncology treatments relative to the presently available chelator compositions due to a variety of superior properties of the disclosed compositions. The present invention also relates to a superior method of making these compounds, complexes, compositions that allows one to make compounds/complexes (and thus, compositions) that were previously unattainable.
ISOTOPE PREPARATION METHOD
The present invention provides a method for the purification of .sup.227Th from a mixture comprising .sup.227Th and .sup.223Ra, said method comprising: i) preparing a first solution comprising a mixture of .sup.227Th and .sup.223Ra ions dissolved in an aqueous solution of first mineral acid; ii) loading said first solution onto a strong base anion exchange resin; iii) eluting .sup.223Ra from said strong base anion exchange resin using a second mineral acid in an aqueous solution; iv) optionally rinsing said strong base anion exchange resin using a first aqueous medium; v) eluting .sup.227Th from said strong base anion exchange resin using a third mineral acid in an aqueous solution whereby to generate a second solution comprising .sup.227Th. The invention further provides a purified .sup.227Th solution, a corresponding pharmaceutical formulation and methods of treatment of neoplastic disease.
RADIOACTIVE PROBE FOR DETECTING HYDROGEN SULFIDE
Provided is a probe for detecting in vivo hydrogen sulfide, specifically, a probe for detecting hydrogen sulfide including a complex compound into which a radioactive isotope Cu is introduced. According to specific embodiments of the present disclosure, as a result of real-time observing animal models, in which hydrogen sulfide involved in various diseases is generated in a large quantity, through optical and nuclear medicine imaging, the probe for detecting hydrogen sulfide according to the present disclosure may selectively bind with hydrogen sulfide to provide images of a site where hydrogen sulfide has abnormally increased in a cell or a tissue, thereby detecting a disease in an unexpected site without affecting the anatomical properties of the body. In addition, the probe for detecting hydrogen sulfide quickly reacts with hydrogen sulfide, thereby solving the existing problem of waiting a predetermined time for testing after an imaging agent is injected. Accordingly, the probe may be effectively used as a means for diagnosing diseases, such as a composition for imaging, an imaging method, etc.