Patent classifications
A61K51/0478
Development of neurokinin-1 receptor-binding agent delivery conjugates
Neurokinin-1 (NK-1) receptor-binding agent delivery conjugates, compositions comprising NK-1 receptor-binding agent delivery conjugates, and methods for making and administering NK-1 receptor-binding agent delivery conjugates are provided. A conjugate may include an NK-1 receptor-binding moiety, a linker group containing at least one linker selected from the group of a releasable linker and a spacer linker, and an active agent linked to the linker group. The active agent may be selected from the group of fluorophore-containing compounds, radionuclide-containing compounds, and therapeutic agents for treatment of tumor cells characterized by over-expression of the NK-1 receptor.
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.
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 β-amyloid in the patient, and acquiring an image to detect the presence or absence of β-amyloid in the patient. A method for detecting or ruling out cancer 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 tissue in the patient; and acquiring an image using a medical imaging technique to detect zinc distribution in tissue in the patient.
LUTEINIZING HORMONE-RELEASING HORMONE RECEPTOR (LHRH-R) CONJUGATES AND USES THEREOF
The present teachings relate generally to conjugates and methods for imaging a tumor microenvironment in a patient, and to conjugates and methods for treating LHRH-R expressing cancer in a patient. The present teachings relate generally to method of making conjugates comprising an LHRH-R antagonist.
SOLUTION COMPRISING FLUORESCENT DYE AS FIDUCIAL MARKER
The present disclosure relates to a solution comprising a water insoluble carbohydrate and a fluorescent dye, such as a near infrared (NIR) contrast agent, wherein the solution sets under aqueous conditions, such as in vivo, to form e.g. a gel, a glass, a semi-solid, a solid, a crystal or any mixtures thereof. The disclosure further relates to preparation of such solution and use of such solution for in vivo imaging and/or guidance of surgery or interventional therapeutic procedures.
Multidentate bifunctional chelating agents for radionuclide complexation in diagnostics and therapy
The invention relates to octadentate ligands of a general formula R.sup.1-D-X-D-X-D-X-D-E-R.sup.2, wherein D is C(O)N(OH) or N(OH)C(O), pyrimidinone or pyridinone, each X independently of any other X is a saturated or partially unsaturated, substituted or unsubstituted linker comprising 8-11 atoms selected from any of N, C, O; R.sup.1 is alkyl, cycloalkyl, arene, or heteroarene, E is a saturated or partially unsaturated, substituted or unsubstituted chain comprising 1-50 atoms and R.sup.2 is a moiety capable of selectively binding to a biomolecule, or a nanoparticle. The invention further relates to complexes of the ligand, particularly radionuclides and their use in radioimmunotherapy and imaging.
99MTC-EDDA/HYNIC-IPSMA AS A RADIOPHARMACEUTICAL FOR DETECTING THE OVEREXPRESSION OF PROSTATE-SPECIFIC MEMBRANE ANTIGEN
The invention relates to a novel radiopharmaceutical that inhibits the prostate-specific membrane antigen (iPSMA), containing hydrazinonicotinamide (HYNIC) as a critical chemical group in increasing in the lipophilicity of the molecule for binding to the hydrophobic sites of the PSMA, combined with the conventional use of HYNIC as a chelating agent for radiometal .sup.99mTc, in which the ethylenediaminetetraacetic acid (EDDA) is used to complete the coordination sphere of the radiometal. The novel radiopharmaceutical .sup.99mTc-EDDA/HYNIC-iPSMA detects, with high affinity and sensitivity in vivo, the overexpressed PSMA protein in prostate cancer cells using SPECT molecular imaging techniques in nuclear medicine. The aim of the invention is to provide a novel specific radiopharmaceutical (radiopharmaceutical for molecular targets) for SPECT, with high sensitivity for the detection of tumours with overexpression of PSMA.
COMPOSITION FOR DETECTING HYDROGEN SULFIDE OR MEASURING HYDROGEN SULFIDE CONCENTRATION AND COMPOSITION COMPRISING SAME AS EFFECTIVE INGREDIENT FOR DIAGNOSING OR IMAGING IN VIVO INFLAMMATION, TISSUES HAVING HYPOXIC DAMAGE, OR CANCER
The present invention relates to a composition for detecting hydrogen sulfide or measuring a concentration of hydrogen sulfide, and a composition comprising same as an effective ingredient for diagnosing or imaging in vivo inflammation, tissues having hypoxic damage, or cancer. The composition for detecting hydrogen sulfide or measuring a concentration of hydrogen sulfide according to the present invention, which comprises the compound represented by formula 1 (.sup.99mTc-alpha-hydroxy acid) having alpha-hydroxy acid labeled with .sup.99mTc, enables the detection or concentration measurement of hydrogen sulfide in in-vitro and in-vivo levels and, as such, can be advantageously used for detecting hydrogen sulfide and measuring a concentration of hydrogen sulfide and furthermore for discovering biological roles of hydrogen sulfide in vivo, especially, for detecting, imaging, and quantitatively measuring hydrogen sulfide in a disease selected from the group consisting of angiogenesis, inflammation, cancer, Alzheimer's disease, cardiovascular ischemia, and cerebrovascular ischemia, or in hypoxic tissues.
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.
PHARMACEUTICAL COMPOSITION COMPRISING TETROFOSMIN AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
The present invention relates to a stable pharmaceutical composition of tetrofosmin or pharmaceutically acceptable salts thereof. It also relates to a lyophilized non-radioactive kit which upon reconstitution with .sup.99mTc-pertechnetate solution gives a stable .sup.99mTc-tetrofosmin radiopharmaceutical composition. It also provides process for the preparation of said radiopharmaceutical compositions and their use in diagnostic imaging procedures. The compositions provide desirable technical attributes such as stability, high radiochemical purity (RCP) and desired bio-distribution.