Patent classifications
A61K51/0478
DOUBLE-LABELED PROBE FOR MOLECULAR IMAGING AND USE THEREOF
The present invention relates to a compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising: A compound or a pharmaceutically acceptable salt thereof of formula (I): (A)-x.sub.1-(B)-x.sub.2-(C), wherein (A) is at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; (C) a dye moiety; x.sub.1 is a spacer covalently connecting (A) and (B); x.sub.2 is a spacer or a chemical single bond connecting (B) and (C); wherein (C) has the formula
##STR00001##
wherein R.sup.1 to R.sup.4, R.sup.9, a, b, Y and X.sup.1 to X.sup.4 have the meaning as indicated in the claims and description. The invention further relates to compositions comprising said compounds as well as a method for detecting neoplastic cells in a sample in vitro with the aid of the compounds or composition.
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.
.SUP.99m.Tc-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.
Multinuclear complexes and their preparation
Multinuclear complexes and methods for preparing them are provided. The discrete multinuclear complexes include a one or more transition metals and a radioisotope having the same coordination geometry as the transition metal. A bridging ligand is coordinated to the transition metal and the radioisotope to link the transition metal and the radioisotope and pendent ligands are coordinated to each of the transition metal and the radioisotope to stabilise the complex. The multinuclear complexes may include a radioisotope or radioelement that can be detected by medical equipment and may find use in therapy and/or the diagnosis of disease in patients.
Methods for cell labeling and medical imaging
Methods of ex vivo labeling of a biological material for in vivo imaging, methods of labeling a biological material in vivo, methods for preparing a labeling agent, and methods for in vivo imaging of a subject using a biological material labeled with a labeling agent are disclosed. In one non-limiting example, the biological material is selected from cells and the labeling agent is a .sup.89Zr-Desferrioxamine-NCS labeling agent.
NANOPARTICLE IMMUNOCONJUGATES
Disclosed herein are nanoparticle immunoconjugates useful for therapeutics and/or diagnostics. The immunoconjugates have diameter (e.g., average diameter) no greater than 20 nanometers (e.g., as measured by dynamic light scattering (DLS) in aqueous solution, e.g., saline solution). In certain embodiments, the conjugates are silica-based nanoparticles with single chain antibody fragments attached thereto.
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.
LABELING PRECURSORS WITH SQUARIC ACID COUPLING
The invention relates to a marking precursor incorporating a chelator or fluorination group for radiolabelling with .sup.44Sc, .sup.47Sc, .sup.55Co, .sup.62Cu, .sup.64Cu, .sup.67Cu, .sup.66Ga, .sup.67Ga, .sup.68Ga, .sup.89Zr, .sup.86Y, .sup.90Y, .sup.90Nb, .sup.99mTc, .sup.111In, .sup.135Sm, .sup.140Pr, .sup.159Gd, .sup.149Tb, .sup.160Tb, .sup.161Tb, .sup.165Er, .sup.166Dy, .sup.166Ho, .sup.175Yb, .sup.177Lu, .sup.186Re, .sup.188Re, .sup.213Bi and .sup.225Ac or with .sup.18F, .sup.131I or .sup.211At, and one or two biological targeting vectors which are coupled to the chelator or fluorinating group via one or more squaric acid groups.
Pharmaceutical compositions of sulfur colloid and processes thereof
The present invention relates to stable pharmaceutical compositions of sulfur colloid, which advantageously provide a high radiochemical purity to .sup.99mTc-pertechnetate without causing the gel formation. The compositions include pre-lyophilized and lyophilized compositions of sulfur colloid. It also relates to a non-radioactive kit which upon reconstitution with .sup.99mTc-pertechnetate solution gives stabilized .sup.99mmTc-Sulfur colloid radiopharmaceutical composition. Further, the process for preparation of said compositions and their use for diagnostic purposes are also disclosed.
TARGETED RADIOPHARMACEUTICALS FOR THE DIAGNOSIS AND TREATMENT OF PROSTATE CANCER
- Niels BÖHNKE ,
- Sabine ZITZMANN-KOLBE ,
- Stefanie Hammer ,
- Sven Wittrock ,
- Donald Bierer ,
- Thorsten POETHKO ,
- Hans Briem ,
- Holger Magnus STEUBER ,
- Martina SCHÄFER ,
- Robin Michael MEIER ,
- Arif CELIK ,
- Cornelia Preusse ,
- Antje Rottmann ,
- Nicolas Werbeck ,
- Alexander KRISTIAN ,
- Bård INDREVOLL ,
- Alan Cuthbertson ,
- Alex PAPPLE
A compound of general formula (I): wherein: n is 1, 2 or 3; R1, R2, R3 and R4, independently represent OH or Q; and 20 Q represents a tissue-targeting moeity selected from the group consisting of or a stereoisomer, a hydrate, a solvate, or a salt thereof, or a mixture of same, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said 25 compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of soft tissue diseases, as a sole agent or in combination with other active ingredients.
##STR00001##