Patent classifications
A61K51/04
Triazine based radiopharmaceuticals and radioimaging agents
Metal complexes including a radionuclide and a compound of Formula I and Formula II are potent inhibitors of PSMA. ##STR00001##
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.
PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) LIGANDS AND USES THEREOF
The present disclosure relates to prostate specific membrane antigen (PSMA) ligands. In particular, the disclosure relates to PSMA ligands having a glutamate-urea-lysine (GUL) moiety and a chelating agent that can comprise a radiometal. The disclosure also relates to the use of these compounds in imaging and in the treatment of prostate cancer.
POSITRON IMAGING TOMOGRAPHY IMAGING AGENT COMPOSITION AND METHOD FOR DETECTION OF BACTERIAL INFECTION
This invention provides a composition comprising the compound having the structure:
##STR00001##
ethyl 2-[.sup.19F]F-4-nitrobenzoate, and at least one acceptable carrier.
This invention also provides a method of detecting the presence of or location of bacteria cells in a subject which comprises determining if an amount of the compound or determining where an amount of the compound having the structure:
##STR00002##
is present in the subject at a period of time after administration of the compound or salt thereof to the subject, thereby detecting the presence of or location of the bacteria cells based on the amount of the compound determined to be present in the subject or detecting the location of the bacteria cells based on the location of the compound determined to be present in the subject.
POSITRON IMAGING TOMOGRAPHY IMAGING AGENT COMPOSITION AND METHOD FOR DETECTION OF BACTERIAL INFECTION
This invention provides a composition comprising the compound having the structure:
##STR00001##
ethyl 2-[.sup.19F]F-4-nitrobenzoate, and at least one acceptable carrier.
This invention also provides a method of detecting the presence of or location of bacteria cells in a subject which comprises determining if an amount of the compound or determining where an amount of the compound having the structure:
##STR00002##
is present in the subject at a period of time after administration of the compound or salt thereof to the subject, thereby detecting the presence of or location of the bacteria cells based on the amount of the compound determined to be present in the subject or detecting the location of the bacteria cells based on the location of the compound determined to be present in the subject.
Granzyme B directed imaging and therapy
Provided herein are compounds useful for imaging granzyme B. An exemplary compound provided herein is useful as a radiotracer for position emission tomography (PET) and/or single photon emission tomography (SPECT) imaging. Methods of imaging granzyme B, combination therapies, and kits comprising the granzyme B imaging agents are also provided.
THIOPURINE-BASED COMPOUND, COMPOSITION, METHOD OF PREPARATION AND APPLICATIONS
A compound for measurement of thiopurine pathway directed systems imaging and therapy including a chelator and a thiopurine ligand is provided. A method of synthesizing the compound is also provided, and the compound may be further prepared in pharmaceutical formulations or kits for therapy or molecular imaging.
Semi-synthetic tissue constructs for tissue regeneration
Methods and compositions for tissue regeneration of the present invention include a biocompatible porous composite of a decellularized tissue and an aptamer-functionalized hydrogel, wherein the aptamers of the aptamer-functionalized hydrogel specifically and reversibly bind to an active agent.
Ultrasmall nanoparticles labeled with Zirconium-89 and methods thereof
Described herein are nanoprobes comprising ultrasmall aminated and cRGDY-conjugated nanoparticles labeled with Zirconium-89 (.sup.89Zr) and methods of their use. The provided compositions are renally clearable and possess suitable blood circulation half-time, high tumor active targeting capability, dominant renal clearance, low liver accumulation, and a high tumor-to-background ratio. The described nanoprobes exhibit great potential as “target-or-clear” tracers to human subjects for systemic targeted imaging (or treatment) of cancer.
DAZA chelators as ligands in liver imaging
The invention relates to compounds according to the general formula (I) or a pharmaceutically acceptable salt of an inorganic or organic acid, a hydrate, a stereoisomer or a solvate thereof, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 and R.sup.12 being selected independently of one another from hydrogen and alkoxy. The compounds of formula (I) as ligands are suitable for the production of radioactively labelled .sup.68Ga, .sup.64Cu, .sup.67Ga, .sup.111In or .sup.99mTc complexes. The invention further relates to a method for producing the compounds of formula (I) and the radioactively labelled complexes and to the use of the radioactively labelled complexes in imaging methods, such as PET/CT, in particular of the liver.