Patent classifications
A61K51/0453
PSMA imaging agents
Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.
Contrast agents for myocardial perfusion imaging
The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.
18/19F-labelled compounds which target the prostate specific membrane antigen
This disclosure relates to novel compounds comprising a zwitterionic trifluoroborate prosthetic group which target prostate-specific membrane antigen (PSMA), e.g. in prostate cancer. The compounds have Formula I, wherein each R1 is an anionic group, L is a linker and R2B-F3 is N(R.sup.3).sub.2CH.sub.2BF.sub.3, a pyridinium group substituted with BF.sub.3 or methyl BF.sub.3, or an azole group substituted with methyl BF3. Methods and uses of imaging and treating PSMA-expressing cancers are also disclosed. ##STR00001##
COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS
The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in .sup.18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.
PSMA Imaging Agents
Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.
SELECTIVE LIGANDS FOR TAU AGGREGATES
The invention provides compounds of formula (I) and compositions comprising compounds of formula (I). The invention further provides uses of the compounds of formula (I) and compositions comprising compounds of formula (I), including the use of such compounds for the detection of tau deposits, and the use of such compounds and compositions as diagnostic agents in the diagnosis or monitoring of the progression of a disease or disorder such as Alzheimer's disease or corticobasal degeneration, or for the prevention or treatment of a disease or disorder such as Alzheimer's disease or corticobasal degeneration.
##STR00001##
Radiotracer derivatives of trimethoprim for diagnostic imaging
The present invention provides radiolabeled trimethoprim which are useful in imaging tests such as PET scans. The compounds show robust bacterial uptake in vitro and identify infections from inflammation or tumor when administered to a subject. The compounds show rapid and sensitive detection of Ec DHFR containing tumors from control tumors and background tissue. In one aspect, a compound having the structure of formula (I) is provided or a pharmaceutically acceptable salt or prodrug thereof, wherein R is defined herein. Also provided are compositions containing these compounds, positron emission tomography reporter probe comprising these compounds, and methods of imaging a bacterial infection, tracking or monitoring bacteria, distinguishing a bacterial infection from inflammation or tumor, monitoring genetically fused protein expression, and monitoring genetically engineered cells in clinical scenarios such as immunotherapy for cancer treatment. ##STR00001##
IN VIVO IMAGING OF TUMOR INFILTRATION LEUKOCYTES
The present invention is directed to the use of radiolabeled ligands of leukocyte function-associated antigen1 (LFA1) receptor in order to image and quantify leukocyte activation, recruitment and in vivo trafficking of tumor infiltrating lymphocytes. Diagnostic methods and methods of monitoring cancer therapy, including immunotherapy represent embodiments of the present invention.
Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor4 (PAR4) inhibitors for treating platelet aggregation
The present invention provides thiazole compounds of Formula I ##STR00001##
wherein W, Y, ##STR00002##
R.sup.0, R.sup.2, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
FLUORINE-18 LABELED COMPOSITIONS AND THEIR USE IN IMAGING OF BIOLOGICAL TISSUE
A method for internal imaging of biological tissue in a subject by positron emission tomography (PET) or single photon emission computer tomography (SPECT), the method comprising: (i) administering to a subject an imaging agent that includes, at minimum, at least one fluorine-18 radionuclide bound directly or indirectly to a fluorophore, and (ii) imaging internal biological tissue of the subject by PET or SPECT. In further embodiments, the method includes (i) administering to a subject an imaging agent that includes at least one fluorine-18 radionuclide bound directly or indirectly to a fluorophore, and at least one biological entity (e.g., blood cell, peptide, nucleotide, aptamer, targeting agent, antibody, or antibody fragment) bound directly or indirectly to the fluorophore; and (ii) imaging internal biological tissue of the subject by PET or SPECT. In some embodiments, the method further includes simultaneously imaging the internal biological tissue by fluorescence imaging.