A61K51/0453

COMPOSITIONS AND METHODS FOR THE TREATMENT AND IMAGING OF CANCER
20210228747 · 2021-07-29 ·

Compositions and methods for treating, detecting, and diagnosing cancer are disclosed.

Organomedicinals for imaging and treatment of neurodegenerative disorders

Provided herein are compounds for the imaging and treatment of TDP43-mediated disorders. The compounds disclosed bind TDP43 aggregates and may be used to diagnose and treat amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD).

Imaging of meningiomas using phenylbenzothiazole, stilbene, or biphenylalkyne derivatives

Methods for detecting or ruling out a meningioma in a patient using a phenylbenzothiazole derivative or a stilbene derivative or a biphenylalkyne derivative, and a medical imaging technique such as positron emission tomography/computed tomography are disclosed. In one version of the method, the stilbene derivative is a compound of formula (X): ##STR00001##

Radiotracer Derivatives Of Trimethoprim For Diagnostic Imaging
20210138093 · 2021-05-13 ·

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##

PSMA targeted fluorescent agents for image guided surgery

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

HSP90-TARGETING CONJUGATES AND FORMULATIONS THEREOF

Conjugates of an active agent attached to a targeting moiety, such as at least one HSP90 binding moiety, via a linker, have been designed. Such conjugates can provide improved temporospatial delivery of the active agent, improved biodistribution and penetration in tumor, and/or decreased toxicity. Methods of making the conjugates and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer.

Styrylbenzothiazole derivatives and uses in imaging methods
11844846 · 2023-12-19 · ·

This disclosure relates to styrylbenzothiazole derivatives for use as in vivo imaging agents for the diagnosis of Parkinson's disease (PD) or other degenerative disorders or conditions of the central nervous system. Early diagnosis is particularly advantageous as neuroprotective treatment can be applied to healthy neural cells to delay or even prevent the onset of debilitating clinical symptoms.

RADIOLIGANDS FOR MYELIN
20210128756 · 2021-05-06 ·

A radioligand for labeling myelin includes a fluorescent trans-stilbene derivative.

Tricarbonyl complexes of transition metals with benzo-heterocyclic derivatives of the cyclopentadienyl anion

Complex compounds of transition metals according to formula (1) wherein the M(CO).sub.3.sup.+ tricarbonyl-metal core forms a complex with the cyclopentadienyl anion linked to heterocyclic moieties of the benzothiazole, benzimidazole and benzoxazole families. The compounds exhibit high blood-brain barrier permeability and can be used in the diagnosis and/or treatment of diseases of the Central Nervous System. ##STR00001##

11C -labeled 06 -benzylguanine, pet probe capable of visualizing 06-methyl guanine methyl-transferase activity, and production method of the same

An object of the invention is to provide a .sup.11C-labeled O.sup.6-benzylguanine capable of obtaining a PET image and a process for producing the same. The .sup.11C-labeled O.sup.6-benzylguanine of the invention is represented by the following chemical formula (a). ##STR00001##
The .sup.11C-labeled O.sup.6-benzylguanine is produced by: a coupling step of cross-coupling a methyl iodide labeled with .sup.11C and the following organotin compound (b) (R.sup.1 represents an alkyl group, and R.sup.2 and R.sup.3 represent a leaving group which can be eliminated with a base) in the presence of a palladium complex, a phosphine ligand, and cuprous halide in an aprotic lactam; and a desorption step of desorbing the leaving groups R.sup.2 and R.sup.3 of the coupling product obtained by the coupling step with a base. ##STR00002##