A61K51/0453

Half-Curcuminoids as Amyloid-Beta PET Imaging Agents
20190255198 · 2019-08-22 ·

Provided herein are curcumin analogues that are able to interact with amyloid beta (A) and to attenuate the copper-induced crosslinking of A. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.

METHODS FOR TREATMENT OF CANCERS
20240165280 · 2024-05-23 ·

The present disclosure relates to methods of treating a subject having cancer with an .sup.225Ac-radiopharmaceutical, which comprises .sup.225Ac chelated with a compound of Formula I:

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wherein the compound binds to neurotensin receptor 1 (NTSR1) and does not cross the blood-brain barrier, and wherein the .sup.225Ac-radiopharmaceutical is administered at a dosage of less than 10 MBq/kg of body weight of the subject or is administered as a unitary dosage of less than 40 MBq to the subject.

TRIAZOLE CONJUGATED UREAS, THIOUREAS, CARBAMATES, AND REVERSED CARBAMATES FOR PSMA-TARGETED IMAGING AGENTS AND USES THEREOF

Triazole conjugated urea-based and thiourea-based scaffolds that have high binding affinity to PSMA are disclosed. These scaffolds can be radiolabeled and used to image cells and tumors that express PSMA. Methods of synthesizing radiofluorinated triazole conjugated urea-based and thiourea-based scaffolds also are disclosed.

Detection of Renal Amyloidosis by Imaging with Stilbene or Phenylbenzothiazole Derivatives

A method for detecting or ruling out renal amyloidosis in a subject is disclosed. The use of a stilbene derivative, such as florbetapir .sup.18F, or a phenylbenzothiazole derivative in positron emission tomography imaging, or integrated positron emission tomography/computed tomography imaging, can serve as a screening test for renal amyloidosis in a subject.

COMPOSITIONS FOR RADIOTHERAPY AND USES THEREOF
20190216956 · 2019-07-18 ·

Provided herein are kits, compositions, and methods for treatment of a disease, disorder, or condition, such as a proliferative disease, disorder, or condition. One aspect provides a composition including a radioisotope and a substrate. Another aspect provides methods for treating a disease, disorder, or condition.

Molecular probes for imaging myelin

A molecular probe for use in the detection of myelin in a subject includes a compound having the general formula selected from the group consisting of: formula (I), and pharmaceutically acceptable salts thereof. ##STR00001##

Heterocyclic molecules for biomedical imaging and therapeutic applications

Probes which target diffuse and fibrillar forms of amyloid beta (A) are described. These probes demonstrate high initial brain penetration and facile clearance from non-targeted regions. The agents can be used to image amyloid quantitatively for monitoring efficacy of A-modifying therapeutics and assist in premortem diagnosis of Alzheimer's disease (AD). Disclosed probes can bind A aggregates of preformed A.sub.1-42 fibrils in vitro and can be used to image fibrillar and diffuse plaques ex vivo in brain sections. Disclosed probes can be used to determine A burden in early stages of AD. These probes can be used for multimodality imaging of A. F-AI-187 (1 M) can detect A plaques in brain sections of APP/PS1 mice. F-AI-187 (10 M) can detect A plaques in the frontal lobe in a brain section of a patient with confirmed AD. Some probes can be used for fluorescence imaging of plaque.

NUCLEAR IMAGING AND RADIOTHERAPEUTICS AGENTS TARGETING CARBONIC ANHYDRASE IX AND USES THEREOF

Highly potent and selective radionuclide-based imaging and therapy agents targeting carbonic anhydrase IX with minimum non-specific organ uptake are disclosed. Methods of imaging and/or treating carbonic anhydrase IX-expressing cells or tumors also are disclosed.

Compounds binding to neuropathological aggregates

The present invention provides compounds binding to neuropathological aggregates of peptides or proteins, including aggregates such as neurofibrillary tangles (NFTs), osynuclein aggregates and other amyloid aggregates. The compounds of the present invention are useful for the detection and/or diagnosis of disorders associated with such neuropathological aggregates. In further aspects, the invention provides diagnostic compositions comprising these compounds, and methods for the preparation of radiolabeled compound from non-radiolabeled precursors.

RADIOFLUORINATED CARBOXIMIDAMIDES AS IDO TARGETING PET TRACER FOR CANCER IMAGING
20190185439 · 2019-06-20 ·

Radiofluorinated carboximidamides are disclosed as selective IDO enzyme radioligands and generate specific binding in accordance with IDO expression in vitro. MicroPET experiments indicate [.sup.18F]IDO49 specifically accumulate in IDO-expressing tumors which confirmed by Western blot and IHC analysis supported. Using Hela tumor bearing models with IFN- treatment confirmed that [.sup.18F]IDO49 accumulation in the IFN- treatment tumor mouse. These results can have implications that [.sup.18F]IDO49 has substantial potential as an imaging agent that targets IDO in tumors.