Patent classifications
A61K51/0453
Half-Curcuminoids as Amyloid-Beta PET Imaging Agents
Provided herein are curcumin analogues that are able to interact with amyloid beta (Aβ) and to attenuate the copper-induced crosslinking of Aβ. 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.
RADIOACTIVE IMIDAZOTHIADIAZOLE DERIVATIVE COMPOUND
The present invention provides a radiolabeled compound represented by the following formula (1), which is a radioactive imidazothiadiazole derivative compound having an affinity for CA-IX, or a salt thereof.
##STR00001##
wherein n is an integer of 1 to 4, and L represents a radionuclide or a mono- to tetravalent group containing a radionuclide.
Compounds useful as imaging agents of hypoxia
The application relates to a compound with the following formula (I): ##STR00001##
its preparation method, its synthesis intermediates and its uses as an imaging agent of hypoxia.
Radioligands for pretargeted pet imaging and methods of their therapeutic use
Described herein are Tz/TCO-based pretargeting strategies using an Al[.sup.18F]-NOTA-labeled tetrazine radioligand. This imaging strategy enables delineation of cancer at earlier time points compared to other imaging strategies and further decreases the radiation dose to healthy tissues compared to directly labeled antibodies. Al-based .sup.18F imaging of small molecules, such as tetrazine, has not been previously achieved due to the decomposition of tetrazine during radiofluorination. Radiofluorination is advantageous over other radiolabeling methods because, in addition to having a shorter half-life, .sup.18F is more readily available to produce and therefore integrated into hospital workflows.
Half-curcuminoids as amyloid-beta PET imaging agents
Provided herein are curcumin analogues that are able to interact with amyloid beta (Aβ) and to attenuate the copper-induced crosslinking of Aβ. 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.
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.
Combination therapies for the treatment of alzheimer's disease and related disorders
The present invention relates to combination therapies for treating Alzheimer's disease or an amyloidosis-associated pathological condition comprising co-administering a therapeutically effective amount of a first compound, and a therapeutically effective amount of a second compound. In certain embodiments, the first compound or the second compound inhibits AB peptide polymerization; is an anti-inflammatory; improves cognitive function, mood, or social behavior; is associated with Tau or alpha-synuclein; or regulates amyloid peptide washout.
COMPOUNDS USEFUL FOR IN VIVO IMAGING OF PROTEIN OXIDATION AND/OR CANCER TREATMENT
Provided herein are compounds of Formula I, Formula II Formula III which are useful in labeling tissues in a subject (e.g., PET imaging of a subject), for treatment of cancer, and/or for preparing a medicament. Also provided are compounds containing a group that is reactive with sulfenylated proteins for treatment of cancer and/or for preparing a medicament. Methods of synthesis of the compounds and precursor compounds are also provided.
Styrylbenzothiazole Derivatives and Uses in Imaging Methods
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.
Deuterium substituted positron emission tomography (PET) imaging agents and their pharmacological application
The present invention relates to deuterated compounds according to Formula I-A, Formula II-A, Formula II-D, and Formula III-A. These compounds can be used as PET imaging agents for evaluating Parkinson's Disease, Alzheimer Disease, and for determining specific serotonin reuptake inhibitor (SSRIi) activity for treatment of depression. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I-A, Formulae II-A, Formula II-D, or Formula III-A, or a pharmaceutically acceptable salt thereof.