A61K51/0463

HETEROCYCLIC COMPOUNDS FOR CANCER IMAGING AND TREATMENT AND METHODS FOR THEIR USE

Compounds having a structure of Formula I:

##STR00001##

or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, X, n.sup.1, n.sup.2, and n.sup.3 are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

METHOD FOR PREPARING AN [18F] RADIOLABELLED COMPOUND WITH LOW WATER CONTENT DURING LABELLING STEP

The invention relates to a method of preparing an [.sup.18F] radio-labelled compound, wherein the water content is controlled. Controlling the water content and the origin of the water within the reaction process has a significant effect on both the yield and the purity of the product of the radio-labelling process.

INHIBITOR OF PROSTATE SPECIFIC MEMBRANE ANTIGEN AND PHARMACEUTICAL USE THEREOF

An inhibitor of a prostate specific membrane antigen and a pharmaceutical use thereof. Specifically, the present solution belongs to the field of radiopharmaceuticals and relates to a compound represented by formula (IV) or a pharmaceutically acceptable salt thereof.

##STR00001##

9H-PYRROLO-DIPYRIDINE DERIVATIVES

The invention relates to 9H-pyrrolo-dipyridine derivatives of formula I, processes for preparing them, pharmaceutical compositions containing them and their use as radiopharmaceuticals in particular as imaging agents for the detection of Tau aggregates.

##STR00001##

Tau imaging probe

An object of the present invention is to provide a probe for imaging a -sheet structure protein which can be used for the diagnosis of conformational diseases, particularly disease (tauopathy) having a cardinal symptom such as intracerebral accumulation of tau protein, for example, Alzheimer's disease. Another object of the present invention is to provide a compound which is highly specific to tau and can image tau with satisfactory sensitivity, and also has high brain transition, low or non-recognized bone-seeking properties and low or non-recognized toxicity. According to the present invention, the above problems are solved by providing a compound of a formula I (wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.a and R.sup.b are as defined in the present description) or a pharmaceutically acceptable salt or solvate thereof.

ALPHA-SYNUCLEIN LIGANDS
20170189566 · 2017-07-06 · ·

The present invention generally relates to various compounds that are useful as -synuclein ligands. The invention further relates to methods of using these compounds and their radiolabeled analogs for the detection of synucleinopathies, including Parkinson's disease (PD).

Novel Tricyclic Modulators of Cannabinoid Receptors
20170096426 · 2017-04-06 ·

The compounds of the invention are modulators of cannabinoid receptors CB1 or CB2. The compounds can be used for the prevention or treatment of, e.g., pain, cancer, skin diseases, weight-associated disorders, chemical addictions, psychiatric disorders, neurodegenerative disorders, bone diseases, and inflammatory diseases. The compounds of the invention can further be used to study these diseases and disorders, as well as cannabinoid receptor biology, by coupling the compounds to, e.g., imaging agents.

Probes for imaging huntingtin protein

Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use. ##STR00001##

Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer

The present technology provides compounds as well as compositions including such compounds useful in targeted radiotherapy of cancer and/or mammalian tissue overexpressing prostate specific membrane antigen (PSMA) where the compounds are represented by the following: ##STR00001## or a pharmaceutically acceptable salt thereof, ##STR00002## or a pharmaceutically acceptable salt thereof, ##STR00003## or a pharmaceutically acceptable salt thereof,
wherein M.sup.1 is independently at each occurrence an alpha-emitting radionuclide. Equivalents of such compounds are also disclosed.

AROMATIC VINYL COMPOUND, METAL COMPLEX THEREOF, AND PREPARATION METHOD THEREFOR AND USE THEREOF
20250073358 · 2025-03-06 ·

Provided are an aromatic vinyl compound, a metal complex thereof, and a preparation method therefor and the use thereof. The aromatic vinyl compound and the metal complex thereof have an inhibitory activity on the binding of PD-1/PD-L1, and therefore the aromatic vinyl compound and the metal complex thereof can be used for treating related diseases such as tumors. In addition, the obtained metal complex can also be used as an imaging agent.

##STR00001##