Conjugates derived from non-steroidal anti-inflammatory drugs (NSAIDs) and methods of use thereof are disclosed, useful for, inter alia, identifying and localizing the site of pathology and/or inflammation responsible for the sensation of pain in a patient; for identifying the sites of primary, secondary, benign, or malignant tumors; and for diagnosing infection or confirming or ruling out suspected infection. The NSAID-based conjugates contain an imaging moiety. The conjugates concentrate at sites of increased cyclooxygenase expression, thus revealing the sites of increased prostaglandin production, which is correlated with pain and inflammation, and correlated with tumor presence and/or location. Identifying areas of increased COX expressing can also aid in screening for infections.

The invention relates to a method for labeling a target compound with a radiometal by photochemically induced conjugation. Furthermore, a chelating compound for use in said method is provided. The chelating compound is characterized by an arylazide moiety which can be photo-conjugated to a target compound and a chelator moiety which can be radiolabelled. The photo-conjugation and radiolabelling are both performed at basic pH performed in a simultaneous one-pot reaction.

The present application relates to 3-cyclic amine-indole derivatives of general Formula (I), to processes for their preparation, to compositions comprising them and to their use in activation of a serotonin receptor in a cell, as well as to treating diseases, disorders or conditions by activation of a serotonin receptor in a cell. The diseases, disorders or conditions include, for example, psychosis, mental illnesses, and other neurological diseases, disorders and conditions.

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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.

Compounds of the general structure (I), which includes: a radioactive entity, which is a beta-energy emitter that produces Cherenkov radiation, a fluorophore that absorbs electromagnetic radiation of a wavelength λ ranging from 300 nm to 500 nm; a fluorophore which emits electromagnetic radiation of a wavelength λ ranging from 650 nm to 950 nm and/or is a photosensitizer which produces reactive oxygen species ROSs; and a vector entity, which may be present or absent. Also, the use of these compounds for an application for near-infrared Cherenkov luminescence imaging and/or for the treatment of deep biological tissues by Cherenkov dynamic phototherapy.

Excessive deposition of extracellular matrix is a hallmark of Idiopathic pulmonary fibrosis (IPF), it is advantageous to target the cells and the mechanisms associated with this process. By targeting myofibroblasts (specialized contractile fibroblasts) that are key for the development of IPF with drugs conjugated with fibroblast activation protein (FAP), this technology helps minimize the production of extracellular matrix in the lungs and provides a new treatment option for patients diagnosed with IPF.

The present invention provides PC.sub.NHCP pincer metal complexes, which are useful as catalysts in various chemical reactions such as hydrogen isotope exchange (HIE) in C(sp.sup.3)-H and/or C(sp.sup.2)-H bond of an organic compound, e.g., a pharmaceutically active compound; hydroboration of alkynes with excellent selectivity; and alkene isomerization with high stereo- and regioselectivity.

A compound comprising a prostate specific membrane antigen (PSMA)-targeting moiety of the following formula or of a salt or a solvate thereof. R.sup.0 is O or S. Each of R.sup.1a, R.sup.1b and R.sup.1c may be —CO.sub.2H, —SO.sub.2H, —SO.sub.3H, —PO.sub.2H, or —PO.sub.3H.sub.2, for example. R.sup.2 may be methylene or a derivative thereof, propylene or a derivative thereof, or a derivative of ethylene, optionally substituted. R.sup.3 is a linker. When the PSMA-targeting moiety is linked to a radiolabeling group, the compound may be used as an imaging agent or therapeutic agent for PSMA-expressing diseases/conditions.

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An organometallic compound represented by Formula 1:

##STR00001## wherein, in Formula 1, groups and variables are the same as described in the specification.

The invention relates to a method of producing the radiolabeled aryl compound (I) Ar—X, or a salt thereof, wherein X is .sup.211At, .sup.210At, .sup.123I, .sup.124I, .sup.125I, or .sup.131I. The method involves reacting the aryl boronic acid compound (II) Ar—Y, or a salt thereof, wherein Y is a borono group (—B(OH).sub.2) or an ester group thereof, with a radionuclide selected from .sup.211At, .sup.210At, .sup.123I, .sup.124I, .sup.125I and .sup.131I, in the presence of an oxidizing agent selected from an alkali metal iodide, an alkali metal bromide, N-bromosuccinimide, N-chlorosuccinimide and hydrogen peroxide, in water.