Novel efficient, time-saving and reliable radiofluorination procedures for the production of .sup.18F-labelled active esters via nucleophilic substitution of the corresponding onium precursors with .sup.18F.sup.− are described. The active ester including [.sup.18F]F-Py-TFP and [.sup.18F]TFB produced by one of these methods was used to prepare PSMA-specific PET tracers such as [.sup.18F]DCFPyL. The key advantages of these inventive methods are efficiency, short time of preparation and excellent amenability to automation. A pharmaceutical composition containing at least one PSMA-specific PET tracers prepared by the inventive method is useful for positron emission tomography (PET) imaging, especially imaging prostate tumor.

Provided herein are kallikrein modulating compounds, pharmaceutical compositions comprising the same, and uses thereof.

The present invention provides thieno[2,3-c]pyrrol-4-one compounds that inhibit activity of extracellular-signal-regulated kinase (ERK) and may be useful in the treatment of cancer.

Methods of isotopic labeling are described herein. For example, a method of isotopically labeling an organic compound, in some embodiments, comprises providing a reaction mixture including the organic compound, an iron complex or a cobalt complex and a source of deuterium or tritium. The organic compound is labeled with deuterium or tritium in the presence of the iron complex or cobalt complex or derivative of the iron complex or cobalt complex.

Methods of isotopic labeling are described herein. For example, a method of isotopically labeling an organic compound, in some embodiments, comprises providing a reaction mixture including the organic compound, an iron complex or a cobalt complex and a source of deuterium or tritium. The organic compound is labeled with deuterium or tritium in the presence of the iron complex or cobalt complex or derivative of the iron complex or cobalt complex.

The present invention provides a new chemical process, a new cassette configuration, and new software for the automated production of multiple batches of an [.sup.18F]labelled compound on a single cassette. The invention allows one synthesizer in one hot cell to produce sequentially a plurality of batches of [.sup.18F]-labelled PET tracer in the same day. In particular, the present invention provides a novel arrangement useful for the trapping of [.sup.18F]fluoride and recovery of [.sup.18O]water.

A method for preparing a radiopharmaceutical and, specifically, a method for preparing an organic fluoride-aliphatic compound usable as a radiopharmaceutical, a method for purifying the prepared organic fluoride-aliphatic compound, and a method for preparing a radiopharmaceutical by using a cassette comprising a backdraft preventing reaction container. A method for preparing an organic fluorinated aliphatic compound includes allowing a fluorine salt to react with a leaving group-containing aliphatic compound by using a multifunctional solvent represented by the following Chemical Formula 1 to obtain an aliphatic compound labeled with [.sup.18F] fluoride substituting for the leaving group. The organic fluoride-aliphatic compound can be prepared and purified through even a simple process at high yield, high efficiency, and high purity, and the radiopharmaceutical can be safely prepared without damage to a synthetic apparatus.

The present invention concerns deuterated catecholamine derivatives as well as pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated catecholamine derivatives as well as physiologically acceptable salts thereof, and also pharmaceutical compositions, which contain these compounds, also in combination with enzyme inhibitors, for the treatment of dopamine deficiency diseases or diseases which are based on disrupted tyrosine transport or disrupted tyrosine decarboxylase, as well as other disorders.

The invention relates to substituted pyridine compounds of Formula I: (I) or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein A.sup.1, X, A.sup.2, R.sup.1a, R.sup.1b, R.sup.1c, G, and z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain. ##STR00001##

A method is provided to purify [F-18]FEONM under a high pressure. The synthesis processes of [F-18]FEONM are integrated. An isolation process of non-toxic radio-high performance liquid chromatography (radio-HPLC) is used to purify the crude product. The method integrates a convention [F-18]FDG synthesizer and a novel radio-HPLC system together in a heat chamber. After radiofluorinating the precursor, the reaction product is purified with an alumina solid-phase column in advance to obtain the crude product while fluorine-18 is removed. Then, diphenyl semipreparative HPLC column is used for a final purification. A non-toxic solvent is used for mobile-phase eluting to remove the unreacted precursor and the phase-transfer solvent. The radiofluorination has a reaction yield about 50 percent (%). The method has an uncorrected radiochemical yield of 10˜20%. Both of the radio-HPLC and the radio-thin layer chromatography (radio-TLC) have radiochemical purity higher than 95%.