The present invention provides compounds of Formula (I) or Formula (II): ##STR00001##
pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.

Compounds of general formula (I) wherein (I) RI-R4 are each independently selected from H and deuterium; and at least one of RI-R4 is deuterium. The compounds have been found to be particularly useful for treating neurodegenerative conditions and in particular but not exclusively conditions such as motor neurone disease.

The invention relates to a process for producing a compound comprising an .sup.18F-difluoromethyl group or a compound comprising an .sup.18F-difluoromethylene group, which process comprises contacting a compound comprising a nucleophilic group with .sup.18F-difluorocarbene. The invention also relates to a compound of Formula (I). Compounds comprising an .sup.18F-difluoromethyl group or an .sup.18F-difluoromethylene group are also the subject of the present invention.

A compound represented by formula I, a racemate, a stereoisomer, a tautomer, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof are provided. In formula I, R.sub.2 and R.sub.4 are independently selected from H or D, respectively; R.sub.1 and R.sub.3 are independently selected from CH.sub.3, CH.sub.2D, CHD.sub.2 or CD.sub.3, respectively; and the compound of formula I contains at least one deuterium atom. While retaining the pharmacological activity of the allopregnanolone, an allopregnanolone derivative that is suitable for oral administration is obtained by means of the structural modification on the hydroxyl group of the allopregnanolone.

##STR00001##

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.

Disclosed are deuterated chenodeoxycholic acid derivatives and pharmaceutical compositions containing the deuterated chenodeoxycholic acid derivatives. In particular, disclosed is a deuterated chenodeoxycholic acid derivative of formula (I), or a crystal form, pharmaceutically acceptable salt, hydrate or solvate thereof, and a pharmaceutical composition containing the same. The deuterated chenodeoxycholic acid derivatives of formula (I) can be used to treat and/or prevent diseases related to the farnesoid X receptor (FXR) and/or G-protein coupled bile acid receptor, such as nonalcoholic steatohepatitis, nonalcoholic fatty liver diseases, gallstones, primary biliary cirrhosis, and cirrhosis.

The present invention relates to a method for the synthesis of a radioactive agent composition comprising at least a purification step carried out in the presence of an antioxidant, to the composition obtained by this method comprising radioactive agent and excipient, and to the method for preventing radiolysis of radioactive agent composition comprising the synthesis of said radioactive agent according to the method of the invention.

Deuterated compounds are provided according to Formula (I): Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. These compounds are contemplated as useful for the prevention and treatment of a variety of CNS-related conditions.

##STR00001##

The present invention relates to a method for synthesizing a radiopharmaceutical using a cartridge, which makes it possible to carry out several steps of reaction required for synthesizing a radiopharmaceutical in the cartridge filled with a polymer. A method for synthesizing a radiopharmaceutical according to the present invention enables each step's reaction to be carried out with the solution confined in the cartridge so as not to flow out, thus being simplified compared to the conventional methods for synthesizing radiopharmaceuticals, and expediting the synthesis thereof.

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 radiolabelling process.