There are provided, inter alia, compositions and methods for covalently binding peptides to proteins.

A process for the preparation of a class of molecules, namely bicyclo[1.1.1]pentanes and derivatives thereof by reaction of [1.1.1]propellane with a variety of reagents under irradiation and/or in the presence of radical initiators to obtain bicyclo[1.1.1]pentanes asymmetrically substituted at position 1 and 3, which are useful as intermediates for the preparation of asymmetrically 1,3-disubstituted bicyclo[1.1.1]pentane derivatives and various physiologically active substances or materials containing these structures.

A process for the preparation of a class of molecules, namely bicyclo[1.1.1]pentanes and derivatives thereof by reaction of [1.1.1]propellane with a variety of reagents under irradiation and/or in the presence of radical initiators to obtain bicyclo[1.1.1]pentanes asymmetrically substituted at position 1 and 3, which are useful as intermediates for the preparation of asymmetrically 1,3-disubstituted bicyclo[1.1.1]pentane derivatives and various physiologically active substances or materials containing these structures.

A process for the preparation of a class of molecules, namely bicyclo[1.1.1]pentanes and derivatives thereof by reaction of [1.1.1]propellane with a variety of reagents under irradiation and/or in the presence of radical initiators to obtain bicyclo[1.1.1]pentanes asymmetrically substituted at position 1 and 3, which are useful as intermediates for the preparation of asymmetrically 1,3-disubstituted bicyclo[1.1.1]pentane derivatives and various physiologically active substances or materials containing these structures.

Provided herein are fatty acid amide (FAAH) cleavable prodrugs of thyromimetics and pharmaceutical compositions comprising these compounds with at least one pharmaceutically acceptable excipient further comprising a peripherally restricted FAAH inhibitor.

Provided herein are fatty acid amide (FAAH) cleavable prodrugs of thyromimetics and pharmaceutical compositions comprising these compounds with at least one pharmaceutically acceptable excipient further comprising a peripherally restricted FAAH inhibitor.

The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

The invention concerns a method for preparing an oxysulphide and fluorinated derivative, said method comprising the reacting, in the presence of an organic solvent, of: i) at least one compound of formula Ea-COOR (I), in which Ea represents the fluorine atom or a group having 1 to 10 carbon atoms chosen from fluoroalkyls, perfluoroalkyls and fluoroalkenyls and R represents hydrogen, a monovalent cation or an alkyl group, and ii) a sulphur oxide, said method being such that the initial molar ratio (sulphur oxide/compound of formula (I)) is less than 0.4 and the concentration of sulphur oxide dissolved in the reaction medium is kept constant for the entire duration of the reaction to a value of between 0.2% and 3% by weight by means of continually adding said sulphur oxide to the reaction medium.

The invention concerns a method for preparing an oxysulphide and fluorinated derivative, said method comprising the reacting, in the presence of an organic solvent, of: i) at least one compound of formula Ea-COOR (I), in which Ea represents the fluorine atom or a group having 1 to 10 carbon atoms chosen from fluoroalkyls, perfluoroalkyls and fluoroalkenyls and R represents hydrogen, a monovalent cation or an alkyl group, and ii) a sulphur oxide, said method being such that the initial molar ratio (sulphur oxide/compound of formula (I)) is less than 0.4 and the concentration of sulphur oxide dissolved in the reaction medium is kept constant for the entire duration of the reaction to a value of between 0.2% and 3% by weight by means of continually adding said sulphur oxide to the reaction medium.