Pharmaceutically active benzothiophene compounds and their pharmaceutically acceptable salts and salt mixtures and pharmaceutically acceptable compositions for the treatment of mental disorders or for mental enhancement, including for entactogenic therapy, and generally for modulating central nervous system activity.

Pharmaceutically active benzothiophene compounds and their pharmaceutically acceptable salts and salt mixtures and pharmaceutically acceptable compositions for the treatment of mental disorders or for mental enhancement, including for entactogenic therapy, and generally for modulating central nervous system activity.

The present disclosure provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

The present disclosure provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Disclosed is a method for producing a mono-cross-coupled aromatic compound (3-1) having one less leaving group than an aromatic compound (1) having at least two leaving groups, the method comprising: preparing the aromatic compound (1) having at least two leaving groups; preparing a compound (2) capable of undergoing a cross-coupling reaction selected from an aromatic boronic acid (2-1), an aromatic amino compound (2-2), a diboronic acid ester (2-3), an aromatic compound (2-4) having a hydroxyl group and an aromatic compound (2-5) having a thiol group; and performing a cross-coupling reaction of the aromatic compound (1) having at least two leaving groups with the compound (2) in the presence of a palladium catalyst and a base, in the absence of a solvent.

Disclosed is a method for producing a mono-cross-coupled aromatic compound (3-1) having one less leaving group than an aromatic compound (1) having at least two leaving groups, the method comprising: preparing the aromatic compound (1) having at least two leaving groups; preparing a compound (2) capable of undergoing a cross-coupling reaction selected from an aromatic boronic acid (2-1), an aromatic amino compound (2-2), a diboronic acid ester (2-3), an aromatic compound (2-4) having a hydroxyl group and an aromatic compound (2-5) having a thiol group; and performing a cross-coupling reaction of the aromatic compound (1) having at least two leaving groups with the compound (2) in the presence of a palladium catalyst and a base, in the absence of a solvent.

One or more SGLT2 inhibitors or pharmaceutically acceptable forms thereof are provided for use in the treatment and/or prevention of a metabolic disorder in a feline animal, preferably where the metabolic disorder is one or more selected from the group consisting of ketoacidosis, pre-diabetes, diabetes mellitus type 1 or type 2, insulin resistance, obesity, hyperglycemia, impaired glucose tolerance, hyperinsulinemia, dyslipidemia, dysadipokinemia, subclinical inflammation, systemic inflammation, low grade systemic inflammation, hepatic lipidosis, atherosclerosis, inflammation of the pancreas, neuropathy and/or Syndrome X (metabolic syndrome) and/or loss of pancreatic beta cell function and/or where the remission of the metabolic disorder, preferably diabetic remission, is achieved and/or maintained.

One or more SGLT2 inhibitors or pharmaceutically acceptable forms thereof are provided for use in the treatment and/or prevention of a metabolic disorder in a feline animal, preferably where the metabolic disorder is one or more selected from the group consisting of ketoacidosis, pre-diabetes, diabetes mellitus type 1 or type 2, insulin resistance, obesity, hyperglycemia, impaired glucose tolerance, hyperinsulinemia, dyslipidemia, dysadipokinemia, subclinical inflammation, systemic inflammation, low grade systemic inflammation, hepatic lipidosis, atherosclerosis, inflammation of the pancreas, neuropathy and/or Syndrome X (metabolic syndrome) and/or loss of pancreatic beta cell function and/or where the remission of the metabolic disorder, preferably diabetic remission, is achieved and/or maintained.

A process is disclosed for the preparation of a compound of formula

##STR00001##

and/or an addition salt of a proton acid, wherein R.sup.1 and R.sup.2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each aryl or aralkyl being optionally further substituted with alkyl, alkoxy and/or halogen.

A process is disclosed for the preparation of a compound of formula

##STR00001##

and/or an addition salt of a proton acid, wherein R.sup.1 and R.sup.2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each aryl or aralkyl being optionally further substituted with alkyl, alkoxy and/or halogen.