The new method of preparing 1-(2-(2,4-di-methylphenylsulphanyl)pheny!)piperazine of formula (I) or its salt comprises a reaction of 2-(2,4-dimethylphenyl-sulphanyl)benzeneamine of formula (XI), wherein Me is methyl, with a suitable precursor of formation of piperazine ring of formula (X11), wherein LG is a leaving group and R is hydrogen or a protective group, in a suitable organic solvent, wherein the reaction is carried out without presence of a base in a neutral or acidic environment.

##STR00001##

The invention provides compounds represented by the general formula I ##STR00001##
wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.

The invention provides compounds represented by the general formula I ##STR00001##
wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.

A compound selected from 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-sulfanyl)-acetyl]-12-epi-mutilins, or 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-oxy)-acetyl]-12-epi-mutilins, wherein 12-epi-mutilin is characterized in that the mutilin ring at position 12 is substituted by two substituents, the first substituent at position 12 of the mutilin ring is a methyl group which methyl group has the inverse stereochemistry compared with the stereochemistry of the methyl group at position 12 of the naturally occurring pleuromutilin ring, the second substituent at position 12 of the mutilin ring is a hydrocarbon group comprising at least one nitrogen atom and all other substituents of the mutilin ring having the same stereochemistry compared with the stereochemistry of the substituents at the corresponding positions in the naturally occurring pleuromutilin ring; optionally in the form of a salt and/or solvate, wherein the naturally occurring pleuromutilin is of formula ##STR00001##
processes for the preparation of such compounds and their use as pharmaceuticals.

A compound selected from 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-sulfanyl)-acetyl]-12-epi-mutilins, or 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-oxy)-acetyl]-12-epi-mutilins, wherein 12-epi-mutilin is characterized in that the mutilin ring at position 12 is substituted by two substituents, the first substituent at position 12 of the mutilin ring is a methyl group which methyl group has the inverse stereochemistry compared with the stereochemistry of the methyl group at position 12 of the naturally occurring pleuromutilin ring, the second substituent at position 12 of the mutilin ring is a hydrocarbon group comprising at least one nitrogen atom and all other substituents of the mutilin ring having the same stereochemistry compared with the stereochemistry of the substituents at the corresponding positions in the naturally occurring pleuromutilin ring; optionally in the form of a salt and/or solvate, wherein the naturally occurring pleuromutilin is of formula ##STR00001##
processes for the preparation of such compounds and their use as pharmaceuticals.

The invention provides compounds having the general Formula (I); and pharmaceutically acceptable salts thereof; wherein the variables R.sup.A, R.sup.AA, subscript n, subscript q, ring A, X.sup.2, L, subscript m, X.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, D and E have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

##STR00001##

The present disclosure relates to tolperisone, or a pharmaceutically acceptable salt or hydrate thereof, with 10 ppm 2-methyl-1-(4-methylphenyl)-propenone (4-MMPPO) or less, methods of producing the same, as well as compositions related thereto. The disclosure further relates to methods of treating a subject with tolperisone under conditions that limit exposure of the subject to tolerable levels of 4-MMPPO.

The present disclosure relates to methods of administering tolperisone to subjects in need thereof. In certain aspects, the present disclosure relates to methods of administering tolperisone to subjects in need thereof, said methods limiting the exposure of the subject to 4-MMPPO.

Compounds are provided according to Formula (I) ##STR00001##
as well as their enantiomers and their racemics, their acid salts, their hydrates or their solvation products. Among a large number of possible meanings, X represents a halogen, Y an oxygen atom; all of the coefficients m, n, r and s have the value 1, R represents an ethyl and R a cycloalkyl. The invention also includes Methods of preparing the above compounds and the pharmaceutical compositions containing them also are provided.

Compounds are provided according to Formula (I) ##STR00001##
as well as their enantiomers and their racemics, their acid salts, their hydrates or their solvation products. Among a large number of possible meanings, X represents a halogen, Y an oxygen atom; all of the coefficients m, n, r and s have the value 1, R represents an ethyl and R a cycloalkyl. The invention also includes Methods of preparing the above compounds and the pharmaceutical compositions containing them also are provided.