A quaternary ammonium salt of formula (I): wherein X is a linking group; Y is O, NH or NR.sup.1 wherein R.sup.1 is H or an optionally substituted hydrocarbyl group; Q.sup.+ is a moiety that includes a quaternary ammonium cation; A.sup.− is an anion; R.sup.2 is an optionally substituted alkylene group; R.sup.3 is hydrogen or an optionally substituted hydrocarbyl group; and n is 0 or a positive integer; provided that n is not 0 when R.sup.3 is hydrogen. ##STR00001##

A quaternary ammonium salt of formula (I): wherein X is a linking group; Y is O, NH or NR.sup.1 wherein R.sup.1 is H or an optionally substituted hydrocarbyl group; Q.sup.+ is a moiety that includes a quaternary ammonium cation; A.sup.− is an anion; R.sup.2 is an optionally substituted alkylene group; R.sup.3 is hydrogen or an optionally substituted hydrocarbyl group; and n is 0 or a positive integer; provided that n is not 0 when R.sup.3 is hydrogen. ##STR00001##

The present invention relates to a method for preparing a pyrroloaminopyridazinone compound and intermediates thereof. Specifically relating to a method for preparing the compound of formula (I), the target product being prepared by means of changing the starting materials and intermediates; the present method has the advantages of reactants such as the starting materials being easy to purchase, the reaction conditions being simple and controllable, the post-reaction treatment method being simple, the yield being high, and being beneficial for industrial production.

##STR00001##

The invention relates to novel small molecule compounds having a basic structure as depicted by formula (A), where in particular exemplary embodiments R.sup.1 is —OH, R.sup.2 is —NO.sub.2 and R.sup.3 is H, R.sup.4 and R.sup.5 are H, one of R.sup.6 and R.sup.7 is selected from H, —CONH.sub.2, and —CONR.sup.9.sub.2, and the other one is selected from —CONR.sup.9.sub.2 and —CONR.sup.11R.sup.9, wherein R.sup.9 and R.sup.11 are (possibly multiply) substituted alkyl and H or alkyl, respectively. The compounds of the invention inhibit the enzyme Catechol-O-methyltransferase (COMT) and exhibit a low off-target profile. The compounds are provided for use as a medicament, in particular for use in prevention or treatment of Parkinson's disease.

The invention relates to novel small molecule compounds having a basic structure as depicted by formula (A), where in particular exemplary embodiments R.sup.1 is —OH, R.sup.2 is —NO.sub.2 and R.sup.3 is H, R.sup.4 and R.sup.5 are H, one of R.sup.6 and R.sup.7 is selected from H, —CONH.sub.2, and —CONR.sup.9.sub.2, and the other one is selected from —CONR.sup.9.sub.2 and —CONR.sup.11R.sup.9, wherein R.sup.9 and R.sup.11 are (possibly multiply) substituted alkyl and H or alkyl, respectively. The compounds of the invention inhibit the enzyme Catechol-O-methyltransferase (COMT) and exhibit a low off-target profile. The compounds are provided for use as a medicament, in particular for use in prevention or treatment of Parkinson's disease.

Disclosed are compounds which may be utilized to inhibit transcription by RNA Polymerase II (Pol II), and in particular to disrupt the Super Elongation Complex (SEC). The compounds may be utilized in pharmaceutical compositions and methods for treating diseases and disorders associated with the biological activity of SEC, and in particular, diseases and disorders that are associated with high levels of expression of genes whose expression is SEC-dependent and that promote, support, or otherwise are required for the disease or disorder such as cancers.

Disclosed are compounds which may be utilized to inhibit transcription by RNA Polymerase II (Pol II), and in particular to disrupt the Super Elongation Complex (SEC). The compounds may be utilized in pharmaceutical compositions and methods for treating diseases and disorders associated with the biological activity of SEC, and in particular, diseases and disorders that are associated with high levels of expression of genes whose expression is SEC-dependent and that promote, support, or otherwise are required for the disease or disorder such as cancers.

Improved processes for producing high purity acesulfame potassium. In one embodiment, the process comprises the steps of contacting a solvent, e.g., dichloromethane, and a cyclizing agent, e.g., sulfur trioxide, to form a cyclizing agent composition and reacting an acetoacetamide salt with the cyclizing agent in the composition to form a cyclic sulfur trioxide adduct. The contact time is less than 60 minutes. The process also comprises forming from the cyclic sulfur trioxide adduct composition a finished acesulfame potassium composition comprising non-chlorinated, e.g., non-chlorinated, acesulfame potassium and less than 35 wppm 5-halo acesulfame potassium, preferably less than 5 wppm.

Improved processes for producing high purity acesulfame potassium. In one embodiment, the process comprises the steps of contacting a solvent, e.g., dichloromethane, and a cyclizing agent, e.g., sulfur trioxide, to form a cyclizing agent composition and reacting an acetoacetamide salt with the cyclizing agent in the composition to form a cyclic sulfur trioxide adduct. The contact time is less than 60 minutes. The process also comprises forming from the cyclic sulfur trioxide adduct composition a finished acesulfame potassium composition comprising non-chlorinated, e.g., non-chlorinated, acesulfame potassium and less than 35 wppm 5-halo acesulfame potassium, preferably less than 5 wppm.

Method for the production of formula (I) lumateperone or its acid addition salts so that the enantiomer compound with stereochemistry 6bR,10aS

##STR00001##

is separated form the cis racemate using resolution and the formula (II) stereoisomer is alkylated with 4-halo-4-fluoro butyrophenone (XI, Br, Cl) to produce the formula (I) lumateperone, or optionally its acid addition salt. The object of the invention also relates to the amorphous form of the morphologically uniform p-toluenesulfonic acid salt of lumateperone and to the naphthalene-2-sulfonic acid salt of lumateperone, to the 1:2 stoichiometry salt of lumateperone formed with naphthalene-2-sulfonic acid.