Abstract: Method for the production of formula (I) lumateperone or its acid addition salts so that the enantiomer compound with stereochemistry 6bR,10aS is separated form the cis racemate using resolution and the formula (II) stereoisomer is alkylated with 4-halo-4?-fluoro butyrophenone (X = I, 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.

Abstract: Method for the production of formula (I) lumateperone or its acid addition salts so that the enantiomer compound with stereochemistry 6bR,10aS is separated form the cis racemate using resolution and the formula (II) stereoisomer is alkylated with 4-halo-4?-fluoro butyrophenone (X=I, 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.

Abstract: Method for the production of formula (I) lumateperone or its acid addition salts so that the enantiomer compound with stereochemistry 6bR,10aS is separated form the cis racemate using resolution and the formula (II) stereoisomer is alkylated with 4-halo-4?-fluoro butyrophenone (X?I, 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.

Abstract: The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by subjecting the oxime of the Formula (II), to ring-closure in the presence of an alkali hydroxide, alkali carbonate or alkali-C1-4 alkoxide in an inert organic solvent, converting the base of the Formula I thus obtained into an acid addition salt or setting free the base of the Formula I from an acid addition salt thereof which comprises reacting a halogen derivative of the general Formula (XIV), (wherein Hal is halogen) with piperidine oxime derivative of the Formula (V), or an acid addition salt thereof in the presence of a base, and using by the ring-closure of the oxime of the Formula II formed a C1-4-alkanol as inert solvent.

Abstract: The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by subjecting the oxime of the Formula (II), to ring-closure in the presence of an alkali hydroxide, alkali carbonate or alkali-C1-4 alkoxide in an inert organic solvent, converting the base of the Formula I thus obtained into an acid addition salt or setting free the base of the Formula I from an acid addition salt thereof which comprises reacting a halogen derivative of the general Formula (XIV), (wherein Hal is halogen) with piperidine oxime derivative of the Formula (V), or an acid addition salt thereof in the presence of a base, and using by the ring-closure of the oxime of the Formula II formed a C1-4-alkanol as inert solvent.

Abstract: The invention refers to novel 2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole derivatives of formula (I) having an influence on the heart and the central nervous system, furthermore pharmaceutical compositions containing the above derivatives, and a process for the preparations of the novel compounds.

Abstract: The disclosed compounds have the formula ##STR1## wherein Q is a 6-membered saturated heterocyclic group or a group S(O)pR.sup.3, whereinp is 0, 1, or 2, andR.sup.3 is alkyl, alkenyl, or phenyl-, which may have halogen or nitro substituents, or phenyl optionally substituted;or NR.sup.4 R.sup.5 whereinR.sup.4 and R.sup.5 are hydrogen, alkyl, alkenyl, phenyl-alkyl, or di-alkyl-amino-alkyl;R.sup.1 and R.sup.2 are hydrogen or alkyl, ortogether form a group (CH.sub.2)n--Y--(CH.sub.2)m, wherein Y is CH.sub.2, or NR.sup.6, wherein R.sup.6 is phenyl-alkyl,n and m are 0 or 1 to 5;Z is NR.sup.7 R.sup.8, whereinR.sup.7 and R.sup.8 each are hydrogen, alkenyl, cycloalkyl, adamantayl, or phenyl-alkyl, which may have one or more substituents ortogether form a group of (CH.sub.2)j--W--(CH.sub.2)k, wherein j and k each are 1 to 3, and W is oxygen, CH.sub.2, CHOH, or NR.sup.10 , wherein R.sup.10 is hydrogen, alkoxycarbonyl, or alkyl, which latter may be substituted.or SR.sup.9, whereinR.sup.