Published:

["<p id=\"p-0001\" num=\"0000\">A compound having the general formula</p>" "<p id=\"p-0002\" num=\"0000\"><chemistry id=\"CHEM-US-00001\" num=\"00001\">\n<img id=\"EMI-C00001\" he=\"20.57mm\" wi=\"13.46mm\" file=\"US09139525-20150922-C00001.TIF\" alt=\"embedded image\" img-content=\"chem\" img-format=\"tif\"/>\n</chemistry>\n<br/>\nwherein A is selected from the group consisting of\n</p>" "<p id=\"p-0003\" num=\"0000\"><chemistry id=\"CHEM-US-00002\" num=\"00002\">\n<img id=\"EMI-C00002\" he=\"16.09mm\" wi=\"50.21mm\" file=\"US09139525-20150922-C00002.TIF\" alt=\"embedded image\" img-content=\"chem\" img-format=\"tif\"/>\n</chemistry>\n<br/>\nto the formation of a compound of the general formula (1)\n</p>" "<p id=\"p-0004\" num=\"0000\"><chemistry id=\"CHEM-US-00003\" num=\"00003\">\n<img id=\"EMI-C00003\" he=\"29.80mm\" wi=\"54.95mm\" file=\"US09139525-20150922-C00003.TIF\" alt=\"embedded image\" img-content=\"chem\" img-format=\"tif\"/>\n</chemistry>\n<br/>\nand a compound of the general formula (2)\n</p>" "<p id=\"p-0005\" num=\"0000\"><chemistry id=\"CHEM-US-00004\" num=\"00004\">\n<img id=\"EMI-C00004\" he=\"30.23mm\" wi=\"55.46mm\" file=\"US09139525-20150922-C00004.TIF\" alt=\"embedded image\" img-content=\"chem\" img-format=\"tif\"/>\n</chemistry>\n<br/>\nrespectively, and pharmaceutically acceptable salts thereof, wherein\n<ul id=\"ul0001\" list-style=\"none\">\n <li id=\"ul0001-0001\" num=\"0000\">R<sup>1 </sup>is a member selected from the group consisting of CF<sub>3</sub>, OSO<sub>2</sub>CF<sub>3</sub>, OSO<sub>2</sub>CH<sub>3</sub>, SOR<sup>4</sup>, SO<sub>2</sub>R<sup>4</sup>, COR<sup>4</sup>, CN, OR<sup>4</sup>, NO<sub>2</sub>, CONHR<sup>4</sup>, 3-thiophene, 2-thiophene, 3-furane, 2-furane, F, Cl, Br and I, wherein R<sup>4 </sup>is as defined below;</li>\n <li id=\"ul0001-0002\" num=\"0000\">R<sup>2 </sup>is a member selected from the group consisting of H, F, Cl, Br, I, CN, CF<sub>3</sub>, CH<sub>3</sub>, OCH<sub>3</sub>, OH, NH<sub>2</sub>, SO<sub>m</sub>CF<sub>3</sub>, O(CH<sub>2</sub>)<sub>m</sub>CF<sub>3</sub>, SO<sub>2</sub>N(R<sup>4</sup>)<sub>2</sub>, CH═NOR<sup>4</sup>, COCOOR<sup>4</sup>, COCOON(R<sup>4</sup>)<sub>2</sub>, (C<sub>1</sub>-C<sub>8</sub>)alkyl, (C<sub>3</sub>-C<sub>8</sub>)cykloalkyl, CH<sub>2</sub>OR<sup>4</sup>, CH<sub>2</sub>(R<sup>4</sup>)<sub>2</sub>, NR<sup>4</sup>SO<sub>2</sub>CF<sub>3</sub>, NO<sub>2</sub>, at phenyl at positions 2, 4, 5 or 6, wherein x and R<sup>4 </sup>are as defined below;</li>\n <li id=\"ul0001-0003\" num=\"0000\">R<sup>3 </sup>is a member selected from the group consisting of hydrogen, CF<sub>3</sub>, CH<sub>2</sub>CF<sub>3</sub>, (C<sub>1</sub>-C<sub>8</sub>)alkyl, (C<sub>3</sub>-C<sub>8</sub>)cykloalkyl, (C<sub>4</sub>-C<sub>9</sub>)cycloalkylmethyl, (C<sub>2</sub>-C<sub>8</sub>)alkenyl, (C<sub>2</sub>-C<sub>8</sub>)alkynyl, 3,3,3-tri-fluoropropyl, 4,4,4-trifluorobutyl, CH<sub>2</sub>SCH<sub>3</sub>, CH<sub>2</sub>CH<sub>2</sub>OCH<sub>3</sub>, CH<sub>2</sub>CH<sub>2</sub>CH<sub>2</sub>F, CH<sub>2</sub>CF<sub>3</sub>, phenylethyl, 2-thiopheneethyl and 3-thiopheneethyl;</li>\n <li id=\"ul0001-0004\" num=\"0000\">R<sup>4 </sup>is a member selected from the group consisting of hydrogen, CF<sub>3</sub>, CH<sub>2</sub>CF<sub>3</sub>, (C<sub>1</sub>-C<sub>8</sub>)alkyl, (C<sub>3</sub>-C<sub>8</sub>)cycloalkyl, (C<sub>4</sub>-C<sub>9</sub>)cycloalkylmethyl, (C<sub>2</sub>-C<sub>8</sub>)alkenyl, (C<sub>2</sub>-C<sub>8</sub>)alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, 2-tetrahydrofurane and 3-tetrahydrofurane;</li>\n <li id=\"ul0001-0005\" num=\"0000\">X is selected from the group consisting of N and sp<sup>3</sup>-hybridized C;</li>\n <li id=\"ul0001-0006\" num=\"0000\">Y is selected from the group consisting of O and, when R<sub>3 </sub>represents H, OH;</li>\n <li id=\"ul0001-0007\" num=\"0000\">Z is selected from the group consisting of H and OH when X is sp<sup>3</sup>-hybridized C or Z represents O or an electronic lone-pair when X is N;</li>\n <li id=\"ul0001-0008\" num=\"0000\">the dashed line represents a bond when X is sp<sup>2</sup>-hybridized C or is absent when X is N;</li>\n <li id=\"ul0001-0009\" num=\"0000\">m is an integer 1 or 2;</li>\n <li id=\"ul0001-0010\" num=\"0000\">n is an integer 1-3;</li>\n <li id=\"ul0001-0011\" num=\"0000\">provided that</li>\n <li id=\"ul0001-0012\" num=\"0000\">when n in Formula 1 is 2, R<sup>1 </sup>is SO<sub>2</sub>CH<sub>3 </sub>and R<sup>2 </sup>is H R<sup>3 </sup>does not represent n-propyl.</li>\n</ul>\n</p>" "<p id=\"p-0006\" num=\"0000\">The invention also relates to a pharmaceutical preparation containing said compound, the use of said compound for the manufacture of a pharmaceutical composition and a method for the treatment of a disorder in the central nervous system of a patient using said compound.</p>"]