| 摘要 |
Described herein are antipyschotic compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S; R<SUP>1 </SUP>is hydrogen, (C<SUB>1-6</SUB>) fluoroalkyl, (C<SUB>3-6</SUB>) cycloalkyl, or (C<SUB>1-4</SUB>) alkyl, wherein the (C<SUB>1-4</SUB>) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH<SUB>2</SUB>CH<SUB>2</SUB>OH, -CN, imidazolidin-2-one, phenyl, or tetrazole wherein tetrazole is unsubstituted or substituted with (C<SUB>1-4</SUB>) alkyl; R<SUP>2 </SUP>is H, halogen, (C<SUB>1-6</SUB>) fluoroalkyl, (C<SUB>3-6</SUB>) cycloalkyl, OR<SUP>6</SUP>, SR<SUP>6</SUP>, NO<SUB>2</SUB>, CN, COR<SUP>6</SUP>, C(O)OR<SUP>6</SUP>, C(OH)R<SUP>6</SUP>, CONR<SUP>7</SUP>R<SUP>8</SUP>, phenyl or (C<SUB>1-6</SUB>) alkyl, wherein the (C<SUB>1-6</SUB>) alkyl is unsubstituted or substituted with a hydroxy; R<SUP>3 </SUP>is hydrogen, (C<SUB>1-6</SUB>)fluoroalkyl , (C<SUB>3-6</SUB>) cycloalkyl, (C<SUB>2-6</SUB>) alkenyl, phenyl, monocyclic heteroaromatic, bicyclic heteroaromatic, or (C<SUB>1-4</SUB>)alkyl wherein (C<SUB>1-4</SUB>) alkyl is unsubstituted or substituted with a phenyl; R<SUP>4 </SUP>and R<SUP>5 </SUP>are independently selected from hydrogen, halogen, (C<SUB>1-6</SUB>) alkyl, (C<SUB>1-6</SUB>) fluoroalkyl, OR<SUP>9</SUP>, SR<SUP>9</SUP>, NO<SUB>2</SUB>, CN, or COR<SUP>9</SUP>; R<SUP>6 </SUP>is hydrogen, (C<SUB>1-6</SUB>) fluoroalkyl, or (C<SUB>1-6</SUB>) alkyl; R<SUP>7 </SUP>and R<SUP>8 </SUP>are independently hydrogen, or (C<SUB>1-6</SUB>) alkyl; R<SUP>9 </SUP>is hydrogen, (C<SUB>1-6</SUB>) fluoroalkyl, (C<SUB>1-6</SUB>) alkyl; Alk is (C<SUB>1-4</SUB>) alkylene unsubstituted or substituted with a hydroxy; Y is oxygen, sulfur, SO<SUB>2</SUB>, or a bond; X is CH<SUB>2</SUB>, C-O, S, O, or SO<SUB>2</SUB>; Z is hydrogen, halogen, (C<SUB>1-6</SUB>) alkyl, (C<SUB>1-6</SUB>)fluoroalkyl, -OH, (C<SUB>1-6</SUB>) alkoxy, (C<SUB>1-6</SUB>) fluoroalkoxy, (C<SUB>1-6</SUB>) alkylthio, (C<SUB>1-6</SUB>) acyl, (C<SUB>1-4</SUB>)alkylsulfonyl, -OCF<SUB>3</SUB>, -NO<SUB>2</SUB>, -CN, carboxamido which may be substituted on the nitrogen by one or two (C<SUB>1-4</SUB>) alkyl groups, and -NH<SUB>2 </SUB>in which one of the hydrogens may be replaced by a (C<SUB>1-4</SUB>) alkyl group and the other hydrogen may be replaced by either a (C<SUB>1-4</SUB>) alkyl group, a (C<SUB>1-6</SUB>) acyl group, or a (C<SUB>1-4</SUB>) alkylsulfonyl group; the phenyl of R<SUP>1</SUP>, R<SUP>2 </SUP>or R<SUP>3 </SUP>is independently unsubstituted or substituted with one to three substituents independently selected from Z; the monocyclic heteroaromatic of R<SUP>3 </SUP>is unsubstituted or substituted with one to three substituents independently selected from Z; the bicyclic heteroaromatic of R<SUP>3 </SUP>is unsubstituted or substituted with one to three substituents independently selected from Z; and salts, solvates, and crystal forms thereof. Also described are the use of the compounds of formula (I) as antagonists of the dopamine D<SUB>2 </SUB>receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I).
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