| abstract |
Described herein are antipyschotic compounds of formula (I) n nwherein,n A is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S; Alk is (C 1-4 ) alkylene optionally substituted with OH, methoxy, ethoxy, or F; Ar is optionally substituted phenyl, naphthyl, monocyclic heteroaromatic, or bicyclic heteroaromatic; R 1 is hydrogen or (C 1-4 ) alkyl optionally substituted with OH, OR 3 , or OCH 2 CH 2 OH,n wherein R 3 is (C 1-2 ) alkyl; n R 2 is H, (C 1-6 ) alkyl, halogen, fluorinated (C 1-6 ) alkyl, OR 4 , SR 4 , NO 2 , CN, COR 4 , CONR 5 R 6 , SO 2 NR 5 R 6 , NR 5 R 6 , NR 5 COR 4 , NR 5 SO 2 R 4 , or optionally substituted phenyl,n wherein R 4 is hydrogen, (C 1-6 ) alkyl, fluorinated (C 1-6 ) alkyl, or optionally substituted phenyl, R 5 and R 6 are independently hydrogen, (C 1-6 ) alkyl, or optionally substituted phenyl; n Z is one or two substituents independently selected from hydrogen, halogen, (C 1-6 ) alkyl, fluorinated (C 1-6 ) alkyl, OR 7 , SR 7 , NO 2 , CN, COR 7 , CONR 8 R 9 , SO 2 NR 8 R 9 , NR 8 SO 2 R 7 , NR 8 R 9 , or optionally substituted phenyl,n wherein R 7 is hydrogen, (C 1-6 ) alkyl, fluorinated alkyl, or optionally substituted phenyl, R 8 and R 9 are independently hydrogen, (C 1-6 ) alkyl, or optionally substituted phenyl; n and salts, solvates, and crystal forms thereof.n nAlso described are the use of the compounds of formula (I) as antagonists of the dopamine D 2 receptor and as agents for the treatment of psychosis and bipolar disorder, and pharmaceutical formulations of the compounds of formula (I). |