| abstract |
The invention relates to novel cinnamide compounds which have 5-HT2C antagonist activity and have the general formula (I), or is a pharmaceutically acceptable salt thereof: in which P is phenyl or naphthyl; R1 is halogen, C¿1-6?alkyl, C1-6alkoxy, C1-6alkylthio, hydroxy, amino, mono- or di-C1-6alkylamino, nitro, CN, CF3, OCF3, aryl, arylC1-6alkyl, arylC1-6alkyloxy or arylC1-6alkylthio; a is 0, 1, 2, 3, 4 or 5; R?2 and R3¿ are independently hydrogen or C¿1-6?alkyl; R?4¿ is hydrogen, halogen, C¿1-6?alkyl, C1-6alkocy, aryl, cyano, haloC1-6alkyl or OCF3; Z is carbon or nitrogen; R?5¿ is either: (i) a group NR6R7 where R?6 and R7¿ are independently hydrogen, optionally substituted C¿1-6?alkyl; or (ii) an optionally substituted N-linked heterocycle; or (iii) an optionally substituted C-linked heterocycle; n is 0, 1, 2 or 3 subject to the proviso that n is not 0 when R?5¿ is a group (i) or (ii); --- represents a single or double bond; X and Y are independently CR8R9 (when --- represents a single bond) or X and Y are independently CR10 (when --- represents a double bond) wherein R?8, R9 and R10¿ are independently hydrogen or C¿1-6?alkyl. Also disclosed are processes for their preparation, compositions containing them and their use in the treatment of CNS and other disorders. |