| 摘要 |
Reaction products of sertindole with an acid or an activated acid, with formaldehyde alone, formaldehyde in the presence of an alcohol or an amine, or with an acyloxymethylene halide, and having general formula (1) wherein X is CO, CS, or CH2, and if X is CO or CS, R is (i) hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl or cycloalk(en)ylalk(en)yl optionally substituted with hydroxy, or optionally substituted phenyl; or (ii) YR1, wherein Y is O or S and R1 is one of the substituents defined for R under (i) above; or (iii) NR2R3, wherein R2 and R3 independently are selected from the substituents defined for R under (i) above or R2 and R3 are combined to form a heterocyclic ring; or if X is CH2, R is: (iv) a group YR1 as defined in (ii); (v) a group NR2R3 as defined in (iii); or (vi) a group OC(O)R4, wherein R4 is as defined for R1; are prodrugs of sertindole and show sustained release of sertindole when injected as formulated in a suitable oil. The compounds are useful in the treatment of mental disorders such as schizophrenia including both negative and positive symptoms, non-schizophrenic psychoses, depression and anxiety. |
