Trifluoromethylthio (and sulfonyl) derivatives of cyproheptadine analogs
Patent 4031222 Issued on June 21, 1977. Estimated Expiration Date: June 21, 1994. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
514/325, Polycyclo ring system is tricyclo-carbocyclic546/203, The polycyclo ring system is tricyclo-carbocyclic546/204Chalcogen bonded directly to the tricyclo-carbocyclic ring system
Cyproheptadine derivatives substituted with a trifluoromethylthio or trifluoromethylsulfonyl group in one of the benzo rings and having a hydroxyalkyl or cycloalkylalkyl group on the piperidine nitrogen are potent antipsychotic agents, with a low propensity to induce extrapyramidal side effects that are experienced with most major tranquilizers. The tranquilizing activity is predominantly in the levorotatory enantiomers, whereas the dextrorotatory enantiomers have anticholinergic activity. Each enantiomer is useful as a source of the other by racemization. The novel compounds are prepared by treatment of the corresponding iodo or bromo compound with bis(trifluoromethylthio)mercury and copper powder.