MY103831A - Lactam derivatives. - Google Patents

Abstract

THE INVENTION RELATES TO TRICYCLIC LACTAMS OF THE GENERAL FORMULA (1)@@(FORMULA 1)@@WHEREIN IM REPRESENTS AN IMIDAZOLYL GROUP OF THE FORMULA:@@(FORMULA 2)@@AND R1 REPRESENTS A HYDROGEN ATOM OR A GROUP SELECTED FROM C1- 6 ALKYL, C3- 6 ALKENYL, C3- 10 ALKYNYL, C3- 7 CYCLOALKYL, C3- 7 CYCLOALKYL C1- 4 ALKYL, PHENYL, PHENYL C1- 3 ALKYL, PHENYLMETHOXYMETHYL, PHENOXYETHYL, PHENOXYMETHYL, - CO2 R5 -COR5, CONR5 R6 OR -SO2 R5 (WHEREIN R5 AND R6 WHICH MAY BE THE SAME OR DIFFERENT, EACH REPRESENTS A HYDROGEN ATOM, A C1- 6 ALKYL OR C3- 7 CYCLOALKYL GROUP OR A PHENYL OR PHENYL C1- 4 ALKYL GROUP, IN WHICH THE PHENYL GROUP IS OPTIONALLY SUBSTITUTED BY ONE OR MORE C1- 4 ALKYL, C1- 4 ALKOXY OR HYDROXY GROUPS OR HALOGEN ATOMS WITH THE PROVISO THAT R5 DOES NOT REPRESENT A HYDROGEN ATOM WHEN R1 REPRESENTS A GROUP - CO2 R5 OR - SO2 R5); ONE OF THE GROUPS REPRESENTED BY R2, R3 AND R4 IS A HYDROGEN ATOM OR A C1- 6 ALKYL, C3- 7 CYCLOALKYL, C3- 6 ALKENYL, PHENYL OR PHENYL C1- 3 ALKYL GROUP AND EACH OF THE OTHER TWO GROUPS WHICH MAY BE THE SAME OR DIFFERENT, REPRESENTS A HYDROGEN ATOM OR A C1- 6 ALKYL GROUP; N REPRESENTS 2 OR 3; AND PHYSIOLOGICALLY ACCEPTABLE SALTS AND SOLVATES THEREOF. THE COMPOUNDS ARE POTENT AND SELECTIVE ANTAGONIST OF THE EFFECT OF 5- HT AT 5- HT3 RECEPTORS AND ARE USEFUL FOR EXAMPLE IN THE TREATMENT OF PSYCHOTIC DISORDERS, ANXIETY, AND NAUSEA AND VOMITING.