MY102646A - Tricyclic ketones - Google Patents

Abstract

THE INVENTION RELATES TO COMPOUNDS OF THE GENERAL FORMULA (I)(FORMULA 1)WHEREIN IM REPRESENTS AN IMIDAZOLYL GROUP OF THE FORMULA;(FORMULA 2)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 C1-4ALKYL, PHENYL, PHENYL1-3ALKYL, -CO2R5, -COR5, -CONR5R6 OR -SO2R5; 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 PHENYLC1-4 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 -CO2R5 OR -SO2R5; 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 PHENYLC1-3 ALKYL GROUP, AND EACH OF THE OTHER TWO GROUPS, WHICH MAY BE THE SAME OR DIFFERENT, REPRESENTS A HYDROGEN ATOM OR A C1-6ALKYL GROUP; Q REPRESENTS A HYDROGEN OR A HALOGEN ATOM, OR A HYDROXY, C1-4ALKOXY, PHENYLC1-3ALKOXY OR C1-6ALKYL GROUP OR A GROUP -NR7R8 OR -CONR7R8; R7 AND R8, WHICH MAY BE THE SAME OR DIFFERENT, EACH REPRESENTS A HYDROGEN ATOM OR A C1-4 ALKYL OR C3-4 ALKENYL GROUP, OR TOGETHER WITH THE NITROGEN ATOM TO WHICH THEY ARE ATTACHED FORM A SATURATED 5 TO 7 MEMBERED RING; N REPRESENTS 1,,2 OR 3; AND A-B REPRESENTS THE GROUP CH-CH2 OR C=CH; AND PHYSIOLOGICALLY ACCEPTABLE SALTS AND SOLVATES THEREOF.THE COMPOUNDS ARE POTENT AND SELECTIVE ANTAGONISTS 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.