CA2178219C — Substituted morpholine derivatives and their use as therapeutic agents

USPTO Abstract

The present invention relates to compounds of formula (I), wherein R1 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, CF3, NO2, CN, SR a, SOR a, SO2R a, C02Ra, CONR a R b, C2-6 alkenyl, C2-6 alkynyl or C1-4 alkyl substituted by C_4 alkoxy, where R a' and R b are hydrogen or C1-4 alkyl; R2 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy substituted by C1-4 alkoxy or CF3; R3 is hydrogen, halogen or CF3; R4 is selected from the definitions of R1; R5 is selected from the definitions of R2; R6 is a 5-membered or 6-membered heterocyclic ring containing 2 car 3 nitrogen atoms optionally substituted by =O, =S or a C1-4 alkyl group, and optionally substituted by an aminoalkyl group; R9a and R9b are joined to form a C5-7 ring; X is C1-4 alkylene optionally substituted by oxo; and Y is a C1-4 alkyl group optionally substituted by hydroxyl; with the proviso that if Y is C1-4 alkyl, R6 is substituted at least by an aminoalkyl group; and pharmaceutically acceptable salts and prodrugs thereof. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.