This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation. The compounds have the following formula: wherein X is -O-, -S-, or -NR5-; R5 is hydrogen, C1-8 alkyl, or an amino protecting group; R4 is Y is -O-, -S-, or -NR8-; Y' is -O- or -S-;