The present invention relates to a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, a method of preparing same and a pharmaceutical composition for preventing and treating metabolic disease including same as an effective ingredient. The novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, an optical isomer thereof, or a pharmaceutically acceptable salt thereof, according to the present invention, has an excellent effect on activation of GPR40 protein and thus has excellent promoting effect of insulin secretion; is nontoxic when co-administrated with other drugs and is possibly co-administrated with other drugs; and has excellent effective effect of activating GPR40 protein in vivo. Therefore, a composition including the novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof may be availably used in a pharmaceutical composition for preventing and treating metabolic disease such as obesity, type I diabetes, type II diabetes, incompatible glucose tolerance, insulin tolerance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, syndrome X, etc.