INDOL DERIVATIVES, THE METHOD FOR PREPARING THEREOF AND PHARMACEUTICAL COMPOSITION FOR THE PREVENTION AND TREATMENT OF METABOLIC DISORDER CONTAINING THE SAME AS AN ACTIVE INGREDIENT

摘要

Indol derivatives are provided to control lipid metabolism and energy metabolism by inhibiting activity of DGAT(Acyl CoA:diacylglycerol acyltransferase), so that they are useful for prevention and treatment of metabolic disorders including obesity and diabetes caused by DGAT. Indol derivatives represented by the formula(1) or pharmaceutically acceptable salts thereof are useful for prevention and treatment of metabolic disorders, wherein R1 is COORa, CONRbRc or C1-C4 alkyl group; Ra is H or C1-C4 alkyl group; Rb and Rc are each independently at least one substituent selected from C3-C5 heteroaryl group containing N, O or S and C3-C5 heterocycle group containing N, O or S, and selected from C1-C5 alkyl group, H and C1-C5 alkyl group; and R2 is selected from H, C5-C7 aryl C1-C5 alkyl group, di-C1-C5 alkylamino C1-C5 alkyl group, C1-C5 alkylcarbonyl group, C1-C5 alkyl C1-C5 alkoxycarbonyl group, C5-C7 aryl C1-C5 alkylsulfonyl group and thiophene C1-C5 alkylsulfonyl group. The indol derivatives represented by the formula(1a) are prepared by reacting 3-(1H-indol-3-yl)propionic acid represented by the formula(2) with amine derivatives represented by the formula(3) having an R1 group in organic solvent in the presence of base and condensation reagents at room temperature.