HYPOGLYCEMIC COMPOUND AND PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION COMPRISING THE HYPOGLYCEMIC COMPOUND, AND APPLICATION THEREOF

摘要

The present invention provides an antihyperglycemic compound and a preparation method thereof, a pharmaceutical composition comprising the antihyperglycemic compound, and an application thereof. The compound is a compound expressed in Formula (I) or a pharmaceutically acceptable salt, solvate, polycrystal, enantiomer, or racemic mixture thereof, wherein R1, R2, R3 and R4 are independently H, optionally substituted alkyl group, optionally substituted naphthenic base, optionally substituted alkyl sulphanyl, optionally substituted alkoxy group, optionally substituted aryl group, or optionally substituted aralkyl; or R1 and R2 together form optionally substituted naphthenic base; or R2 and R3 together form optionally substituted heterocyclic group; or R3 and R4 together form optionally substituted heterocyclic group. The compound is actively transported by a PepT1 transporter, then absorbed by gastrointestinal tract, and decomposed by enzyme in the intestinal tract and liver, to slowly generate Saxagliptin. Therefore, the plasma drug concentration of the Saxagliptin is increased or the staying time of the Saxagliptin in the blood is prolonged, and the stable plasma drug concentration improves the hypoglycemic effect and lowers side effects.