申请人:Ijichi Chiori
公开号:US20080175837A1
公开(公告)日:2008-07-24
The present invention provides a Dpp4 inhibitor which comprises a leucine derivative of the following formula (1) or a methionine derivative of the following formula (2):
wherein each R1 and R3 represents a hydrogen atom (H) and an L-amino acid residue; R2 represents a hydroxyl group (OH), alkoxy group having 1 to 6 carbon atoms, amino group (NH2), alkylamino group having 1 to 6 carbon atoms, glycine residue, β-alanine residue, L-amino acid (except for proline, alanine and phenylalanine) residue or L-amino-acid amide (except for proline amide, alanine amide and phenylalanine amide) residue; and R4 represents a hydroxyl group (OH), alkoxy group having 1 to 6 carbon atoms, amino group (NH2), alkylamino group having 1 to 6 carbon atoms, glycine residue, β-alanine residue, L-amino acid (except for proline and alanine) residue or L-amino-acid amide (except for proline amide and alanine amide) residue. These derivatives also act as autophagy regulators.
本发明提供了一种Dpp4抑制剂,其包括以下式(1)的亮氨酸衍生物或以下式(2)的甲硫氨酸衍生物:其中每个R1和R3代表氢原子(H)和L-氨基酸残基;R2代表羟基(OH),具有1到6个碳原子的烷氧基,氨基(NH2),具有1到6个碳原子的烷基氨基,甘氨酸残基,β-丙氨酸残基,L-氨基酸(除脯氨酸、丙氨酸和苯丙氨酸外)残基或L-氨基酸酰胺(除脯氨酸酰胺、丙氨酸酰胺和苯丙氨酸酰胺外)残基;以及R4代表羟基(OH),具有1到6个碳原子的烷氧基,氨基(NH2),具有1到6个碳原子的烷基氨基,甘氨酸残基,β-丙氨酸残基,L-氨基酸(除脯氨酸和丙氨酸外)残基或L-氨基酸酰胺(除脯氨酸酰胺和丙氨酸酰胺外)残基。这些衍生物还作为自噬调节剂。