公开(公告)号：US20080175837A1

公开(公告)日：2008-07-24

申请号：US11927051

申请日：2007-10-29

申请人： Chiori Ijichi ,  Naoyuki Yamada ,  Toshihiro Hatanaka ,  Kenji Takehana ,  Giovanni Miotto ,  Oriano Marin ,  Andrea Carpi ,  Denis Bertaggia

发明人： Chiori Ijichi ,  Naoyuki Yamada ,  Toshihiro Hatanaka ,  Kenji Takehana ,  Giovanni Miotto ,  Oriano Marin ,  Andrea Carpi ,  Denis Bertaggia

IPC分类号： A61K39/395 ,  A61K38/05 ,  A61P3/10 ,  A61P3/04 ,  C07C229/04 ,  G01N33/53 ,  A61P25/22 ,  C07K16/40

CPC分类号： A61K31/195 ,  C07K16/2896 ,  C07K16/40

摘要： 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.

摘要翻译： 本发明提供一种Dpp4抑制剂，其包含下式（1）的亮氨酸衍生物或下式（2）的甲硫氨酸衍生物：其中R 1和R 3表示氢原子（H）和L-氨基酸残基 ; R2表示羟基（OH），碳原子数1〜6的烷氧基，氨基（NH2），碳原子数1〜6的烷基氨基，甘氨酸残基，β-丙氨酸残基，L-氨基酸（脯氨酸， 丙氨酸和苯丙氨酸）残基或L-氨基酸酰胺（脯氨酸酰胺，丙氨酸酰胺和苯丙氨酸酰胺除外）残基; R 4表示羟基（OH），碳原子数1〜6的烷氧基，氨基（NH 2），碳原子数1〜6的烷基氨基，甘氨酸残基，β-丙氨酸残基，L-氨基酸（脯氨酸 和丙氨酸）残基或L-氨基酸酰胺（除脯氨酰胺和丙氨酸酰胺除外）残基。 这些衍生物也作为自噬调节剂。