INHIBITORS OF DIPEPTIDYL PEPTIDASE IV Russian patent published in 2006 - IPC C07D403/12 A61K31/495 A61P5/00 

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

SUBSTANCE: invention relates to series of new compounds that are inhibitors of enzyme dipeptidyl peptidase IV. Invention proposes a compound chosen from derivatives of the formula (1) its tautomers and stereomers and pharmaceutically acceptable salts of indicated derivatives, tautomers and isomers wherein R¹ represents hydrogen atom (H) or -CN; X¹ represents sulfur atom (S), oxygen atom (O), -SO₂ or -CH₂; X² represents -CO, -CH₂ or a covalent bond; Het represents nitrogen-containing heterocycle; n = 1-5. Invention proposes a pharmaceutical composition possessing properties of inhibitor of enzyme dipeptidyl peptidase IV, and a method for treatment of at least one diseases among diabetes mellitus type 2, reduced tolerance to glucose, growth hormone deficiency, polycystic ovary syndrome and autoimmune and inflammatory diseases. Invention provides preparing series of inhibitors of dipeptidyl peptidase IV showing the improved affinity to enzyme, preparing pharmaceutical compositions and their using in treatment of some human diseases including the reduced tolerance to glucose and diabetes mellitus of type 2.

EFFECT: valuable biochemical and medicinal properties of inhibitors.

14 cl, 6 tbl, 123 ex