NOVEL DIPEPTIDYL PEPTIDASE IV INHIBITORS, SYNTHESIS METHODS THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID INHIBITORS

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to a novel compound of general formula I ; , ;and a pharmaceutically acceptable salt thereof, where X denotes CH₂, CHF or S, Y denotes CN, R₁, R₂, R₃ and R₄ denotes hydrogen, n equals 1, m equals 0 or 1, R denotes R₁₁, R₁₂ or R₁₃, where R₁₁ includes at least one group selected from the following b) or c), where optionally substituted heterocyclic and heteroaryl groups are bonded with a noradamantyl part either directly or through a methylene adjacent group or a C-C bond or C-N bond; b) the substituted 5-member heteroaryl group, in which the heteroaryl ring is a monocyclic aromatic ring system, includes two or more heteroatoms selected from nitrogen and oxygen; c) the heterocyclic group is optionally substituted with a C₁-C₃ alkyl or oxo group, where the heterocyclic ring system is a 5-9-member mono- or bicyclic ring system with one or more heteroatoms selected from a group consisting of nitrogen and sulphur, where heteroatoms can also be present as functional groups, where the heterocyclic ring system can contain one or two double bonds, and where the monocyclic heterocyclic ring can be condensed with a phenyl ring, R₁₂ is selected from hydrogen, halogen, hydroxy, amino and C₁-C₄ alkoxy; R₁₃ is a substituted phenyl, where the substitutes, which can be identical or different, include at least one group selected from a) hydrogen; b) nitro, amino; c) the saturated or unsaturated monocyclic heterocyclic ring system is optionally substituted with one or more groups selected from C₁-C₃ alkyl and oxo, where the heterocyclic ring system is a 5-member ring with one or more heteroatoms selected from a group consisting of nitrogen and sulphur, where the heteroatoms can also be present as functional groups. The present invention also relates to a pharmaceutical composition having dipeptidyl peptidase IV inhibiting activity, methods of obtaining the novel compound of formula I and use in treating type II diabetes and diabetic complications as well as for treating dyslipidaemia, hypercholesteremia, obesity and hyperglycaemia.;EFFECT: novel dipeptidyl peptidase IV inhibitors.;10 cl, 1 tbl, 43 ex