DERIVATIVES OF PYRIDO[2,1-A]ISOQUINOLINE AS INHIBITORS OF DPP-IV Russian patent published in 2007 - IPC C07D471/04 A61K31/445 A61P3/10 C07D295/00 C07D275/00 C07D221/12 C07D213/00 C07D207/00 

FIELD: organic chemistry, biochemistry, medicine.

SUBSTANCE: invention describes derivatives of pyrido[2,1-a]isoquinoline of the formula (I): wherein R¹ means (lower)-alkyl, unsubstituted phenyl, phenyl mono-, di- or tri-substituted with (lower)-alkyl or (lower)-alkoxy-group, pyrrolyl, pyridynyl or (lower)-alkyl substituted with cycloalkyl or phenyl; each among R², R and R⁴ means independently hydrogen, halogen atom, hydroxy-, (lower)-alkoxy-group or (lower)-alkenyl wherein (lower)-alkoxy-group and (lower)-alkenyl are optionally substituted with groups: (lower)-alkoxycarbonyl, unsubstituted phenyl, phenyl substituted with di-(lower)-alkylamine or cyano-group, thiazolyl substituted with (lower)-alkyl, pyridinyl or morpholino-group; R⁵ means hydrogen atom, (lower)-alkyl or phenyl optionally substituted with halogen atom, (lower)-alkoxy- or hydroxy-group; R⁶ means hydrogen atom, (lower)-alkyl or hydroxy-(lower)-alkyl; or R and R⁶ in common with carbon atoms to which they are bound form phenanthridine; R⁷ means hydrogen atom or (lower)-alkyl. Also, invention describes a method for synthesis of compounds of the formula (I) and preparing a pharmaceutical composition. Proposed compounds are used in treatment or prophylaxis of diseases associated with enzyme DPP-IV, i. e. dipeptidyl peptidase IV, such as diabetes mellitus and firstly non-insulin dependent diabetes mellitus and disturbed tolerance to glucose.

EFFECT: valuable medicinal and biochemical properties of compounds and pharmaceutical composition.

21 cl, 1 tbl, 107 ex