DERIVATIVES OF PYRIDO[2,1-A]ISOQUINOLINE AS INHIBITORS OF DPP-IV

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