AMIDO-SUBSTITUTED DERIVATIVES OF XANTHINE POSSESSING INHIBITORY EFFECT ON ACTIVITY OF PHOSPHOENOLPYRUVATE CARBOXYKINASE (PEPCK), METHOD FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION AND USING Russian patent published in 2007 - IPC C07D473/02 A61K31/52 A61P3/10 

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel derivatives of xanthine of the formula (I): possessing inhibitory effect on activity of phosphoenolpyruvate carboxykinase. In compound of the formula (I) R¹ is chosen from group consisting of lower alkenyl, lower alkynyl, lower alkenyl substituted with halogen atom, phenyl and phenyl substituted with one or two substitutes chosen independently from group comprising halogen atom, hydroxy-group, lower alkoxy-group, nitro-group, amino-group or 5- or 6-membered aromatic heterocyclic ring comprising 1, 2, 3 or 4 nitrogen atoms added to phenyl by ring carbon atom; R² is chosen from group comprising unsubstituted lower alkyl, lower alkyl substituted with lower alkoxy-group or hydroxy-group, lower alkenyl, phenyl, -(CH₂)_n-unsubstituted lower cycloalkyl and -(CH₂)_n-lower cycloalkyl substituted with at least one substitute chosen from group comprising carboxy-group, lower alkyl, carboxy-lower alkyl and lower alkyl substituted with hydroxy-group, -(CH₂)_n-C(O)R^b wherein R^b is chosen from group comprising hydroxyl, lower alkoxy-group, hydrogen atom, benzyl, lower alkyl and -NHR^b wherein R^b is chosen from group comprising lower alkoxy-group, -NHR^c wherein R^c is chosen from group comprising hydrogen atom, benzyl, lower alkyl and -NHR^d wherein R^d is chosen from group comprising hydrogen atom and carboxy-lower alkyl; -(CH₂)_n-unsubstituted aromatic 5-membered heterocyclic ring comprising one oxygen or sulfur atom, -(CH₂)-aromatic 5-membered heterocyclic ring comprising one oxygen or sulfur atom wherein ring is substituted with carboxylic acid residue, -(CH₂)_n-unsubstituted aromatic 5-membered heterocyclic ring comprising 1, 2 or 3 nitrogen atoms, -(CH)_n-nonaromatic 5- or 6-membered heterocyclic ring comprising at least one oxygen atom and two nitrogen atoms or not comprising nitrogen atoms wherein nonaromatic heterocyclic ring has no substitutes or comprises one ring carbon atom as carbonyl, and wherein R³ means: and others. Also, invention relates to pharmaceutically acceptable salts of compounds, pharmaceutical composition based on thereof, using and inhibition of activity of PEPCK.

EFFECT: improved method of synthesis, valuable medicinal and biochemical properties of compounds and pharmaceutical composition.

32 cl, 1 tbl, 125 ex