QUINOLINE DERIVATIVES AS NEUROPEPTIDE Y ANTAGONISTS Russian patent published in 2007 - IPC C07D401/04 C07D401/14 C07D405/14 C07D215/42 C07D215/46 A61K31/4709 A61K31/495 A61P3/04 A61P3/10 A61P9/10 

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel derivatives of quinoline that can be used as ligands of neuropeptide Y (NPY) receptors and being first of all as neuropeptide Y (NPY) antagonists. Invention describes compounds of the formula (I): wherein R¹ means -O-R⁴ or -NR⁵R⁶; R² means hydrogen atom, alkyl, alkoxy-group or halogen atom; R³ means alkyl or halogen atom; R means hydrogen atom, alkyl, phenyl, phenyl substituted with 1-3 substitutes chosen independently of one another from group comprising alkyl, cyano-group, trifluoromethyl, alkoxy-group, halogen atom, pyrrolidinylcarbonyl and nitro-group, alkoxyalkyl or heterocyclyl that means saturated or aromatic 4-10-membered heterocycle comprising one heteroatom chosen from nitrogen, oxygen atoms; R⁵ and R⁶ are chosen independently of one another from group comprising hydrogen atom, alkyl or phenyl; or R⁵ and R⁶ in common with nitrogen atom (N) to which they are added form 5-10-membered heterocyclic ring comprising nitrogen atom optionally; A¹ means 5-7-membered saturated heterocyclic ring comprising nitrogen atom added to quinoline ring and the second nitrogen atom optionally and wherein ring is substituted optionally with 1-3 substitutes chosen independently of one another from group comprising alkyl, alkoxy-, hydroxy-group, hydroxyalkyl, alkoxyalkyl, tetrahydropyranyloxyalkyl and cycloalkylalkoxy-group; A² means -CH₂- or -C(O)- wherein alkyl individually or in combination means alkyl group with a direct chain that comprises 1-8 carbon atoms; and their pharmaceutically acceptable salts and alkyl esters. Also, invention describes methods for synthesis of compounds of the formula (I) and pharmaceutical composition based on thereof.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

21 cl, 1 tbl, 117 ex