PYRIDINE-3-CARBOXAMIDE DERIVATIVES AS CB1 INVERSE AGONISTS Russian patent published in 2010 - IPC C07D213/64 C07D213/74 A61K31/465 A61P25/34 A61P3/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula: ,

where R¹ is selected from a group consisting of cycloalkyl which is unsubstituted or substituted with hydroxy or lower alkoxy, lower hydroxylalkyl, lower hydroxyhalogenalkyl, -CH₂-CR⁹R¹⁰-cycloalkyl; R⁹ is hydrogen or lower alkyl; R¹⁰ is hydrogen, hydroxy or lower alkoxy; R² is hydrogen; X is O or NR¹⁴; R¹⁴ is hydrogen or lower alkyl; R³ is selected from a group consisting of lower alkyl, cycloalkyl, lower cycloalkylalkyl, lower alkoxyalkyl, lower halogenalkyl, lower carbamoylalkyl, lower phenylalkyl, lower heterocyclylalkyl, where the heterocyclyl is a saturated 4- or 5-member ring containing one or two oxygen atoms, lower heteroarylalkyl, where the heteroaryl group is unsubstituted or mono- or disubstituted with a halogen, and phenyl which is unsubstituted or mono- or disubstituted with a halogen; or R³ and R¹⁴ together with a nitrogen atom to which they are bonded form an N-heterocyclic ring selected from pyrrolidinyl, piperidinyl or azepanyl; R⁴ and R⁸ independently denote hydrogen or halogen; R⁵ and R⁷ are independently selected from a group consisting of hydrogen, halogen, lower halogenalkyl, lower halogen, alkoxy and cyano; R⁶ is selected from a group consisting of hydrogen, halogen, lower halogenalkyl, lower halogen alkoxy and cyano; and pharmaceutically acceptable salts thereof, as well as to a pharmaceutical composition based on said compounds, which has CB1 modulating activity.

EFFECT: novel compounds which can be used to treat and prevent diseases associated with modulation of CB1 receptors, such as obesity, are obtained and described.

23 cl, 153 ex