NOVEL INDOLE OR BENZIMIDAZOLE DERIVATIVES Russian patent published in 2010 - IPC C07D235/12 C07D401/06 C07D209/12 A61K31/4184 A61P3/04 

FIELD: chemistry.

SUBSTANCE: present invention relates to compounds of formula I , where X is N or CH; R¹ is -C(O)-NR⁸R⁹ or -C(O)-OR¹⁰, and R² is hydrogen; or alternatively R² is and R¹ is hydrogen or halogen; Y is N or CH; R³, R⁴, R⁵ and R⁶ are independently selected from a group consisting of hydrogen, halogen, (lower)alkoxy, (lower)fluoroalkyl, (lower)fluoroalkoxy and (lower)fluoroalkylsulfanyl; or R³ and R⁴ together with carbon atoms with which they are bonded form a 6-member unsaturated ring which can contain one nitrogen heteroatom; R⁷ is hydrogen or (lower)alkyl; R⁸ is hydrogen or NH₂; R⁹ is selected from a group consisting of (lower)alkyl, (lower)alkenyl, (lower)alkoxyalkyl, -(CH₂)_m-(C₃-C₇)cycloalkyl, -(CH₂)_m-piperidinyl, -(CH₂)_m-phenyl, where the phenyl ring is unsubstituted or substituted with one or two groups selected from halogen, (lower)alkoxy, (lower)fluoroalkyl and (lower)fluoroalkoxy, -(CH₂)_m-naphthyl and pyridylamino; R¹⁰ is (lower)alkenyl; R¹¹ is selected from a group consisting of -C(O)-R¹², -SO₂-R¹³ and -SO₂-NR¹⁴R¹⁵; R¹² is selected from a group consisting of (lower)alkyl, (lower)alkoxyalkyl, -(CH₂)_n-(C₃-C₇)-cycloalkyl, -(CH₂)_n-phenyl and -(CH₂)_n-pyridyl, where phenyl or pyridyl are unsubstituted or substituted with one (lower)alkyl; R¹³ is selected from (lower)alkyl or -(CH₂)_n-phenyl, where phenyl is unsubstituted or substituted with one (lower)alkyl; R¹⁴ is (lower)alkyl; R¹⁵ is (lower)alkyl; m equals 0, 1 or 2; n equals 0 or 1; and all their pharmaceutically acceptable salts. The invention also relates to a pharmaceutical composition based on formula I compounds.

EFFECT: novel indole and benzimidazole derivatives which have modulating effect on the CB₁ receptor are obtained.

26 cl, 3 tbl, 148 ex