DERIVATIVES OF TETRAHYDROCARBAZOLES, METHOD OF OBTAINING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM Russian patent published in 2010 - IPC C07D209/86 C07D209/88 C07D471/04 C07D401/12 C07D401/14 C07D411/06 C07D413/14 A61K31/40 A61P3/06 A61P3/10 A61P25/28 

FIELD: medicine.

SUBSTANCE: invention relates to compounds of general formula (I) and their pharmaceutically acceptable salts and pharmaceutically acceptable asters, possessing activity with respect to LXRα and/or LXRβ receptors. Compounds can be applied for treatment and prevention of diseases mediated by LXRα and/or LXRβ receptors, namely: increased level of lipids and cholesterol level, atherosclerotic diseases, diabetes, metabolic syndrome, dyslipidermia, sepsis, inflammatory diseases, pancreatitis, liver cholestasis/fibrosis, and diseases which include inflammatory component, such as Alzheimer's disease and reduced/improvable cognitive function. In general formula n represents integer number from 0 to 3; R¹ is independently selected from group consisting of halogen, -CN, -NO₂, -SO₂Me, lower alkyl, -OR¹¹, pyperidinyl and -N(R¹¹)(R¹¹), where R¹¹ is independently selected from lower alkyl and H, X¹, X², X³ and X⁴ are independently selected from nitrogen and carbon, on condition that, not more than two of X¹, X², X³ and X⁴ can simultaneously represent nitrogen, and in case when two of X¹, X², X³ and X⁴ represent nitrogen, n represents 0,1 or 2; k represents integer number 0 or 1; R2 represents H; R³ represents H, lower alkyl or halogen; R⁴ represents aryl, heteroaryl, lower alkylaryl or lower alkylheteroaryl, each of which is optionally substituted with substituents in amount from one to five, which are independently selected from group consisting of halogen, lower alkyl, -OR⁴¹, lower alkinyl and NR⁴²R⁴³, where R⁴¹ represents lower alkyl, R⁴² and R⁴³ independently on each other represent hydrogen or lower alkyl, or NR⁴²R⁴³ represents pyrrolidinyl, or R⁴ represents lower alkyl; R⁵ is selected from group, heteroaryl, consisting of and , said aryl and heteroaryl being optionally substituted in one or more positions with one or more substituents, independently selected from group consisting of H, halogen, lower alkyl and (CH₂)_VR⁵³, where R⁵¹ is selected from group consisting of H, lower alkyl, lower alkenyl and lower alkylaryl, said lower alkylaryl is optionally substituted in one or more positions with one or more lower alkyl, -CN, halogen, group -COOR⁵⁴ and group -CH₂OR⁵⁴, where R⁵⁴ represents lower alkyl or H; R⁵² represents lower alkyl or -H; R⁵³ represents H, lower alkyl, C₃-C₆-cycloalkyl, -COOR⁵⁵, -N(R⁵⁵)(R⁵⁶), -CH₂OH, -CN, CF₃, -CONH₂ or -CH₂OR⁵⁵, where R⁵⁵ is independently selected from group consisting of lower alkyl, -H, -C(O)aryl or -C(O)-lower alkyl, and R⁵⁶ is selected from group consisting of H, lower alkyl, -C(O)CF₃, -C(O)aryl, -C(O)-lower alkyl and lower alkylaryl, and where said aryl and lower alkylaryl are optionally substituted in one or more positions with one or more lower alkyl, halogen, group COOR⁵⁷ and group -CH₂OR⁵⁷, where R⁵⁷ represents lower alkyl or -H, or R⁵⁵ and R⁵⁶ together with atom to which they are bound, form ring system; or R⁵³ represents aryl, which can be optionally substituted with benzyloxy, carboxy, lower alkoxycarbonyl, hydroxy-(lower alkyl), halogen, carbamoyl, (lower alkyl)carbamoyl, di-(lower alkyl)carbamoyl, m represents integer number from 0 to 2; v represents integer number from 0 to 4; where term "lower alkyl" separately or in combination with other groups refers to branched or linear monovalent alkyl radical, containing from one to six carbon atoms, where term "aryl" separately or in combination with other groups refers to phenyl or naphthyl, and where term "hetyeroaryl" refers to aromatic 5- or 6-member ring, which can include 1-3 heteroatoms selected from nitrogen, oxygen and/or sulphur, and which can be condensed with phenyl group.

EFFECT: increase of compound application efficiency.

38 cl, 5 dwg, 137 ex