ORGANIC COMPOUNDS Russian patent published in 2013 - IPC C07D417/04 C07D417/14 C07D401/04 C07D401/14 C07D409/14 C07D409/04 C07D405/04 A61K31/4427 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I), wherein V is specified in -O- or a single bond; W is specified in -N(R⁵)C(O)-, -S(O)_t- and -C(O)O-; X is specified in C(H) or N; Y is specified in S, N(H) or N(CH₃); p means 0 or 2; t means 1 or 2; R¹ is specified in a group consisting of hydrogen, C_1-6alkyl optionally substituted by 1 or 2 halogroups, C_3-7cycloalkylC_1-6alkyl, 2,3-dihydro-1H-indenyl, C₆arC_1-6alkyl optionally substituted by one or two halogroups and heteroarylC_1-6alkyl, wherein a heteroaryl fragment of the heteroarylalkyl group means 5-6-member monocyclic heteroaryl containing 1 or 2 heteroatoms independently specified in a group consisting of nitrogen optionally oxidated, oxygen and sulphur, or a heteroaryl fragment of the heteroarylalkyl group means 9-member bicyclic heteroaryl containing 1 or 2 heteroatoms independently specified in a group consisting of nitrogen, oxygen and sulphur, wherein monocyclic heteroaryl of the heteroarylalkyl group may be optionally substituted by one or two substitutes independently specified in a group consisting a halogroup, a cyanogroup, C_1-6alkyl, haloC_1-6alkyl and C_1-6alkyl-O-C(O)-; R² is specified in a group consisting of hydrogen, C_1-6alkyl optionally substituted by phenoxy, hydroxy C_1-6alkyl, C_3-7cycloalkyl, C_3-7cycloalkylC_1-6alkyl, phenyl optionally substituted by a halogroup, haloC_1-6alkyl, C₆arC_1-6alkyl (optionally substituted by a halogroup, haloC_1-6alkyl or haloC_1-6alkoxygroup), 2-oxo-imidazolidinyl, heterocyclylC_1-6alkyl and heteroarylC_1-6alkyl, wherein heterocyclyl of heterocyclylalkyl means 5- or 6-member monocycle containing oxygen, and wherein a heteroaryl fragment of the heteroarylalkyl group means 5-6-member monocycle containing 1-3 heteroatoms specified in a group consisting of nitrogen, oxygen and sulphur, or a heteroaryl fragment of the heteroarylalkyl group means 9- or 10-member bicycle containing 1 to 2 heteroatoms specified in a group consisting of nitrogen and sulphur, wherein monocyclic heteroaryl of the heteroaryl alkyl group may be optionally substituted by 1 or 2 substitutes independently specified in a group consisting of a halogroup, C_1-6alkyl, haloC_1-6alkyl and phenyl optionally substituted by a halogroup; R³ is specified in a group consisting of hydrogen and alkyl; two adjacent R⁴ groups together with carbon atoms whereto attached can form phenyl; R⁵ means hydrogen; or a pharmaceutically acceptable salt thereof.

EFFECT: preparing the heterocyclic derivatives which modulate activity of stearoyl CoA desaturase, methods of using the above derivatives for modulating activity of stearoyl CoA desaturase and pharmaceutical compositions containing the above derivatives.

26 cl, 1 tbl, 153 ex