PIPERIDINE/PIPERAZINE DERIVATIVES Russian patent published in 2013 - IPC C07D295/135 A61K31/451 A61K31/495 A61P3/06 A61P9/00 A61P35/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I) possessing a property of DGAT inhibitor, its N-oxides, its pharmaceutically acceptable salts and solvates, as well as to a based pharmaceutical composition and their application. In general formula (I) , A represents CH or N; a dash line represents an optional bond provided A represents a carbon atom; X represents -O-C(=O)-; -NR^x-C(=O)-; -Z-C(=O)-; -Z-NR^x-C(=O)-; -NR^X-C(=S)-; Z represents C_1-6alkandiyl; R^x represents hydrogen; Y represents -C(=O)-NR^x- or -NR^x-C(=O)-; R¹ represents aryl¹ or Het¹; R² represents C_3-6cycloalkyl, phenyl, 2,3-dihydro-1,4-benzodioxynyl, or a 6-member aromatic heterocycle containing 1 or 2 N atoms wherein said phenyl or the 6-member aromatic heterocycle containing 1 or 2 N atoms may be optionally substituted by one, two, three or four substitutes with each substitute independently specified in a group consisting of halogen; C_1-6alkyl, C_1-6alkyloxy, C_1-6alkylthio; C_1-6alkyloxycarbonyl, nitro; mono- or di(C_1-4alkyl)amino; R⁴R³N-C_1-6alkyl; Het-C(=O)-C_1-4alkyl; R³ represents C_1-4alkyl; R⁴ represents C₁.₄alkyl; R⁵ represents hydrogen; C_1-4alkyl; C_1-4alkylcarbonyl; R⁶ represents hydrogen or C_1-4alkyl; or R⁵ and R⁶ may be taken together with a nitrogen atom whereto bound to form a saturated monocyclic 5, 6 or 7-member heterocycle which may additionally contain one or more heteroatoms each of which independently specified in O, S, S(=O)_P or N; and such heterocycle may be optionally substituted by C_1-4alkyl; R' represents hydrogen or halogen; aryl represents phenyl or phenyl substituted by halogen, C_1-6alkyl, polyhalogen C_1-6alkyl; C_1-6alkylxoycarbonyl; aryl represents phenyl or fluorenyl; each of said phenyl or fluorenyl may be optionally substited by one or two substitutes with each substitute independently specified in a group involving oxo; carboxyl; halogen; C_1-6alkyl optionally substituted by carboxyl or C_1-4alkyloxycarbonyl; C_1-6alkyloxy; C_1-6alkyloxycarbonyl; amino; aryl; Het; Het represents a monocyclic nonaromatic or aromatic heterocycle containing at least one heteroatom each independently specified in O, S, S(=O)_p or N; or a bicyclic nonaromatic or aromatic heterocycle containing at least one heteroatom each independently specified in N; said monocyclic heterocycle or said bicyclic heterocycle may be optionally substituted by at least one or two substitutes with each substitute independently specified in a group containing oxo; or C_1-6alkyl; Het¹ represetns a monocyclic nonaromatic or aromatic heterocycle containing at least one heteroatom each independently specified in S or N; said monocyclic heterocycle may be optionally substituted by one substitute, particularly by one or two substitutes with each substitute independently specified in a group consisting of hydroxyl, oxo, C_1-6alkyl, C_1-6alkyloxycarbonyl, aryl; Het; p has the value of 2.

EFFECT: there are presented new piperidine/piperazine derivatives.

17 cl, 10 tbl, 146 ex