Oxazolidinone derivative as CETP inhibitor, its preparation method, and pharmaceutical composition comprising the same

摘要

Disclosed are a novel oxazolidinone derivative exhibiting inhibitory activity against CETP, a preparation method thereof, and a pharmaceutical composition comprising the same. Exhibiting excellent inhibitory activity against CETP, the oxazolidinone derivative can be effectively applied to the prevention or treatment of various CETP enzyme activity- or HDL cholesterol level-related diseases such as dyslipidemia, atherosclerosis, and coronary heart disease.

主权项

1. A compound represented by the following Chemical Formula 1: wherein, X is N, Y is N or CH; R1 is selected from the group consisting of hydrogen, cyano, halogen, halogen-substituted or unsubstituted C1 to C6 alkyl, —NR4R5, —(O)SO2R6 which is optionally substituted with C1-C4 alkyl or may not be, substituted or unsubstituted C3 to C20 cycloalkyl, substituted or unsubstituted C3 to C20 heterocyclic, substituted or unsubstituted C6 to C40 aryl, and substituted or unsubstituted C3 to C40 heteroaryl; R4 and R5 are independently selected from the group consisting of hydrogen, C1 to C4 alkyl, and C3 to C6 cycloalkyl with a proviso that when R4 and R5 are independently C1 to C4 alkyl, R4 and R5 may be linked to each other to form a hetero cycle containing N; the substituted C3 to C20 cycloalky or the C3 to C20 heterocyclic in R1 may be substituted with a functional radical selected from the group consisting of halogen, halogen-substituted or unsubstituted C1 to C4 alkyl, C1 to C4 hydroxyalkyl, —(CH2)nCOR7, and —(CH2)nCO(O)R7; the substituted C6 to C40 aryl in R1 may be substituted with a functional radical selected from the group consisting of halogen, cyano, nitryl, C1 to C4 alkyl, C1 to C4 hydroxyalkyl, and C1 to C4 alkoxy; the C3 to 40 heteroaryl in R1 may be substituted with cyano, nitryl, oxo, —NR8R9, halogen, halogen-substituted or unsubstituted C1 to C4 alkyl, C1 to C4 hydroxyalkyl, C1 to C4 alkoxy, —(CH2)nCOR10, and —(CH2)nCO(O)R10; R2 is selected from the group consisting of hydrogen, hydroxy-substituted or unsubstituted C1 or C6 alkyl, C3 to C7 cycloalkyl, and —(CH2)nCO(O)R11; R3 is selected from the group consisting of C1 to C6 alkyl which may be substituted with substituted or unsubstituted C3 to C7 cycloalkyl or may not be, substituted or unsubstituted C3 to C7 cycloalkyl, substituted or unsubstituted C3 to C20 heterocyclic, and substituted or unsubstituted C6 to C20 spirocyclic heterocyclic; R2 and R3 may be linked to each other to form a heterocycle containing N, said heterocycle being substituted with halogen-substituted or unsubstituted C1 to C4 alkyl or not; the C3 to C7 cycloalkyl in R3 may be substituted with a functional radical selected from the group consisting of oxo, —NR12R13, C1 to C4 hydroxyalkyl, and —(CH2)nCO(O)R14; the substituted C3 to C20 heterocycle and the substituted C6 to C20 spirocyclic heterocyclic in R3 may be independently substituted with a functional radical selected from the group consisting of oxo, C1 to C4 alkyl, C1 to C4 alkoxy, (CH2)nCO(O)R15, —COR16, and —SO2R17; R16 and R17 are independently C1 to C4 alkyl or —NR18R19; R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R18 and R19 are independently hydrogen or C1 to C4 alkyl; n is an integer of 0, 1 or 2; an isomer thereof, or a pharmaceutically acceptable salt thereof.