4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVE OR SALTS THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME

摘要

The present invention provides a 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The 4,5-dihydro-1H-pyrazole derivative or its pharmaceutically acceptable salt effectively increases the LXR transcriptional activity, and therefore can be usefully applied for preventing or treating a dysfunction in cholesterol metabolism, such as cholesterol gallstone, hyperlipidemia, or coronary atherosclerosis.

主权项

1. A compound of Formula 1 or its pharmaceutically acceptable salt: wherein, L and L′ are, independently each other, —(CH2)n—, n is 0, 1, 2, or 3, Ring X and Ring Y are, independently each other, a C3˜C6 cycloalkyl ring, an aryl ring, a heteroaryl ring, or a heterocyclic ring, R1 and R3 are, independently each other, hydrogen or halogen, R2 and R4 are, independently each other, hydrogen; halogen; a C1˜C5 alkyl group optionally substituted with one or more halogens; a C1˜C5 alkoxy group; an aryl group; a heteroaryl group; or a heterocyclic group, when R2 and R4 are, independently each other, an aryl group, a heteroaryl group or a heterocyclic group, the aryl group, the heteroaryl group or the heterocyclic group is optionally substituted with one or more substituents selected from the group consisting of halogen; hydroxyl; cyano; azido; C1˜C5 alkyl optionally substituted with one or more substituents selected from the group consisting of halogen, hydroxy, and hydroxyimino; C2˜C6 alkenyl; C2˜C6 alkynyl; C3˜C6 cycloalkyl; aryl; heteroaryl; heterocyclic; —SO3H; —SO2R; —SOR; —SR;—OR; —COR; —CO2R; —OC(═O)R; —OCO2R; —OC(═O)NRR′; —NR″C(═O)R′″; —NR″C(═O)OR′″; —NR″SO2R′″; —CONR″R′″; and —NR″R′″,
R and R′ are, independently each other, hydrogen; a C1˜C5 alkyl group optionally substituted with one or more substituents selected from the group consisting of halogen, hydroxy and C3˜C6 cycloalkyl; a C3˜C6 cycloalkyl group; an aryl group optionally substituted with one or more halogens; an aralkyl group; a heteroaryl group; or a heterocyclic group, R″ and R′″ are, independently each other, hydrogen; a C1˜C5 alkyl group optionally substituted with one or more substituents selected from the group consisting of halogen and hydroxy; a C3˜C6 cycloalkyl group; or an aryl group, p is 0, 1, 2, 3, 4, or 5, and R5 is CF2CF3 or C(CF3)2OH.