CHIRAL LOW-TOXICITY CB1 RECEPTOR INHIBITOR, PREPARATION METHOD THEREFOR, AND USE THEREOF

摘要

The present invention relates to a chiral low-toxicity CB1 receptor inhibitor, a preparation method therefor, and a use thereof. The CB1 receptor inhibitor is a compound represented by General Formula I or a pharmaceutically acceptable salt, solvate, polymorph, an enantiomer or a racemic mixture thereof. The chiral, low-toxicity diaryl substituted pyrazole derivative CB1 receptor inhibitor has an in-vitro CB1 receptor inhibition activity equivalent to that of rimonabant and blood-brain barrier permeability lower than that of rimonabant. Due to the introduction of a hydroxyl group, and especially the presence of an optically asymmetric center, the selectivity is higher, and the toxicity and especially the central nervous system toxicity are obviously lower than those of rimonabant, thus being useful in preparation of drugs for drug rehabilitation, weight reduction, prevention or treatment of diabetes mellitus and cardiovascular diseases, and even useful in all medical areas relevant to the CB1 receptor inhibitor.