BIARYL- OR HETEROCYCLIC BIARYL-SUBSTITUTED DERIVATIVES OF CYCLOHEXENE AS CETP INHIBITORS Russian patent published in 2017 - IPC C07D263/22 C07D263/18 C07D263/08 C07D413/08 C07D413/10 A61K31/421 A61K31/443 A61K31/506 A61P9/00 

FIELD: pharmacology.

SUBSTANCE: invention relates to a biaryl or heterocyclic biaryl-substituted cyclohexene derivatives of formula I a stereoisomer thereof or a pharmaceutically acceptable salt thereof, wherein R¹ is -H or -C₁-C₃ alkyl; R² is -C₁-C₃alkyl; each of R³, R⁴, R⁵ and R⁶ is independently -H, halogen, -NO₂ , -C₁-C₃alkyl or -OC₁-C₃alkyl; R⁷ is -H, -(C=O)OR⁸ or -C(O)-NR¹¹R¹²; R⁸; R⁸ is -H or -C₁-C₃alkyl; R¹¹ and R¹² are each independently -H or -C₁-C₃alkyl or can form a 4 to 6-member non-aromatic ring, wherein the non-aromatic ring may contain a N heteroatom and 0 to 1 O heteroatom, and one or more -H in the non-aromatic ring may be replaced by halogen or -OH; each of A¹, A² and A³ is independently N or CR⁹, where, if A² or A³ is N, A¹ is CR⁹; R⁹ is -H, halogen, -C₁-C₃alkyl or -OC₁-C₃alkyl; B is N or CR¹⁰; R¹⁰ is -H, halogen, -OC₁-C₃alkyl or -(C=O)OR⁸; provided that one or more H atoms in -C₁-C₃alkyl or -OC₁-C₃alkyl can be substituted with -F or -CH₃, and if R⁷ is -H, B is CR¹⁰ and R¹⁰ is -(C=O)OR⁸, and if R⁷ is not -H, R¹⁰ not -(C=O)OR⁸. The invention relates to a pharmaceutical composition having a CETP inhibitory activity comprising, as an active ingredient, a compound of formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The compounds of the invention are intended to prevent or treat dyslipidemia or diseases associated with dyslipidemia, including angina pectoris, myocardial infarction or arteriosclerosis.

EFFECT: biaryl- or heterocyclic biaryl-substituted derivatives of cyclohexene as CETP inhibitors.

11 cl, 32 tbl, 172 ex