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
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Authors
Dates
2017-08-07—Published
2014-01-29—Filed