NOVEL DUAL ACTING ATI AND ETA RECEPTOR ANTAGONISTS (DARA) Russian patent published in 2011 - IPC C07D471/04 C07D413/14 C07D417/14 A61K31/422 A61K31/4375 A61K31/4709 A61P9/12 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula , where R3 has any

of the formulae , where R1 is selected from

,

where each R2 independently denotes hydrogen, halogen, C₁-C₈alkyl, C₁-C₈alkoxy- C₁-C₈alkyl, C₁-C₈alkoxy; R4 denotes a five- or six-member monocyclic ring system, having two heteroatoms selected from O, N and S, such as pyrazinyl, isoxazole or thiazolyl, each of which can be optionally substituted with one or more of the following substitutes: C₁-C₈alkyl or C₁-C₈alkoxy; R5 and R6 independently denote hydrogen or C₁-C₈alkyl; R7 and R8 together form a cyclopentyl ring; R9 independently denotes C₁-C₈alkyl; R9a independently denotes C₁-C₈alkylcarbonyl or phenylcarbonyl; R10 denotes hydrogen; R11 independently denotes C₁-C₈alkyl or C₁-C₈alkoxy; R12 denotes hydrogen or -COOR17; R13 independently denotes hydrogen, phenyl and a 6-member heteroaryl containing one heteroatom selected from N; R17 denotes hydrogen; R23 denotes (a) C₁-C₈alkyl, phenyl, a 5-member heteroaryl containing 1-2 heteroatoms selected from S and N, where any phenyl or heteroaryl residue is optionally substituted with a halogen, C₁-C₈alkyl or C₁-C₈alkoxy; R24 denotes C₁-C₈alkyl; R27 denotes H, C₁-C₈alkyl, C₁-C₈alkoxy, O-phenyl, S-phenyl; R29 denotes -(CH₂)_w-COOR17; where w=0; R31 denotes hydrogen; and pharmaceutically acceptable salts thereof. The invention also relates to a method of producing the disclosed compounds, a pharmaceutical composition, having dual acting ATI and ETA receptor antagonist properties, containing the disclosed compound as an active component, use of the compound in preparing a medicinal agent and methods of treating arterial hypertension.

EFFECT: high effectiveness of the compounds.

8 cl, 1 dwg, 39 ex