NOVEL 1,2,3,4-TETRAHYDROQUINOXALINE DERIVATIVE CONTAINING PHENYL GROUP AS SUBSTITUTE, HAVING SULPHONIC ACID ESTER STRUCTURE OR SULPHONIC ACID AMIDE STRUCTURE, AND HAVING GLUCOCORTICOID RECEPTOR BINDING ACTIVITY Russian patent published in 2013 - IPC C07D241/44 C07D401/12 C07D405/12 C07D409/12 C07D413/12 A61K31/498 A61K31/5377 A61P3/00 A61P5/50 A61P11/00 A61P25/00 A61P9/12 A61P27/06 A61P29/00 A61P37/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula (1) or salts thereof, where in formula (1) R¹ is a lower C₁-C₆alkyl group, a lower C₃-C₆cycloalkyl group, a phenyl group, a heterocyclic group, which relates to a residue formed by removing a hydrogen atom from a saturated or unsaturated monocyclic heterocyclic ring containing one, two or three heteroatoms in the ring, selected from a nitrogen atom, an oxygen atom and a sulphur atom, or a phenyl(C₁-C₆alkyl) group; in cases when R¹ is a lower C₁-C₆alkyl group, that lower C₁-C₆alkyl group can have, as substitute(s), one, two or three groups selected from a halogen atom, a heterocyclic group which relates to a residue formed by removing a hydrogen atom from a saturated monocyclic heterocyclic ring containing one or two heteroatoms in the ring, selected from a nitrogen atom and an oxygen atom, a carboxyl group, a lower C₁-C₆alkoxycarbonyl group, a lower C₁-C₆alkylamino group, a lower C₁-C₆alkylamino group, substituted with a lower C₁-C₆alkylamino group, a lower C₁-C₆alkylamino group, substituted with a phenyl group; in cases when R¹ is a phenyl group, a heterocyclic group which relates to a residue formed by removing a hydrogen atom from a saturated or unsaturated monocyclic heterocyclic ring containing one, two or three heteroatoms in the ring, selected from a nitrogen atom, an oxygen atom or a sulphur atom, or a phenyl(C₁-C₆alkyl) group, that phenyl, heterocyclic or phenyl(C₁-C₆alkyl) group can contain, as substitute(s), one, two or three groups selected from a halogen atom, a lower C₁-C₆alkyl group, a hydroxyl group or a lower C₁-C₆alkoxy group; R² is a hydrogen atom or a lower C₁-C₆alkyl group; R³ is a hydrogen atom or a lower C₁-C₆alkyl group; R⁴ and R⁵ can be identical or different and are a hydrogen atom or a lower C₁-C₆alkyl group; R⁶ is a hydrogen atom or a lower C₁-C₆alkyl group; R⁷ is a phenyl group or a heterocyclic group which relates to a residue formed by removing a hydrogen atom from a saturated monocyclic heterocyclic ring containing one heteroatom in the ring, selected from an oxygen atom and a sulphur atom; in cases where R⁷ is a phenyl group or a heterocyclic group which relates to a residue formed by removing a hydrogen atom from a saturated monocyclic heterocyclic ring containing one heteroatom in the ring, selected from an oxygen atom and a sulphur atom, that phenyl or heterocyclic group can contain, as substitute(s), one or two groups selected from a halogen atom, a lower C₁-C₆alkyl group, a hydroxyl group, a lower C₁-C₆alkoxy group and a nitro group; W is an oxygen atom or NR⁸; R⁸ is a hydrogen atom or a lower C₁-C₆alkyl group; X is an oxygen atom or a sulphur atom; Y is a lower C₁-C₆alkylene group; Z is an oxygen atom, a sulphur atom, NR⁹ or OCO; R⁹ is a hydrogen atom or a lower C₁-C₆alkyl group. The invention also relates to a pharmaceutical composition based on said compounds, having GR binding activity.

EFFECT: obtaining novel compounds and a pharmaceutical composition based on said compounds, which can be used in medicine as glucocorticoid receptor modulators.

10 cl, 1 tbl, 3 ex