NONSTEROID COMPOUNDS EFFECTIVE AS GLUCOCORTICOID RECEPTOR MODULATORS Russian patent published in 2011 - IPC C07D471/04 A61K31/55 A61P5/44 A61P29/00 

FIELD: medicine.

SUBSTANCE: invention refers to new amino acid derivatives of formula (I), , in which R-groups have the following value: -R₁ is -H;-R₂ is -C(O)R₁₅ or -SO₂R₁₅; -R₃ is -H;-R₄ is -H or -(1-4C)alkyl; -R₆ is -H; -R₇ is -H; -R₈ is -H, cyanogroup, halogen, nitrogroup; -(1-6C)alkyl optionally substituted by amino group, hydroxyl or halogen; -heteroaryl representing a 5 or 6-members aromatic ring containing one or more heteroatoms N optionally substituted by -(1-4C) alkyl; -C(R₁₆)NOR₁₆, -C(O)N(R₁₇)₂, -C(O)R₁₈ or -C(O)OR₁₉; -R₉ is -H; -R₁₀ is -H or -(1-4C)alkyl; -R₁₁ is -H; -R₁₂ is -H; -R₁₃ is -H; -R₁₄ is -H; -R₁₅ is -H; -(1-6C)alkyl, -(2-6C)alkynyl, -O(2-6C)alkyl) all optionally substituted by one or more, halogen, cyanogroup or 5-members heteroaryl where 5-members heteroaryl represents an aromatic ring containing one or more heteroatoms selected from a group including N, O or S; -(hetero)aryl representing 5 or 6-members aromatic ring system containing one or more heteroatoms selected from group including N, O or S, optionally substituted by -(1-4C)alkyl, halogen or NH₂; -NH₂, -(di)(1-4C)alkylamihogroup, -(1-4C)alkylamihogroup or -NR₁₆OR₁₆; R₁₆ is -H or -(1-4C)alkyl; -R₁₇ is -H or -(1-6C)alkyl optionally substituted by halogen, or 5 or 6-members heteroaryl or aryl optionally substituted by halogen, -(1-4C)alkyl or -(1-4C)alkoxygroup where heteroaryl represents an aromatic ring containing one or more heteroatoms selected from the group including N, O or S; -R18 is -H or -(1-4C)alkyl; -R₁₉ is -H or -(1-6C)alkyl.

EFFECT: compounds of this invention are high-specific to glucocorticoid receptor and can be used for treating inflammatory diseases.

6 cl, 58 ex