HYDROXAMATE DERIVATIVES SUITABLE AS DEACETYLASE INHIBITORS Russian patent published in 2007 - IPC C07D209/16 C07D403/12 C07D405/12 C07D401/12 C07D413/12 C07D471/04 C07D409/12 C07C259/06 A61K31/165 A61K31/4045 A61K31/4025 A61K31/4523 A61K31/5377 A61K31/4427 A61P35/00 

FIELD: synthesis of biologically active compounds.

SUBSTANCE: invention relates to hydroxamate derivatives described by general formula I: , in which R₁ represents H or linear C₁-C₆-alkyl; R₂ hydrogen, С₁-С₁₀-alkyl optionally substituted by 1-5 constituents selected from hydroxy, amino, hydroxyalkyl; C₄-C₉-cycloalkyl; aryl; C₄-C₉-heterocycloalkyl, C₄-C₉-heterocycloalkylalkyl containing 2 heteroatoms (nitrogen and/or oxygen); C₄-C₉-cycloalkylalkyl; arylalkyl; heteroarylalkyl containing 1-4 nitrogen atoms as heteroatoms; -(CH₂)_nC(O)R₆, -(CH₂)_nOC(O)R₆, -N(R₁₂)C(O)-W; HONH-C(O)-CH=C(R₁)arylalkyl, and (CH₂)_nR₇; R₃ and R₄, identical or different, independently denote hydrogen, optionally OH-substituted C₁-C₆-alkyl; C(O)-O-W, or -N(R₁₂)C(O)W; or R₃ and R₄ together with carbon atom, to which they are linked, represent C=O; or R₂ together with carbon atom, to which it is linked, and R₃ together with carbon atom, to which it is linked, can form C₄-C₉-heterocycloalkyl containing 2 nitrogen atoms as heteroatoms; or mixed aryl or non-aryl polyheterocyclic ring; R₅ is selected from hydrogen; C₁-C₆-alkyl; C₄-C₉-cycloalkyl; C(O)-W; aryl optionally substituted by 1-2 constituents selected from halogen and hydroxyalkyl; heteroaryl containing nitrogen as heteroatom; arylalkyl; aromatic polycycle; polyheteroaryl containing 1-2 nitrogen atoms as heteroatoms and optionally substituted by 1-2 substituents selected from hydroxyalkyl, halogen, alkyl, and aryl; mixed aryl-nonaryl polyheterocycle containing nitrogen or oxygen atom as heteroatom and optionally substituted by groups -N-OH, =N-OH; n, n₁, n₂, and n₃, identical or different, are independently selected from within a range of 0-6; X and Y, identical or different, are independently selected from hydrogen, halogen, and nitro group; or pharmaceutically acceptable salt thereof. Invention also relates to a pharmaceutical composition showing inhibitory activity toward hydroxamate derivative of general formula I in combination with one or several pharmaceutically acceptable carriers. Hydroxamate derivative of general formula I are also appropriate for treating proliferative disease and regulating p21 promoter.

EFFECT: enabled use of hydroxamate derivatives as deacetylase inhibitors.

42 cl, 6 tbl, 272 ex