2-AMINO-4-PHENYLAZOLINE DERIVATIVES AND USE THEREOF AS HSP90 MODULATORS Russian patent published in 2011 - IPC C07D239/84 C07D401/12 C07D403/12 A61K31/517 A61P35/00 A61P31/12 A61P17/00 A61P17/06 A61P19/02 A61P25/28 A61P3/10 A61P1/16 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula I, which are HSP90 (heat-shock proteins) inhibitors and can be used to prepare a medicinal agent for treating tumorous diseases affected by HSP90 inhibition. In formula I R¹ denotes Hal, H, OA or A, R², R³ each independently denotes -O-(X)_s-Q, -NHCO-(X)_s-Q, -CONH-(X)_s-Q, -NH(CO)NH-(X)_s-Q, -NH(CO)O-(X)_s-Q, -NHSOr(X)_s-Q, NHCOA, Hal, Het or H, where, if R²=H, then R³≠H, or if R³=H, then R²≠H, R⁴ denotes H, R⁵ denotes H, Hal, A, OA, (CH₂)_nCOOH, (CH₂)_nCOOA, O(CH₂)_oCONH₂, NHCOOA, NHCO(CH₂)_nNH₂, NHCONHA or O(CH₂)_oHet¹, A denotes a straight or branched alkyl containing 1-10 carbon atoms, in which 1-5 hydrogen atoms may be substituted with F, Cl and/or Br, X denotes a straight or branched C₁-C₁₀ alkylene which is unsubstituted or substituted once, twice or thrice by A, O A, OH, Hal, CN, COOH, COOA, CONH₂, NH₂, NHCOA, NHCOOA, Q denotes H, Ar or Het, Ar denotes phenyl which is unsubstituted or substituted once, twice or thrice with A, OA, OH, NO₂, Hal, CN, (CH₂)_nCOOH, (CH₂)_nCOOA and/or tetrazole, Het denotes a cyclic saturated or aromatic 5-6-member heterocycle containing 1-2 N and/or O atoms, optionally condensed with a benzene ring which may be substituted once, twice or thrice with A, OA, OH and/or =O (carbonyl oxygen), Het¹ denotes a monocyclic saturated, unsaturated or aromatic heterocycle containing 1-2 N and/or O atoms, which may be mono- or disubstituted with A, OA, OH, Hal and/or =O (carbonyl oxygen), Hal denotes F, Cl, Br or I, n equals , 1, 2, 3 or 4, o equals 1, 2 or 3, s equals 0, 1 or 2.

EFFECT: high efficiency of using said derivatives.

4 cl, 4 dwg, 1 tbl, 29 ex