THIOHYDANTOIN DERIVATIVES USEFUL AS ANDROGEN RECEPTOR ANTAGONISTS Russian patent published in 2016 - IPC C07D233/42 C07D233/86 C07D401/04 C07D401/14 C07D403/10 C07D413/10 C07D413/14 C07D417/14 A61K31/4164 A61K31/4178 A61P5/28 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, in particular to novel thiohydantoin derivatives of general formula (I) or pharmaceutically acceptable salts thereof, where Z is selected from CF₃, C₁-C₃ alkoxy and halogen; Y is selected from halogen; W denotes oxygen; R₃ and R₄ are independently selected from C₁-C₄ alkyl, or R₃ and R₄ and a carbon atom, to which they are bonded, form a 3-6-member cycloalkyl ring; A₁ denotes phenyl or pyridyl optionally substituted with one halogen; A₂ is (CH₂)_mY₁(CH₂)_nQ, where m and n are integers independently selected from 0-2, and where at least one of m or n is not equal to zero; Q is selected from C(O)NHR″, C(R_xR_y)C(O)NR″R₁″, cyano, C(O)OR″, C(O)NR″R₁″ and 5-member heteroaryl containing 2 heteroatoms selected from nitrogen, oxygen and sulphur; and Y₁ is selected from a direct bond and -O-; R″ and R₁″ are independently selected from hydrogen, C₁-C₆ alkyl, or NR″R₁″ together form a 4-6-member heterocyclic ring additionally containing 0-1 oxygen atoms, where one carbon atom can be optionally substituted with one hydroxyl group; R_x and R_y are independently selected from hydrogen or methyl; or C(R_xR_y) together form a 3-5-member cyclic alkyl ring. Invention also relates to a pharmaceutical composition and a local pharmaceutical composition based on the thiohydantoin derivative of formula (I).

EFFECT: technical result is obtaining novel thiohydantoin derivatives useful for antagonizing androgen receptor activity.

17 cl, 1 tbl, 69 ex