| 摘要 |
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 CF, C-Calkoxy and halogen; Y is selected from halogen; W denotes oxygen; Rand Rare independently selected from C-Calkyl, or Rand Rand a carbon atom, to which they are bonded, form a 3-6-member cycloalkyl ring; Adenotes phenyl or pyridyl optionally substituted with one halogen; Ais (CH)Y(CH)Q, 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(RR)C(O)NR″R″, cyano, C(O)OR″, C(O)NR″R″ and 5-member heteroaryl containing 2 heteroatoms selected from nitrogen, oxygen and sulphur; and Yis selected from a direct bond and -O-; R″ and R″ are independently selected from hydrogen, C-Calkyl, or NR″R″ 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; Rand Rare independently selected from hydrogen or methyl; or C(RR) 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 |
