TUN YUchzhi (CN),ТУН Ючжи (CN),TUN YUchzhi,ТУН Ючжи
申请号：
RU2014138827/04
公开号：
RU0002598854C2
申请日:
2012.03.08
申请国别(地区):
RU
年份:
2016
代理人:
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 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(RxRy)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； Rx and Ry are independently selected from hydrogen or methyl； or C(RxRy) 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 exИзобретение относится к области органической химии, а именно к новым производным тиогидантоина общей формулы (I) или к их фармацевтически приемлемым солям, где Z выбирают из CF3, С1-С3 алкокси и галогена； Y выбирают из галогена； W означает кислород； R3 и R4 независимо выбирают из С1-С4 алкила, или R3 и R4 и атом углерода, к которому они присоединены, образуют 3-6-членное циклоалкильное кольцо； A1 представляет собой фенил или пиридил, необязательно замещенные одним галогеном； А2 является (СН
