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SUBSTITUTED PYRIMIDINES AND USE THEREOF AS JNK MODULATORS
专利权人:
F.KHOFFMANN-LJA ROSH AG
发明人:
DANN Dzhejms Patrik (US),ДАНН Джеймс Патрик (US),GOLDSTEJN Dejvid Majkl (US),ГОЛДСТЕЙН Дейвид Майкл (US),GON Leji (US),ГОН Лейи (US),KhOGG Dzhoan Khiter (US),ХОГГ Джоан Хитер (US),MIShU Kristof (US),М,DANN DZHEJMS PATRIK,ДАНН Джеймс Патрик,GOLDSTEJN DEJVID MAJKL,ГОЛДСТЕЙН Дейвид Майкл,GON LEJI,ГОН Лейи,KHOGG DZHOAN KHITER,ХОГГ Джоан Хитер,MISHU KRISTOF,МИШУ Кристоф,PALMER UAJLI SOLANG,ПАЛМЕР Уайли
申请号:
RU2009125672/04
公开号:
RU0002493155C2
申请日:
2007.11.28
申请国别(地区):
RU
年份:
2013
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to novel pyrimidine derivatives of general formula (I), or pharmaceutically acceptable salts thereof, where X1 denotes N, N-R3, C-R3 or O; X2 denotes N, CH or C-CH3; X3 denotes N or C, where X1, X2 and X3 all do not simultaneously denote N; X4, X5 each independently denotes C or N; X6 denotes N or C-R1 ; where at least two and not more than four of X1, X2, X3, X4, X5 and X6 denotes N; and where the bonds between X1 and X2, X2 and X3, X3 and X4, X4 and X5, X5 and X1, as well as X5 and X6 can each independently be single or double, or , can form an aromatic ring, under the condition that a chemically stable structure is formed; R denotes -(cyclohexyl)R2; R1 denotes a halide, nitro group, -CN, -CH2CN, -OH, -NH2, -COOH or -Y1R4; Y1 denotes -O-, -SO2, -NHSO2-, -C(O)O- or a bond; R4 denotes (C1-C6)alkyl, phenyl or benzyl, each of which is substituted with 0-3 times with a hydroxy group or a halogen; n equals 0, 1 or 2; R3 denotes H or (C1-C6)alkyl; R2 denotes H, -OH, =O or -Y2-Y3-Y4-R5, where Y2 denotes -C(O)-, -C(O)NRa-, -NH- or a bond; Y3 denotes (C1-C6)alkylene or a bond; Y4 denotes -NRa-, -S-, -SO2-, -NRaC(O)-, -NHSO2- or a bond; R5 denotes (C1-C6)alkyl, (C3-C10)cycloalkyl, a 5-6-member heterocyclyl containing 1-2 heteroatoms selected from N and O, where R5 is optionally substituted with -OH or -NHRa; where each Ra independently denotes hydrogen or (C1-C6)alkyl; Z denotes hydrogen. The invention also relates to a pharmaceutical composition based on a compound of formula (I).EFFECT: obtaining novel pyrimidine derivatives which are useful for therapeutic or preventive treatment of a c-Jun N-terminal kinase-mediated disorder.14 cl, 3 tbl, 26 exНастоящее изобретение относится к области органической химии, а именно к новым производным пиримидина общей формулы (I), или к его фармацевтически приемлемым солям, где X1 обозначает N, N-R3, C-R3 или O; X2 обозначает N, CH или C-CH3; X3 обозначает N или C, где Х1, X2 и X3 все одновр
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