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COMPOUND AS WNT SIGNAL INHIBITOR, ITS COMPOSITIONS AND APPLICATION
专利权人:
KYURDZHENIKS INK.
发明人:
AN Sunchzhu (CN),АНЬ Сунчжу (CN),AN Sunchzhu,АНЬ Сунчжу
申请号:
RU2014150338
公开号:
RU0002627712C2
申请日:
2012.06.15
申请国别(地区):
RU
年份:
2017
代理人:
摘要:
FIELD: pharmacology.SUBSTANCE: invention relates to a heterocyclic compound of the general formula (I) or an N-oxide thereof, wherein X1, X2, X3 and X4 independently represent CR4 or N, where0 or 1 of X1-X4 can be N; Y1, Y2 andY3 are hydrogen; R1 is selected from hydrogen, , C6 aryl, 6-member heterocycloalkyl containing 2 heteroatoms selected from N and O, and 5- or 6-member heteroaryl containing 1-4 heteroatoms selected from N, O and S, wherein eachof C6 aryl, 6-member heterocycloalkyl and 5- or 6-member heteroaryl may be optionally substituted with one R4; R2 is selected from hydrogen, halogen, C1-6 alkyl, , C6 aryl and 6-member heteroaryl containing 1 to 2 N atoms, where eachof C6 aryl and 6-member heteroaryl may be optionally substituted with oneR4. If X5 is N, R2 is selected from halogen, C1-6 alkyl, , C6 aryl and 6-member heteroaryl containing 1 to 2 N atoms, where eachof C6 aryl, and 6-member heteroaryl may be optionally substituted with one R4; each R4 Is independently selected from hydrogen, halogen, cyano, oxo, C1-6 alkoxy, -C(O)OR5, -C(O)R5,C1-6 alkyl. Moreover , C1-6 alkyl may be optionally substituted with1 to 3 substituents selected from halogen and cyano; R5 is C1-6 alkyl; and where the central structure of Formula I, limited by X5, X6, X7 andX8, is:orThe invention also relates to particular compounds, a method for inhibiting the secretion of WNT signalling in a cell, use of a compound of formula (I), a method for treatment of a disorder mediated by WNT. .EFFECT: new heterocyclic compounds have been obtained that are useful for treatment of cancer, fibrosis and osteoarthritis.22 clНастоящее изобретение относится к области органической химии, а именно к гетероциклическому соединению общей формулой (I) или его N-оксиду, где X1, Х2, Х3 и Х4 независимо представляют собой CR4 или N, где 0 или 1 из X1-X4 может представлять собой N; Y1, Y2 и Y3 представляют собой водород; R1 выбран из водорода, , С6 арила, 6-членного гетероциклоалкила, содержащего 2 гетероат
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