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METHOD FOR PREPARING DIHYDROINDENAMIDE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS AND USING THEM AS PROTEIN KINASE INHIBITOR
专利权人:
KHARBIN GLORIA FARMASJUTIKALS KO.; LTD.;KHARBIN GLORIA FARMAS'JUTIKALS KO.
发明人:
JaN Sjujtsin (CN),ЯН Сюйцин (CN),SJuEh Lun (CN),СЮЭ Лун (CN),LO Tszjuan' (CN),ЛО Цзюань (CN),JAN SJUJTSIN,ЯН Сюйцин,SJUEH LUN,СЮЭ Лун,LO TSZJUAN,ЛО Цзюань
申请号:
RU2011125376/04
公开号:
RU0002528408C2
申请日:
2009.12.24
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to new dihydroindenamide specified in compounds described by general formula II, or their pharmaceutically acceptable salts. In general formula II, R1 represents piperazinyl which can be optionally substituted by one R1a; R1a represents H, CH3, C(O)Rd or C(O)ORa; Y represents pyrimidyl; Z represents pyridyl or pyrimidyl; Ra represents tert-butyl and Rd represents CH3. The above compounds represent tert-butyl-4-{5-[({(4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl}amino)carbonyl)-2,3-dihydro-1H-inden-1-yl}piperazine-1-carboxylate; N-(4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl)-1-piperazin-1-yl-2,3-dihydro-1H-indene-5-carboxamide; 1-[4-acetylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl)-2,3-dihydro-1H-inden-5-carboxamide; (1R)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl)-2,3-dihydro-1H-inden-5-carboxamide; (1S)-N-[3-(4,5′-bipyrimidin-2-ylamino)-4-methylphenyl]-1-(4-methylpiperazin-1-yl)-2,3-dihydro-1H-inden-5-carboxamide; (1R)-N-[3-(4,5′-bipyrimidin-2-ylamino)-4-methylphenyl]-1-(4-methylpiperazin-1-yl)-2,3-dihydro-1H-inden-5-carboxamide; (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-4-ylpyrimidin-2-yl)amino]phenyl)-2,3-dihydro-1H-inden-5-carboxamide and (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl)-2,3-dihydro-1H-inden-5-carboxamide sulphate.EFFECT: compounds inhibit activity of protein kinases specified in Abl, c-Kit and PDGFR, and can find application for treating diseases related to disturbed activity of the above protein kinases, eg leukaemia and other cancers.4 cl, 4 tbl, 16 exИзобретение относится к новым дигидроинденамидам, выбранным из соединений, соответствующих общей формуле II, или их фармацевтически приемлемым солям. Соединения ингибируют активность протеинкиназ, выбранных из Abl, c-Kit и PDGFR, и могут найти применение для лечения заболеваний, связан
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中国工程科技知识中心
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