KALDARELLI Marina (IT),КАЛЬДАРЕЛЛИ Марина (IT),ANDZHOLINI Mauro (IT),АНДЖОЛИНИ Мауро (IT),BERIYA Italo (IT),БЕРИЯ Итало (IT),BRASKA Mariya Gabriella (IT),БРАСКА Мария Габриелла (IT),KAZUSHELLI Franche,KALDARELLI MARINA,КАЛЬДАРЕЛЛИ Марина,ANDZHOLINI MAURO,АНДЖОЛИНИ Мауро,BERIYA ITALO,БЕРИЯ Итало,BRASKA MARIYA GABRIELLA,БРАСКА Мария Габриелла,KAZUSHELLI FRANCHESKO,КАЗУШЕЛЛИ Франческо,DALESSIO ROBERTO
申请号：
RU2013139353/04
公开号：
RU0002591191C2
申请日:
2012.01.19
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
FIELD: chemistry.SUBSTANCE: present invention relates to novel tricyclic pyrrole derivatives of formula (I) or pharmaceutically acceptable salts thereof, which modulate protein kinase activity, selected from MPS1, PIM-1 and PIM-2. Compounds can be used in treating diseases caused by impaired protein kinase activity regulation. Such diseases can be selected from ovarian cancer, breast cancer, melanoma, colon cancer, leukaemia, pancreatic cancer and myeloma. In formula (I) , where R1 denotes hydrogen, straight or branched C1-C6alkyl or aryl, selected from phenyl, containing substitutes, selected from halogen atoms, C1-C6alkoxy, C1-C6alkyl, diC1-C6alkylamino, 6-member heterocyclyl, containing one or two nitrogen atoms in the cycle, and optionally substituted in its turn C1-C6alkyl, 5-member heterocyclyl, containing one nitrogen atom, di(C1-C6alkyl)amino, [di(C1-C6alkyl)aminoC1-C6alkyl](C1-C6alkyl)amino, gihyroxyC1-C6alkyl； R2 means group of -NR″R′″, where R″ and R′″ both denote hydrogen or straight or branched C1-C6 alkyl, or one of R″ and R′″ denotes hydrogen, and the other is selected from C1-C6alkyl, substituted phenyl and 2,3-dioxo-1,3-dihydro-2H-isoindol-2-yl； and aryl, which is a phenyl substituted C1-C6alkyl C1-C6alkoxy； R3 is selected from hydrogen； straight or branched C1-C6alkyl, optionally substituted amino； hydroxyC1-C6alkyl； C1-C6alkoxyC1-C6alkyl； 6-7-membered heterocyclil containing nitrogen atom as heteroatoms and optionally substituted C1-C6alkoxycarbonyl； and C3-C6cycloalkyl, optionally substituted amino； R4 denotes hydrogen or straight or branched C1-C6alkyl； X denotes group selected from -NR′- and -S-, where R′ denotes hydrogen； A denotes group selected from -(CH2)3-, -(CH2)2- and -CH=CH-.EFFECT: invention also describes method of producing compounds.8 cl, 4 tbl, 32 exНастоящее изобретение относится к новым трициклическим производным пиррола формулы (I) или их фармацевтически приемлемым солям, которые модулируют активность протеинкиназ, выбранных и
