DORSCH, DIETER,SIRRENBERG, CHRISTIAN,MUELLER, THOMAS J.J.,MERKUL, EUGEN,AMATUNU KARAPETYAN, GNUNI
申请号：
EP14000623.0
公开号：
EP2746281A3
申请日:
2012.01.09
申请国别(地区):
EP
年份:
2014
代理人:
摘要：
Verbindungen der Formel Iworin R, R1, R2 und R3 die in Anspruch 1 angegebenen Bedeutungen haben, sind Inhibitoren der PDK1 und der Zellproliferation/ Zellvitalität und können zur Behandlung von Tumoren eingesetzt werden.7-Azaindole derivatives (I) and their salts, tautomers or stereoisomers, including their mixtures in all ratios, are new. 7-Azaindole derivatives of formula (I) and their salts, tautomers or stereoisomers, including their mixtures in all ratios, are new. R : indazole-3-, -4- or -7-yl, imidazo[1,2-a]pyrimidin-3- or -5-yl, quinolin-4-, -5- or -8-yl, isoquinolin-1-, -4 - or -5-yl, 1H-pyrrolo [3,2-c]pyridine-3 -, -4- or -7-yl, 1H-pyrrolo[2,3-c] pyridine-3-, -4- or -7-yl, furo[2,3-c]pyridine-3-, -4- or -7- yl, furo[3,2-b]pyridine-3- or -7-yl, 2,6-naphthyridin-1-or-4-yl or amino-quinoline-4-, -5 - or -8-yl (all optionally mono- or di-substituted by R 5>；-), 1,8-naphthyridin-4-yl (optionally substituted by R 5>；at 7th position) or 1,8-naphthyridin-4-yl (optionally substituted by A, Hal, CN, -[C(R 6>；) 2] n-Cyc, OR 6>；, N(R 6>；) 2, SO 2A Or SO 2Ar 1>；)； R 1>； : H or A1a； R 2>； : H, A1a or -[C(R 6>；) 2] n-Ar 1>；； R 3>； : H, A, Hal, CN, -[C(R 6>；) 2] n-Ar 1>；, -[C(R 6>；) 2] n-Het, -[C(R 6>；) 2] n-Cyc, OR 6>；or N(R 6>；) 2； R 5>； : A, Hal, CN, -[C(R 6>；) 2] n-Ar 1>；, -[C(R 6>；) 2] n-Het, -[C(R 6>；) 2] n-Cyc, OR 6>；. N(R 6>；) 2, SO 2A or SO 2Ar 1>；； R 6>； : H or A1a； A : 1-6C-alkyl (where one or two CH 2groups are optionally replaced by O, N, S and/or -CH=CH, and 1-7 H atoms are replaced by F)； A1a : 1-4C-alkyl； Cyc : 3-7C-cycloalkyl； Ar 1>； : phenyl (optionally substituted by 1-3 Hal, A, -[C(R 6>；) 2] n-OR 6>；, N(R 6>；) 2, CN, COOR 6>；, CON(R 6>；) 2, NR 6>；COA, NR 6>；SO 2A, COR 6>；, SO 2N(R 6>；) 2and/or S(O) nA)； Het : optionally saturated mono-or bicyclic aryl heterocycle with 1-4 N, O and/or S (optionally mono- or di-substituted by Hal, A, -[C(R 6>；) 2] nOR 6>；, N(R 6>；) 2, NO 2,
