发明名称 7-AZAINDOLE DERIVATIVES
摘要 Compounds of the formula (I) in which R, R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors.
申请公布号 US2016130269(A1) 申请公布日期 2016.05.12
申请号 US201614987946 申请日期 2016.01.05
申请人 MERCK PATENT GmbH 发明人 DORSCH Dieter;SIRRENBERG Christian;MUELLER Thomas J.J.;MERKUL Eugen;KARAPETYAN Gnuni Amatunu
分类号 C07D471/04 主分类号 C07D471/04
代理机构 代理人
主权项 1. A compound of the formula I wherein R denotes isoquinolin-1-, -4-, -5- or -6-yl which is unsubstituted or mono- or disubstituted by R5; R1 denotes H or A′, R2 denotes H, A′ or —[C(R6)2]n—Ar, R3 denotes H, A, Hal, CN, —[C(R6)2]n—Ar, —[C(R6)2]n-Het, —[C(R6)2]n-Cyc, OR6 or N(R6)2, R5 denotes A, Hal, CN, —[C(R6)2]n—Ar, —[C(R6)2]n-Het, —[C(R6)2]n-Cyc, OCyc, OHet′, OR6, N(R6)2, SO2A, SO2Ar or ═O, R6 denotes H or A′, A denotes unbranched or branched alkyl having 1-6 C atoms, in which one or two CH2 groups may be replaced by O, N and/or S atoms and/or by —CH═CH— groups and/or, in addition, 1-7 H atoms may be replaced by F, A′ denotes unbranched or branched alkyl having 1-4 C atoms or Cyc, Cyc denotes cycloalkyl having 3, 4, 5, 6 or 7 C atoms, Ar denotes phenyl which is unsubstituted or mono-, di- or trisubstituted by Hal, A, —[C(R6)2]nOR6, N(R6)2, NO2, CN, COOR6, CON(R6)2, NR6COA, NR6SO2A, COR6, SO2N(R6)2 and/or S(O)nA, Het denotes a mono- or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms which is unsubstituted or mono- or disubstituted by Hal, A, —[C(R6)2]nOR6, N(R6)2, NO2, CN, COOR6, CON(R6)2, NR6COA, NR6SO2A, COR6, SO2NR6 and/or S(O)nA, Het′ denotes a monocyclic saturated heterocycle having 1 or 2 N, O and/or S atoms which is unsubstituted or mono- or disubstituted by A and/or ═O, Hal denotes F, Cl, Br or I, n denotes 0, 1 or 2, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
地址 Darmstadt DE